Hyperuricemia(HUA)is a metabolic disease characterized by high levels of uric acid(UA)in the blood and varying degrees of kidney damage.Desirable nanoliposomes should simultaneously exhibit efficient biocompatibility ...Hyperuricemia(HUA)is a metabolic disease characterized by high levels of uric acid(UA)in the blood and varying degrees of kidney damage.Desirable nanoliposomes should simultaneously exhibit efficient biocompatibility and effective drug delivery.However,they both usually require special structural properties.Herein,we propose a strategy to prepare nanoliposomes with varying rigidity by replacing cholesterol(CH)with phytosterol esters(PE).The results showed that the particle size of PE naringenin nanoliposomes(PE-NAR)was 179.5 nm,and the encapsulation efficiency(EE)was 79.93%.In atomic force microscopy(AFM)tests,PE-NAR showed a 1-fold increase in rigidity compared to CH naringenin nanoliposomes(CH-NAR).By observing the effects of naringenin nanoliposomes(NAR-NLs)on the physiological and biochemical indicators in HUA mice,we explore its impact on kidney damage and inflammatory pathways in HUA mice.The results show that NAR-NLs significantly inhibit UA levels and improve kidney damage.Compared to oral naringenin,NAR-NLs generally enhance the in vivo antioxidant effects of naringenin.Furthermore,high-rigidity PE-NAR downregulated the renal inflammatory factor interleukin-1β(IL-1β)to 6.67%,demonstrating the highest inhibitory effect.Further experiments have demonstrated that naringenin exerts a protective effect in kidney injury by inhibiting the activation of NOD like receptor protein 3(NLRP3)inflammasome and reducing oxidative stress within the body.In summary,by adjusting the rigidity of the nanoliposomes,the oral administration of naringenin can effectively improve the alleviation of HUA.展开更多
Previous studies have shown that berberine has neuroprotective effects against Alzheimer’s disease,including antagonizing tau phosphorylation,and inhibiting acetylcholinesterase activity and neural cell apoptosis.How...Previous studies have shown that berberine has neuroprotective effects against Alzheimer’s disease,including antagonizing tau phosphorylation,and inhibiting acetylcholinesterase activity and neural cell apoptosis.However,its low bioavailability and adverse reactions with conventional administration limit its clinical application.In this study,we prepared berberine nanoliposomes using liposomes characterized by low toxicity,high entrapment efficiency,and biodegradability,and modified them with lactoferrin.Lactoferrin-modified berberine nanoliposomes had uniform particle size and high entrapment efficiency.We used the lactoferrin-modified berberine nanoliposomes to treat a mouse model of Alzheimer’s disease established by injection of amyloid-beta 1-42 into the lateral ventricle.Lactoferrin-modified berberine nanoliposomes inhibited acetylcholinesterase activity and apoptosis in the hippocampus,reduced tau over-phosphorylation in the cerebral cortex,and improved mouse behavior.These findings suggest that modification with lactoferrin can enhance the neuroprotective effects of berberine nanoliposomes in Alzheimer’s disease.展开更多
Light-responsive carriers have been used for the controlled release of antitumor drugs in recent years.However, most light-responsive vectors require high-energy ultraviolet or visible light to achieve local drug rele...Light-responsive carriers have been used for the controlled release of antitumor drugs in recent years.However, most light-responsive vectors require high-energy ultraviolet or visible light to achieve local drug release, and ultraviolet light would cause cellular damage. Near-infrared light has a deeper tissuepenetration depths and minimal harm to tissues, but it is difficult to cleave the chemical bond directly.The aim of this study is to develop a novel near-infrared light-responsive carrier for local release of antitumor drugs. Unsaturated phospholipids can be oxidized by singlet oxygen to achieve liposomal drug release, and singlet oxygen can be produced by photosensitizer under light irradiation. A new near-infrared light-responsive nanoliposome was designed that imparts light-triggered local drug release. Nanoliposomes, which were composed of matrix phospholipids and unsaturated phospholipids, were prepared by ammonium sulfate gradient method, and loaded with antitumor drug doxorubicin(DOX) and photosensitizer 1,4,8,11,15,18,22,25-octabutoxypalladium phthalocyanine. Under near-infrared light, photosensitizers could produce singlet oxygen and damage tumor cells by photodynamic therapy. Simultaneously, the unsaturated phospholipids were oxidized by singlet oxygen and result in DOX release, causing sustained cell damage by chemotherapy. Near-infrared light-responsive nanoliposomes exhibit enhanced anticancer activity owing to combined treatment of photodynamic therapy and chemotherapy. A new platform is thus offered for designing effective intracellular drug-release systems, holding great promise for future cancer therapy.展开更多
The objective of this study is to compare the targeting ability of activated carbon nanoparticles and nanoliposomes,which are used as carriers for delivering docetaxel(DTX)to the metastatic lymph nodes.In this study,w...The objective of this study is to compare the targeting ability of activated carbon nanoparticles and nanoliposomes,which are used as carriers for delivering docetaxel(DTX)to the metastatic lymph nodes.In this study,we first prepared the DTX-loaded activated carbon nanoparticles(DTX-AC-NPs)by modifying the activated carbon with nitric acid oxidation and absorbing DTX in the concentrated nitro-oxide nanocarbon.We then prepared DTX-loaded nanoliposomes(DTX-LPs)by the proliposome method.The physiochemical properties of DTX-AC-NPs and DTX-LPs were carefully evaluated in vitro.The metastatic lymph node uptake and the injection site retention were investigated by analyzing the DTX concentration in metastatic lymph nodes and injection sites.The result showed that DTX-AC-NPs and DTX-LPs with suitable and stable physicochemical properties could be used for in vivo lymph node targeting studies.DTX-AC-NPs significantly increased DTX-AUC_((0-24)) and prolonged DTX-retention in metastatic lymph nodes compared to DTX-LPs and non-modified activate carbon in vivo.This study demonstrated activated carbon nanoparticles may be potential intralymphatic drug delivery system to preferentially target regional metastatic lymph nodes.展开更多
The encapsulation of an antimicrobial formulation based on essential oils(EOs)and citrus extract(CE)mixture into nanoemulsion(NE),gelled emulsion(GE),and nanoliposomes(NL)was performed.The encapsulation forms(NE,GE,an...The encapsulation of an antimicrobial formulation based on essential oils(EOs)and citrus extract(CE)mixture into nanoemulsion(NE),gelled emulsion(GE),and nanoliposomes(NL)was performed.The encapsulation forms(NE,GE,and NL)were evaluated further for their stability,encapsulation efficiency(EE),controlled release of bioactive ingredients,in vitro and in situ antimicrobial activity.Results showed that all colloidal systems exhibited similar stability behaviors.Among all colloidal systems,NL witnessed the smallest particle size(91.9 nm)with the lowest polydispersity index(0.230)and highest zeta potential(36 mV)NL has retained the antimicrobial formulation longer,controlled the release over time,and maintained the total phenolic content.The in vitro results showed that GE improved the antimicrobial activity against Escherichia coli,Listeria monocytogenes,Bacillus subtilis,Candida albicans,and Aspergillus flavus.In situ,the test exhibited that GE applied on the bread surface extended the shelf-life and delayed Bacillus subtilis proliferation to 36 days without affecting the sensory properties of baked bread compared to 14 and 24 days in the non-treated group and treated group with sorbate,a chemical additive widely used in bakery products.Consequently,encapsulating natural antimicrobials represents an exciting process that could improve the bioactivity and shelf-life extension of the bread.展开更多
Nanoliposomes have a broad range of applications in the treatment of autoimmune inflammatory diseases because of their ability to considerably enhance drug transport.For their clinical application,nanoliposomes must b...Nanoliposomes have a broad range of applications in the treatment of autoimmune inflammatory diseases because of their ability to considerably enhance drug transport.For their clinical application,nanoliposomes must be able to realize on-demand release of drugs at disease sites to maximize drug-delivery efficacy and minimize side effects.Therefore,responsive drug-release strategies for inflammation treatment have been explored;however,no specific design has been realized for a responsive drug-delivery system based on pyroptosis-related inflammation.Herein,we report a pioneering strategy for self-adaptive pyroptosis-responsive liposomes(R8-cardiolipin-containing nanoliposomes encapsulating dimethyl fumarate,RC-NL@DMF)that pre-cisely release encapsulated anti-pyroptotic drugs into pyroptotic cells.The activated key pyroptotic protein,the N-terminal domain of gasdermin E,selectively integrates with the cardiolipin of liposomes,thus forming pores for controlled drug release,pyroptosis,and inflammation inhibition.Therefore,RC-NL@DMF exhibited effective therapeutic efficacies to alleviate autoimmune inflammatory damages in zymosan-induced arthritis mice and dextran sulfate sodium-induced inflammatory bowel disease mice.Our novel approach holds great promise for self-adaptive pyroptosis-responsive on-demand drug delivery,suppressing pyroptosis and treating autoimmune inflammatory diseases.展开更多
Nanoliposomes are bilayer phospholipid vesicles used to encapsulate and deliver therapeutic agents.The study was aimed to investigate the effects of critical variables on nanoliposomes characteristics.Imatinib mesylat...Nanoliposomes are bilayer phospholipid vesicles used to encapsulate and deliver therapeutic agents.The study was aimed to investigate the effects of critical variables on nanoliposomes characteristics.Imatinib mesylate-loaded nanoliposomes were formulated by the two-step emulsification process using a high-speed homogenizer system and probe-type ultrasonicator.The Box-Behnken design was utilized to optimize the process parameters.The mean particle size of nanoliposomes was found to be 211 nm to 623.3 nm with a low value of polydispersity index(0.005 to 0.7).Zeta potential values varied from‒27.6 mV to‒9.2 mV in uncoated nanoliposomes to+27.5 mV in chitosan-coated nanoliposomes.The encapsulation efficiency in formulation NLP-H8 containing 200 mg of phosphatidylcholine,homogenization speed of 12000 rpm,and 7 min of sonication time was found to be 76.49%without the coating and 85.4%in 0.2%w/v chitosan-coated nanoliposomes.TEM image confirmed the spherical shape of nanoliposomes.In-vitro drug release study demonstrated that the optimized nanoliposomal formulations released 84.67%of the loaded drug after 24 h in 0.1 N HCl.The IC_(50)value of formulation NLP-H8 was found to be 7.98μM.Nanoliposomal formulations were prepared successfully with suitable size,morphology,encapsulation efficiency,and drug release.The models developed in this study may be utilized further as a response surface for the various parameters of nanoliposomes.展开更多
The present study focuses on optimizing the preparation conditions of coenzyme Q10(CoQ10)-loaded liposomes(LPs),aiming to overcome the limitations of conventional LPs.Cholesterol,commonly used for LPs stabilization,pr...The present study focuses on optimizing the preparation conditions of coenzyme Q10(CoQ10)-loaded liposomes(LPs),aiming to overcome the limitations of conventional LPs.Cholesterol,commonly used for LPs stabilization,prompts exploration of alternative phytosterols due to its health concerns.This study evaluates the optimal concentrations of cholesterol andβ-sitosterol,along with CoQ10 by analyzing their effects on particle size and entrapment efficiency(EE)using response surface methodology.It further investigates how cholesterol andβ-sitosterol impact key physicochemical attributes,including lipid oxidation stability,cellular adhesion property,and cellular antioxidant activity.Incorporating cholesterol led to increased particle size but decreased CoQ10-loaded LPs’EE.Conversely,β-sitosterol incorporation increased both particle size and EE.The optimal sterol,including cholesterol andβ-sitosterol,and CoQ10 concentration was 0.605 and 0.150 mg/mL,respectively.Notably,significant differences between cholesterol andβ-sitosterol exhibited in lipid oxidation stability and cellular antioxidant activity of CoQ10-loaded LPs prepared with optimal conditions(p<0.05).Under heat treatment at 60℃ for 2 h,β-sitosterol-containing LPs suppressed malondialdehyde production approximately 15%more effectively than cholesterol-containing LPs.Moreover,β-sitosterol elevated cellular antioxidant activity by around 11%in Caco-2 monolayers compared to cholesterol.These findings highlightβ-sitosterol’s potential to enhance CoQ10-loaded LPs’physicochemical attributes,proposing applications for cholesterol-free,stable LPs with improved bioactivity in the food and pharmaceutical industries.展开更多
Background:Diquat,a commonly employed bipyridyl herbicide,is recognized for its hepatotoxic effects attributed to the generation of reactive oxygen species.Baicalin(BAI),a flavonoid derivative,has garnered significant...Background:Diquat,a commonly employed bipyridyl herbicide,is recognized for its hepatotoxic effects attributed to the generation of reactive oxygen species.Baicalin(BAI),a flavonoid derivative,has garnered significant research interest for its hepatoprotective properties.Nevertheless,the clinical application of BAI is constrained by its limited water solubility and poor bioavailability.To address these challenges,BAI-nanoliposome(BAI-NL)has emerged as a novel drug delivery platform aimed at enhancing therapeutic outcomes.Methods:We used diquat-induced liver injury mouse model and AML12 hepatocytes to test the pro-tective effect of BAI and BAI-NL on liver inflammation,oxidative stress,and mitochondrial function.The parameters included histological,biochemical,and molecular biological analyses.Results:In the diquat-induced model,both BAI and BAI-NL exhibited effectiveness on attenuating liver inflammation.Ex vivo analyses further indicated that BAI-NL was superior to BAI in preserving mito-chondrial membrane potential,reducing oxidative stress,and modulating the phosphatase and tensin homolog-induced putative kinase 1(PINK1)/Parkin RBR E3 ubiquitin-protein ligase(Parkin)signaling pathway.These findings enhanced mitophagy and facilitated the removal of damaged mitochondria.Conclusions:BAI-NL exhibited superior hepatoprotective effects compared to free BAI,possibly by re-ducing inflammation,preserving mitochondrial homeostasis,and reinstating autophagic balance through modulation of the PINK1/Parkin signaling pathway.These outcomes indicate a groundbreaking method for addressing liver diseases and underscore the potential of nanoliposome technology in augmenting the efficacy of natural compounds.展开更多
Immunotherapy with interleukin-2(IL-2)in treating cancers is subject to several limitations such as systemic side effects and reduced efficacy against tumors with low immune cell infiltration despite its promise.To ad...Immunotherapy with interleukin-2(IL-2)in treating cancers is subject to several limitations such as systemic side effects and reduced efficacy against tumors with low immune cell infiltration despite its promise.To address these challenges,IL-2-So-Lipo,a novel liposomal formulation combining IL-2 with sorafenib derivative,was developed as an anti-angiogenic drug that inhibits the growth of new blood vessels which play crucial roles in tumor growth.Sorafenib derivatives could target at melanoma-specific receptors,further enhancing liposomal specificity at the tumor site.Our results demonstrated that the prepared IL-2-So-Lipo significantly enhanced anti-tumor activity compared to IL-2 or sorafenib monotherapies,as well as their combination.In a B16F10 melanoma model,IL-2-So-Lipo was found to significantly inhibit tumor progression(tumor volume of 108.01±62.99 mm^(3))compared to the control group(tumor volume of 1,397.13±75.55 mm^(3)),improving the therapeutic efficacy.This enhanced efficacy is attributed to the targeted delivery of IL-2 which promoted the infiltration and activation of cytotoxic T lymphocytes.Additionally,liposomal encapsulation of sorafenib derivatives enhanced its delivery efficiency,promoting tumor cell apoptosis and suppressing angiogenesis.Mechanistically,IL-2-So-Lipo could kill tumors by inducing a shift towards an anti-tumor immune response via facilitating the polarization of macrophages towards the M1 phenotype.Furthermore,IL-2-So-Lipo downregulated several key proteins in the MAPK signaling pathway,exerting a significant role in mediating tumor resistance to sorafenib.These findings underscore the potential of IL-2-So-Lipo as a promising strategy to improve the therapeutic efficacy of immunotherapy and targeted therapy in cancers.Moreover,the combination of IL-2 and sorafenib in a liposomal delivery system overcame the limitations of conventional IL-2 therapy,offering a synergistic approach to improve therapeutic outcomes for solid tumors.展开更多
Conventional nutritional supplements frequently demonstrate limited clinical effectiveness due to the harsh milieu of the gastrointestinal tract,inefficient transepithelial transport,and rapid systemic clearance.Nanol...Conventional nutritional supplements frequently demonstrate limited clinical effectiveness due to the harsh milieu of the gastrointestinal tract,inefficient transepithelial transport,and rapid systemic clearance.Nanoliposomal delivery platforms-lipid bilayer vesicles on the nanometer scale-have attracted attention as an adaptive strategy to shield sensitive nutrients,navigate biological barriers,and deliver payloads directly to target tissues or even sub-cellular organelles.Despite a growing body of literature,a consolidated appraisal of design principles,targeting modalities,and translational hurdles is still needed to guide future nutraceutical innovation.We aim to:(1)Summarize the physicochemical foundations of nanoliposomal nutrient carriers;(2)Delineate state-of-the-art approaches for organ-specific and organelle-specific targeting,with particular emphasis on renal and mitochondrial delivery;(3)Evaluate current evidence supporting therapeutic benefits in cardiometabolic,neuroprotective,and renal-repair contexts;and(4)Map unresolved challenges-including manufacturing scale-up,cost,and regulatory oversight-to inform a roadmap for clinical translation.A systematic literature search was performed across PubMed,Web of Science,and Scopus through May 2025 using Boolean combinations of“nanoliposome”,“nutrient”,“targeted delivery”,“bioavailability”,and organ-specific terms(e.g.,“kidney”,“mitochondria”).Primary research articles,systematic reviews,and relevant meta-analyses written in English were included.Data were extracted on liposomal composition,particle size,surface modifications(e.g.,polyethylene glycol,ligand conjugation),in vitro and in vivo bio-distribution,efficacy outcomes,and safety profiles.Key design variables were mapped against reported biological performance to identify convergent principles.Sixty-four original studies and twenty-one reviews met inclusion criteria.Encapsulation within phosphatidylcholine-rich bilayers consistently enhanced nutrient stability in simulated gastric fluid and improved Caco-2 trans-epithelial transport two-fold to ten-fold compared with free compound controls.Ligand-mediated strategies-such as folate,lactoferrin,or peptide conjugation-achieved organ-specific accumulation,with kidney-directed liposomes demonstrating up to a four-fold increase in renal cortex uptake.Mitochondrial targeting using amphipathic peptides(e.g.,SS-31)or triphenylphosphonium moieties delivered antioxidant nutrients to the organelle,restoring mitochondrial membrane potential and reducing reactive oxygen species(ROS)in preclinical cardiomyopathy and neurodegeneration models.Endosomal escape was most effectively triggered by fusogenic lipids(e.g.,dioleoylphosphatidylethanolamine)or pH-responsive polymers.PEGylation prolonged circulation half-life by 3-6 hours but elicited anti-polyethylene glycol antibodies in approximately one-quarter of recipients;emerging natural sterol-mimetic or collagen-mimetic coatings showed comparable stealth behavior with superior biodegradability.Scalability remains limited:Only three studies reported pilot-scale(>10 L)batches with Good Manufacturing Practice-compliant reproducibility.Targeted nanoliposomal systems substantially improve nutrient stability,absorption,and tissue specificity,offering a credible route to transform supplement efficacy for cardiometabolic,renal,and neuroprotective indications.Optimization of lipid composition,escape mechanisms,and biocompatible surface chemistries can further enhance therapeutic indices.Nonetheless,industrial-scale manufacturing,cost containment,and immunogenicity mitigation remain critical obstacles.Addressing these gaps through standardized characterization protocols,head-to-head clinical trials,and biomaterial innovation will be essential to unlock the full potential of nanoliposomal nutraceuticals in routine healthcare practice.展开更多
Although the appearance of Doxil alleviated the cardiotoxicity of DOX, the progression-free survival of patients was not prolonged compared with traditional medication regimens, and side effects such as hand-foot synd...Although the appearance of Doxil alleviated the cardiotoxicity of DOX, the progression-free survival of patients was not prolonged compared with traditional medication regimens, and side effects such as hand-foot syndrome has occurred. In order to solve this dilemma, we have designed a novel co-delivery strategy to construct a co-loaded liposome of berberine(BER) and doxorubicin(DOX), which was called Lipo Be Do. The optimal synergistic ratio of the two drugs was screened by cell cytotoxicity experiments in vitro, and the optimal attenuation ratio was further determined by in vivo cardiac H&E staining pathological sections. The optimal combination treatment caused a robust increase in apoptotic cells of 4T1, as compared to drug alone treatment. The prepared co-loaded liposome, Lipo Be Do, had high encapsulation efficiency and good stability. The nanoliposome carrier controlled the biological fate of the drugs and maintained a pre-defined optimal ratio in vivo. The Lipo Be Do significantly inhibited tumor growth in 4T1 murine mammary carcinoma model compared with Doxil(P < 0.05), and completely overcame the myocardial rupture toxicity caused by Doxil in mice. Our co-loaded liposome delivery platform technology provided a new direction for the clinical treatment of triple-negative breast cancer and the safe application of DOX.展开更多
Psoriasis is an inflammatory skin disease that is intricately linked to oxidative stress.Antioxidation and inhibition of abnormal proliferation of keratinocytes are pivotal strategies for psoriasis.Delivering drugs wi...Psoriasis is an inflammatory skin disease that is intricately linked to oxidative stress.Antioxidation and inhibition of abnormal proliferation of keratinocytes are pivotal strategies for psoriasis.Delivering drugs with these effects to the site of skin lesions is a challenge that needs to be solved.Herein,we reported a nanotransdermal delivery system composed of all-trans retinoic acid(TRA),triphenylphosphine(TPP)-modified cerium oxide(CeO2)nanoparticles,flexible nanoliposomes and gels(TCeO_(2)-TRA-FNL-Gel).The results revealed that TCeO_(2)synthesized by the anti-micelle method,with a size of approximately 5 nm,possessed excellent mitochondrial targeting ability and valence conversion capability related to scavenging reactive oxygen species(ROS).TCeO_(2)-TRA-FNL prepared by the film dispersion method,with a size of approximately 70 nm,showed high drug encapsulation efficiency(>96%).TCeO_(2)-TRA-FNL-Gel further showed sustained drug release behaviors,great transdermal permeation ability,and greater skin retention than the free TRA.The results of in vitro EGF-induced and H2O2-induced models suggested that TCeO_(2)-TRA-FNL effectively reduced the level of inflammation and alleviated oxidative stress in HaCat cells.The results of in vivo imiquimod(IMQ)-induced model indicated that TCeO_(2)-TRA-FNL-Gel could greatly alleviate the psoriasis symptoms.In summary,the transdermal drug delivery system designed in this study has shown excellent therapeutic effects on psoriasis and is prospective for the safe and accurate therapy of psoriasis.展开更多
Pancreatic cancer is one of the leading causes of cancer death worldwide.Adjuvant chemotherapy has been developed based on the experiences made with palliative chemotherapy, and advocated to improve long-term survival...Pancreatic cancer is one of the leading causes of cancer death worldwide.Adjuvant chemotherapy has been developed based on the experiences made with palliative chemotherapy, and advocated to improve long-term survival of patients with this disease. However, the optimal chemotherapeutic regimen remains controversial. Recently, Conroy et al demonstrated the impressive benefits of modified FOLFIRINOX over gemcitabine alone in the multicenter Partenariat de Recherche en Oncologie Digestive 24(PRODIGE-24) trial. The remarkable results mark a new milestone in treating resectable pancreatic cancer and have now changed the standard of care for this patient population. In this commentary, we discuss an issue of difference of tumor grade between the PRODIGE-24 trial and previous phase III trials. We also discuss potential biomarkers predicting therapeutic response to modified FOLFIRINOX. Finally,we summarize several ongoing clinical trials of replacing part of the FOLFIRINOX regimen with Xeloda/S-1/nanoliposomal irinotecan for pancreatic cancer.展开更多
Crocetin displays strong antioxidant,anti-inflammatory and anti-depression activity which is promising to relieve symptoms of fatigue.As a carotenoid,crocetin is difficult to dissolve in water and highly unstable agai...Crocetin displays strong antioxidant,anti-inflammatory and anti-depression activity which is promising to relieve symptoms of fatigue.As a carotenoid,crocetin is difficult to dissolve in water and highly unstable against many environmental factors.Nanoliposome is used to encapsulate crocetin to improve its water dispersion.In the present study,the antifatigue activities and potential mechanism of crocetin loaded nanoliposome(CLN)was extensively investigated.The potential antifatigue pathway of CLN was analyzed.Furthermore,impact of CLN on the gut microbiota structure was examined which contributes to its antifatigue functions.CLN significantly increases exhaustive swimming time of fatigue mice,decreases the blood contents of lactic,blood urea nitrogen(BUN)and malondialdehyde(MDA).At the same time,CLN improves the activity of glutathione peroxidase(GSH-Px)and succinate dehydrogenase(SDH)enzyme,attenuates the oxidant stress in mice.CLN activates the adenosine monophosphate-activated kinase(AMPK)/peroxisome proliferator-activated receptor gamma coactivator-1α(PGC-1α)signaling pathway of fatigue mice,increases the mRNA expression of ATP synthase.It also increases mRNA expression of mitochondrial transcription factor A(TFAM)which promotes mitochondrial biogenesis.Additionally,CLN ameliorates the gut microbiota structure by increasing the abundance of genus such as Lactobacillus in fatigue mice.In summary,CLN exerts strong anti-fatigue properties by decreasing the oxidant stress and the contents of harmful metabolites,augmenting the production of ATP,and potentially ameliorating the gut microbiota structure.展开更多
Liposome, albumin and polymer polyethylene glycol are nanovector formulations successfully developed for anti-cancer drug delivery. There are significant differences in pharmacokinetics, efficacy and toxicity between ...Liposome, albumin and polymer polyethylene glycol are nanovector formulations successfully developed for anti-cancer drug delivery. There are significant differences in pharmacokinetics, efficacy and toxicity between pre- and post-nanovector modification. The alteration in clinical pharmacology is instrumental for the future development of nanovector-based anticancer therapeutics. We have reviewed the results of clinical studies and translational research in nanovectorbased anti-cancer therapeutics in advanced pancreatic adenocarcinoma, including nanoparticle albumin-bound paclitaxel and nanoliposomal irinotecan. Furthermore, we have appraised the ongoing studies incorporating novel agents with nanomedicines in the treatment of pancreatic adenocarcinoma.展开更多
Nanoliposome is a useful dosage form to increase solubility and absorption of simvastatin(SMV), and consequently improves its therapeutic effects. However, in vivo toxicity of SMV could also be elevated accompanied by...Nanoliposome is a useful dosage form to increase solubility and absorption of simvastatin(SMV), and consequently improves its therapeutic effects. However, in vivo toxicity of SMV could also be elevated accompanied by the absorption enhancement, which is a decisive factor for the clinical application of SMV nanoliposome(SMV-Lipo), but has not been studied systematically and reported so far. In this study, organ toxicity of SMV-Lipo was evaluated in mice in the presence and absence of isoproterenol and compared to those of free SMV. Results demonstrated that compared to free SMV, the SMV-Lipo administrated at an equal dose of 25 mg/kg/d led to severe myocardiotoxicity, hepatotoxicity at baseline and more pronounced liver injury with elevation of alanine aminotransferase. In addition, muscular adverse effect was also observed in SMV-Lipo treated group but not in SMV group. Pharmacokinetic studies revealed that compared to free SMV, the SMV-Lipo administration significantly improved the plasma SMV concentration, and the oral bioavailability was 6.5 times of free SMV. Notably, when the dosage of free SMV increased to 50 mg/kg/d, yielding the comparable plasma concentration as SMV-Lipo given at 25 mg/kg/d, the myocardiotoxicity was observed in free SMV treated mice as well, which further confirmed that the enhanced absorption of SMV by the nanoliposomal formulation resulted in more severe myocardiotoxicity than the equal dose of free SMV.展开更多
Catechin(CTC)is a phenolic active compound with multiple biological activities.However,CTC is relatively unstable,easily oxidized and poorly soluble in water,showing limited bioavailability,which is a challenge for it...Catechin(CTC)is a phenolic active compound with multiple biological activities.However,CTC is relatively unstable,easily oxidized and poorly soluble in water,showing limited bioavailability,which is a challenge for its application in the pharmaceutical and food industry.The purpose of this study was to promote the controlled release of CTC in the simulated gastrointestinal(GI)tract by using biopolymer-coupled nanoliposomes(NL).The nanoliposome was characterized by multifunctional polycrystalline X-ray diffraction(XRD),and Fourier transform infrared spectroscopy(FTIR).The results exhibited that the size of the nanocarrier was in the range of 87-178 nm,the encapsulation efficiency of CTC was 93.5%,and the combination of chitosan(CS)and alginate(ALG)was better than that of monopolymer.In vitro digestion studies showed that ALG-CS-NL significantly controlled the release of CTC by the diffusion,dissolution,and slow release mechanism and retained about 33%-37%of CTC under the GI condition.These results demonstrated that ALG-CS-NL could increase the stability of CTC,which may be important for the development of nutraceutical-enriched functional foods.展开更多
Sanghuangporus vaninii as a valuable edible fungus represents a high source of polyphenols with multidimensional bioactivities.However,the conundrum of the oral bioavailability of polyphenols limits its biological act...Sanghuangporus vaninii as a valuable edible fungus represents a high source of polyphenols with multidimensional bioactivities.However,the conundrum of the oral bioavailability of polyphenols limits its biological activity.Therefore,a strategy of nanoliposome was employed to enhance oral bioavailability of polyphenols from S.vaninii.In this study,a polyphenol component(PV5)with excellent inhibition of HepG2 cells was isolated and purified from S.vaninii.For enhancing bioavailability and bioactivity of PV5,nanoliposomes-loaded with PV5(PV5-NPs)with an average particle size of(110.17±2.01)nm were prepared,and improved the oral bioavailability of PV5 in vivo.Additionally,PV5-NPs synergistically enhanced the antitumor activity in the H22 tumor bearing mice,reflecting in reducing tumor size and increasing levels of pro-apoptotic factors.The mechanism of PV5-NPs against liver tumor might be attributed to the blocking MEK/ERK pathway.The bioactive agents of PV5 such as Phellibaumin A,Phelligridin_C and Hispidin played a key role in the antitumor activity.Consequently,this study indicated that nanoliposomes could be used as a potential strategy for elevating bioavailability and bioactivity of polyphenols from S.vaninii.展开更多
The 6-4 photolyase can specifically repair 6-pyrimidine-4-pyrimidinone(6-4 PP)photoproduct from UVBtriggered DNA damage.However,its application for skin damage hasn’t been reported yet.This study prepared the novel 6...The 6-4 photolyase can specifically repair 6-pyrimidine-4-pyrimidinone(6-4 PP)photoproduct from UVBtriggered DNA damage.However,its application for skin damage hasn’t been reported yet.This study prepared the novel 6-4 photolyase nanoliposomes(6-4 NL),derived from UVB-resistant Antarctic Chlamydomonas sp.ICE-L,which effectively removed 6-4 PPs in UVB-induced skin.The 6-4 NL mitigated oxidative stress by remarkably reducing ROS,MDA and 8-OHdG,and enhancing SOD activity.Anti-inflammatory action was associated with the inhibition of NF-κB pathways by downregulating TNF-α,IL-6,COX-2 and NF-κB.The 6-4 NL regulated mitogen-activated protein kinase pathways via significantly diminishing expression of JNK,ERK and p38,and their phosphorylated forms.Additionally,anti-wrinkle effects were evidenced by significantly reducing the expression of AP-1,MMP-1 and MMP-2,and increasing hydroxyproline levels.These findings provided convincing evidence for the protective mechanisms of 6-4 NL against UVB-induced skin damage,as well as for the potential application in preventing photoaging and skin diseases.展开更多
基金funded by National Key R&D Plan of China(2024YFE0109500)the National Natural Science Foundation of China(32472367,32372249)Key Program of the Natural Science Foundation of Zhejiang Province(HZSZ25C200001).
文摘Hyperuricemia(HUA)is a metabolic disease characterized by high levels of uric acid(UA)in the blood and varying degrees of kidney damage.Desirable nanoliposomes should simultaneously exhibit efficient biocompatibility and effective drug delivery.However,they both usually require special structural properties.Herein,we propose a strategy to prepare nanoliposomes with varying rigidity by replacing cholesterol(CH)with phytosterol esters(PE).The results showed that the particle size of PE naringenin nanoliposomes(PE-NAR)was 179.5 nm,and the encapsulation efficiency(EE)was 79.93%.In atomic force microscopy(AFM)tests,PE-NAR showed a 1-fold increase in rigidity compared to CH naringenin nanoliposomes(CH-NAR).By observing the effects of naringenin nanoliposomes(NAR-NLs)on the physiological and biochemical indicators in HUA mice,we explore its impact on kidney damage and inflammatory pathways in HUA mice.The results show that NAR-NLs significantly inhibit UA levels and improve kidney damage.Compared to oral naringenin,NAR-NLs generally enhance the in vivo antioxidant effects of naringenin.Furthermore,high-rigidity PE-NAR downregulated the renal inflammatory factor interleukin-1β(IL-1β)to 6.67%,demonstrating the highest inhibitory effect.Further experiments have demonstrated that naringenin exerts a protective effect in kidney injury by inhibiting the activation of NOD like receptor protein 3(NLRP3)inflammasome and reducing oxidative stress within the body.In summary,by adjusting the rigidity of the nanoliposomes,the oral administration of naringenin can effectively improve the alleviation of HUA.
基金financially supported by Shenzhen Sanming Project of Medicine and Health, No. SZSM201612049 (to KJC)the Shenzhen Municipal Basic Research Project for Discipline Layout of China, No. JCYJ20170413161352000 (to YHL)Guangdong Basic Research Project, No. 2020A1515011427 (to ZZW)
文摘Previous studies have shown that berberine has neuroprotective effects against Alzheimer’s disease,including antagonizing tau phosphorylation,and inhibiting acetylcholinesterase activity and neural cell apoptosis.However,its low bioavailability and adverse reactions with conventional administration limit its clinical application.In this study,we prepared berberine nanoliposomes using liposomes characterized by low toxicity,high entrapment efficiency,and biodegradability,and modified them with lactoferrin.Lactoferrin-modified berberine nanoliposomes had uniform particle size and high entrapment efficiency.We used the lactoferrin-modified berberine nanoliposomes to treat a mouse model of Alzheimer’s disease established by injection of amyloid-beta 1-42 into the lateral ventricle.Lactoferrin-modified berberine nanoliposomes inhibited acetylcholinesterase activity and apoptosis in the hippocampus,reduced tau over-phosphorylation in the cerebral cortex,and improved mouse behavior.These findings suggest that modification with lactoferrin can enhance the neuroprotective effects of berberine nanoliposomes in Alzheimer’s disease.
基金supported by the National Natural Science Foundation of China (Nos. 30801441 and 81773278)。
文摘Light-responsive carriers have been used for the controlled release of antitumor drugs in recent years.However, most light-responsive vectors require high-energy ultraviolet or visible light to achieve local drug release, and ultraviolet light would cause cellular damage. Near-infrared light has a deeper tissuepenetration depths and minimal harm to tissues, but it is difficult to cleave the chemical bond directly.The aim of this study is to develop a novel near-infrared light-responsive carrier for local release of antitumor drugs. Unsaturated phospholipids can be oxidized by singlet oxygen to achieve liposomal drug release, and singlet oxygen can be produced by photosensitizer under light irradiation. A new near-infrared light-responsive nanoliposome was designed that imparts light-triggered local drug release. Nanoliposomes, which were composed of matrix phospholipids and unsaturated phospholipids, were prepared by ammonium sulfate gradient method, and loaded with antitumor drug doxorubicin(DOX) and photosensitizer 1,4,8,11,15,18,22,25-octabutoxypalladium phthalocyanine. Under near-infrared light, photosensitizers could produce singlet oxygen and damage tumor cells by photodynamic therapy. Simultaneously, the unsaturated phospholipids were oxidized by singlet oxygen and result in DOX release, causing sustained cell damage by chemotherapy. Near-infrared light-responsive nanoliposomes exhibit enhanced anticancer activity owing to combined treatment of photodynamic therapy and chemotherapy. A new platform is thus offered for designing effective intracellular drug-release systems, holding great promise for future cancer therapy.
基金the support of Pharmacy Laboratory Centre and Animal Centre of Shenyang Pharmaceutical Universitysupported by the State Key Laboratory(Long-acting and Targeting Drug Delivery System)the Special Construction Project(Taishan ScholarePharmacy Specially Recruited Experts).
文摘The objective of this study is to compare the targeting ability of activated carbon nanoparticles and nanoliposomes,which are used as carriers for delivering docetaxel(DTX)to the metastatic lymph nodes.In this study,we first prepared the DTX-loaded activated carbon nanoparticles(DTX-AC-NPs)by modifying the activated carbon with nitric acid oxidation and absorbing DTX in the concentrated nitro-oxide nanocarbon.We then prepared DTX-loaded nanoliposomes(DTX-LPs)by the proliposome method.The physiochemical properties of DTX-AC-NPs and DTX-LPs were carefully evaluated in vitro.The metastatic lymph node uptake and the injection site retention were investigated by analyzing the DTX concentration in metastatic lymph nodes and injection sites.The result showed that DTX-AC-NPs and DTX-LPs with suitable and stable physicochemical properties could be used for in vivo lymph node targeting studies.DTX-AC-NPs significantly increased DTX-AUC_((0-24)) and prolonged DTX-retention in metastatic lymph nodes compared to DTX-LPs and non-modified activate carbon in vivo.This study demonstrated activated carbon nanoparticles may be potential intralymphatic drug delivery system to preferentially target regional metastatic lymph nodes.
基金financially supported by the Natural Sciences and Engineering Research Council of Canada(NSERC,Collaborative Research and Development program,project#CRDPJ 488702-15)the Consortium for Research and Innovation in Industrial Bioprocesses in Quebec(CRIBIQ,project#2015-023-PR-C16)+2 种基金the Ministry of Agriculture,Fisheries and Food of Quebec(MAPAQProject#IA-115316)their industrial partners Biosecur Lab(A Kerry Company),Skjodt-Barrett Foods Inc.,Foodarom Group Inc.And Kerry Inc.Yosra Ben-Fadhel was a fellowship recipient of the Armand-Frappier Foundation.
文摘The encapsulation of an antimicrobial formulation based on essential oils(EOs)and citrus extract(CE)mixture into nanoemulsion(NE),gelled emulsion(GE),and nanoliposomes(NL)was performed.The encapsulation forms(NE,GE,and NL)were evaluated further for their stability,encapsulation efficiency(EE),controlled release of bioactive ingredients,in vitro and in situ antimicrobial activity.Results showed that all colloidal systems exhibited similar stability behaviors.Among all colloidal systems,NL witnessed the smallest particle size(91.9 nm)with the lowest polydispersity index(0.230)and highest zeta potential(36 mV)NL has retained the antimicrobial formulation longer,controlled the release over time,and maintained the total phenolic content.The in vitro results showed that GE improved the antimicrobial activity against Escherichia coli,Listeria monocytogenes,Bacillus subtilis,Candida albicans,and Aspergillus flavus.In situ,the test exhibited that GE applied on the bread surface extended the shelf-life and delayed Bacillus subtilis proliferation to 36 days without affecting the sensory properties of baked bread compared to 14 and 24 days in the non-treated group and treated group with sorbate,a chemical additive widely used in bakery products.Consequently,encapsulating natural antimicrobials represents an exciting process that could improve the bioactivity and shelf-life extension of the bread.
基金sustained by the National Natural Science Foundation of China(82072512,52273152,22161132027)Zhejiang Provincial Natural Science Foundation of China(LY23H060013,LY21H070001,LY20H160044,LBY21H060003).
文摘Nanoliposomes have a broad range of applications in the treatment of autoimmune inflammatory diseases because of their ability to considerably enhance drug transport.For their clinical application,nanoliposomes must be able to realize on-demand release of drugs at disease sites to maximize drug-delivery efficacy and minimize side effects.Therefore,responsive drug-release strategies for inflammation treatment have been explored;however,no specific design has been realized for a responsive drug-delivery system based on pyroptosis-related inflammation.Herein,we report a pioneering strategy for self-adaptive pyroptosis-responsive liposomes(R8-cardiolipin-containing nanoliposomes encapsulating dimethyl fumarate,RC-NL@DMF)that pre-cisely release encapsulated anti-pyroptotic drugs into pyroptotic cells.The activated key pyroptotic protein,the N-terminal domain of gasdermin E,selectively integrates with the cardiolipin of liposomes,thus forming pores for controlled drug release,pyroptosis,and inflammation inhibition.Therefore,RC-NL@DMF exhibited effective therapeutic efficacies to alleviate autoimmune inflammatory damages in zymosan-induced arthritis mice and dextran sulfate sodium-induced inflammatory bowel disease mice.Our novel approach holds great promise for self-adaptive pyroptosis-responsive on-demand drug delivery,suppressing pyroptosis and treating autoimmune inflammatory diseases.
基金supported by the grant-in-aid to the Department of Pharmaceutical Sciences,Maharshi Dayanand University,Rohtak,India,under the plan of Major Research Project[F.No.-43-485/2014(SR)]by University Grants Commission,India.
文摘Nanoliposomes are bilayer phospholipid vesicles used to encapsulate and deliver therapeutic agents.The study was aimed to investigate the effects of critical variables on nanoliposomes characteristics.Imatinib mesylate-loaded nanoliposomes were formulated by the two-step emulsification process using a high-speed homogenizer system and probe-type ultrasonicator.The Box-Behnken design was utilized to optimize the process parameters.The mean particle size of nanoliposomes was found to be 211 nm to 623.3 nm with a low value of polydispersity index(0.005 to 0.7).Zeta potential values varied from‒27.6 mV to‒9.2 mV in uncoated nanoliposomes to+27.5 mV in chitosan-coated nanoliposomes.The encapsulation efficiency in formulation NLP-H8 containing 200 mg of phosphatidylcholine,homogenization speed of 12000 rpm,and 7 min of sonication time was found to be 76.49%without the coating and 85.4%in 0.2%w/v chitosan-coated nanoliposomes.TEM image confirmed the spherical shape of nanoliposomes.In-vitro drug release study demonstrated that the optimized nanoliposomal formulations released 84.67%of the loaded drug after 24 h in 0.1 N HCl.The IC_(50)value of formulation NLP-H8 was found to be 7.98μM.Nanoliposomal formulations were prepared successfully with suitable size,morphology,encapsulation efficiency,and drug release.The models developed in this study may be utilized further as a response surface for the various parameters of nanoliposomes.
基金supported by the National Research Foundation of Korea(NRF)grant funded by the Korea government(MSIT)(No.2021R1A2C2013460).
文摘The present study focuses on optimizing the preparation conditions of coenzyme Q10(CoQ10)-loaded liposomes(LPs),aiming to overcome the limitations of conventional LPs.Cholesterol,commonly used for LPs stabilization,prompts exploration of alternative phytosterols due to its health concerns.This study evaluates the optimal concentrations of cholesterol andβ-sitosterol,along with CoQ10 by analyzing their effects on particle size and entrapment efficiency(EE)using response surface methodology.It further investigates how cholesterol andβ-sitosterol impact key physicochemical attributes,including lipid oxidation stability,cellular adhesion property,and cellular antioxidant activity.Incorporating cholesterol led to increased particle size but decreased CoQ10-loaded LPs’EE.Conversely,β-sitosterol incorporation increased both particle size and EE.The optimal sterol,including cholesterol andβ-sitosterol,and CoQ10 concentration was 0.605 and 0.150 mg/mL,respectively.Notably,significant differences between cholesterol andβ-sitosterol exhibited in lipid oxidation stability and cellular antioxidant activity of CoQ10-loaded LPs prepared with optimal conditions(p<0.05).Under heat treatment at 60℃ for 2 h,β-sitosterol-containing LPs suppressed malondialdehyde production approximately 15%more effectively than cholesterol-containing LPs.Moreover,β-sitosterol elevated cellular antioxidant activity by around 11%in Caco-2 monolayers compared to cholesterol.These findings highlightβ-sitosterol’s potential to enhance CoQ10-loaded LPs’physicochemical attributes,proposing applications for cholesterol-free,stable LPs with improved bioactivity in the food and pharmaceutical industries.
基金supported by grants from the National Key Re-search and Development Program of China(2023YFC3603100 and 2023YFC3603105)“Leading Goose”R&D Program of Zhejiang Province(2022C03076-4).
文摘Background:Diquat,a commonly employed bipyridyl herbicide,is recognized for its hepatotoxic effects attributed to the generation of reactive oxygen species.Baicalin(BAI),a flavonoid derivative,has garnered significant research interest for its hepatoprotective properties.Nevertheless,the clinical application of BAI is constrained by its limited water solubility and poor bioavailability.To address these challenges,BAI-nanoliposome(BAI-NL)has emerged as a novel drug delivery platform aimed at enhancing therapeutic outcomes.Methods:We used diquat-induced liver injury mouse model and AML12 hepatocytes to test the pro-tective effect of BAI and BAI-NL on liver inflammation,oxidative stress,and mitochondrial function.The parameters included histological,biochemical,and molecular biological analyses.Results:In the diquat-induced model,both BAI and BAI-NL exhibited effectiveness on attenuating liver inflammation.Ex vivo analyses further indicated that BAI-NL was superior to BAI in preserving mito-chondrial membrane potential,reducing oxidative stress,and modulating the phosphatase and tensin homolog-induced putative kinase 1(PINK1)/Parkin RBR E3 ubiquitin-protein ligase(Parkin)signaling pathway.These findings enhanced mitophagy and facilitated the removal of damaged mitochondria.Conclusions:BAI-NL exhibited superior hepatoprotective effects compared to free BAI,possibly by re-ducing inflammation,preserving mitochondrial homeostasis,and reinstating autophagic balance through modulation of the PINK1/Parkin signaling pathway.These outcomes indicate a groundbreaking method for addressing liver diseases and underscore the potential of nanoliposome technology in augmenting the efficacy of natural compounds.
基金supported by the Macao Science and Technology Development Fund (FDCT 0148/2022/A3 and 0019/2024/RIA1)the National Natural Science Foundation of China (No. 81572979)
文摘Immunotherapy with interleukin-2(IL-2)in treating cancers is subject to several limitations such as systemic side effects and reduced efficacy against tumors with low immune cell infiltration despite its promise.To address these challenges,IL-2-So-Lipo,a novel liposomal formulation combining IL-2 with sorafenib derivative,was developed as an anti-angiogenic drug that inhibits the growth of new blood vessels which play crucial roles in tumor growth.Sorafenib derivatives could target at melanoma-specific receptors,further enhancing liposomal specificity at the tumor site.Our results demonstrated that the prepared IL-2-So-Lipo significantly enhanced anti-tumor activity compared to IL-2 or sorafenib monotherapies,as well as their combination.In a B16F10 melanoma model,IL-2-So-Lipo was found to significantly inhibit tumor progression(tumor volume of 108.01±62.99 mm^(3))compared to the control group(tumor volume of 1,397.13±75.55 mm^(3)),improving the therapeutic efficacy.This enhanced efficacy is attributed to the targeted delivery of IL-2 which promoted the infiltration and activation of cytotoxic T lymphocytes.Additionally,liposomal encapsulation of sorafenib derivatives enhanced its delivery efficiency,promoting tumor cell apoptosis and suppressing angiogenesis.Mechanistically,IL-2-So-Lipo could kill tumors by inducing a shift towards an anti-tumor immune response via facilitating the polarization of macrophages towards the M1 phenotype.Furthermore,IL-2-So-Lipo downregulated several key proteins in the MAPK signaling pathway,exerting a significant role in mediating tumor resistance to sorafenib.These findings underscore the potential of IL-2-So-Lipo as a promising strategy to improve the therapeutic efficacy of immunotherapy and targeted therapy in cancers.Moreover,the combination of IL-2 and sorafenib in a liposomal delivery system overcame the limitations of conventional IL-2 therapy,offering a synergistic approach to improve therapeutic outcomes for solid tumors.
文摘Conventional nutritional supplements frequently demonstrate limited clinical effectiveness due to the harsh milieu of the gastrointestinal tract,inefficient transepithelial transport,and rapid systemic clearance.Nanoliposomal delivery platforms-lipid bilayer vesicles on the nanometer scale-have attracted attention as an adaptive strategy to shield sensitive nutrients,navigate biological barriers,and deliver payloads directly to target tissues or even sub-cellular organelles.Despite a growing body of literature,a consolidated appraisal of design principles,targeting modalities,and translational hurdles is still needed to guide future nutraceutical innovation.We aim to:(1)Summarize the physicochemical foundations of nanoliposomal nutrient carriers;(2)Delineate state-of-the-art approaches for organ-specific and organelle-specific targeting,with particular emphasis on renal and mitochondrial delivery;(3)Evaluate current evidence supporting therapeutic benefits in cardiometabolic,neuroprotective,and renal-repair contexts;and(4)Map unresolved challenges-including manufacturing scale-up,cost,and regulatory oversight-to inform a roadmap for clinical translation.A systematic literature search was performed across PubMed,Web of Science,and Scopus through May 2025 using Boolean combinations of“nanoliposome”,“nutrient”,“targeted delivery”,“bioavailability”,and organ-specific terms(e.g.,“kidney”,“mitochondria”).Primary research articles,systematic reviews,and relevant meta-analyses written in English were included.Data were extracted on liposomal composition,particle size,surface modifications(e.g.,polyethylene glycol,ligand conjugation),in vitro and in vivo bio-distribution,efficacy outcomes,and safety profiles.Key design variables were mapped against reported biological performance to identify convergent principles.Sixty-four original studies and twenty-one reviews met inclusion criteria.Encapsulation within phosphatidylcholine-rich bilayers consistently enhanced nutrient stability in simulated gastric fluid and improved Caco-2 trans-epithelial transport two-fold to ten-fold compared with free compound controls.Ligand-mediated strategies-such as folate,lactoferrin,or peptide conjugation-achieved organ-specific accumulation,with kidney-directed liposomes demonstrating up to a four-fold increase in renal cortex uptake.Mitochondrial targeting using amphipathic peptides(e.g.,SS-31)or triphenylphosphonium moieties delivered antioxidant nutrients to the organelle,restoring mitochondrial membrane potential and reducing reactive oxygen species(ROS)in preclinical cardiomyopathy and neurodegeneration models.Endosomal escape was most effectively triggered by fusogenic lipids(e.g.,dioleoylphosphatidylethanolamine)or pH-responsive polymers.PEGylation prolonged circulation half-life by 3-6 hours but elicited anti-polyethylene glycol antibodies in approximately one-quarter of recipients;emerging natural sterol-mimetic or collagen-mimetic coatings showed comparable stealth behavior with superior biodegradability.Scalability remains limited:Only three studies reported pilot-scale(>10 L)batches with Good Manufacturing Practice-compliant reproducibility.Targeted nanoliposomal systems substantially improve nutrient stability,absorption,and tissue specificity,offering a credible route to transform supplement efficacy for cardiometabolic,renal,and neuroprotective indications.Optimization of lipid composition,escape mechanisms,and biocompatible surface chemistries can further enhance therapeutic indices.Nonetheless,industrial-scale manufacturing,cost containment,and immunogenicity mitigation remain critical obstacles.Addressing these gaps through standardized characterization protocols,head-to-head clinical trials,and biomaterial innovation will be essential to unlock the full potential of nanoliposomal nutraceuticals in routine healthcare practice.
基金the Career Development Program for Yong and Middle-aged Teachers in Shenyang Pharmaceutical University。
文摘Although the appearance of Doxil alleviated the cardiotoxicity of DOX, the progression-free survival of patients was not prolonged compared with traditional medication regimens, and side effects such as hand-foot syndrome has occurred. In order to solve this dilemma, we have designed a novel co-delivery strategy to construct a co-loaded liposome of berberine(BER) and doxorubicin(DOX), which was called Lipo Be Do. The optimal synergistic ratio of the two drugs was screened by cell cytotoxicity experiments in vitro, and the optimal attenuation ratio was further determined by in vivo cardiac H&E staining pathological sections. The optimal combination treatment caused a robust increase in apoptotic cells of 4T1, as compared to drug alone treatment. The prepared co-loaded liposome, Lipo Be Do, had high encapsulation efficiency and good stability. The nanoliposome carrier controlled the biological fate of the drugs and maintained a pre-defined optimal ratio in vivo. The Lipo Be Do significantly inhibited tumor growth in 4T1 murine mammary carcinoma model compared with Doxil(P < 0.05), and completely overcame the myocardial rupture toxicity caused by Doxil in mice. Our co-loaded liposome delivery platform technology provided a new direction for the clinical treatment of triple-negative breast cancer and the safe application of DOX.
基金supported by Zhejiang Provincial Natural Science Foundation of China under Grant No.LYY21H300001Zhejiang Medical and Health Science and Technology project under Grant No.2021KY906Hangzhou Medical Key Discipline Construction Project under Grant No.[2021]21–39
文摘Psoriasis is an inflammatory skin disease that is intricately linked to oxidative stress.Antioxidation and inhibition of abnormal proliferation of keratinocytes are pivotal strategies for psoriasis.Delivering drugs with these effects to the site of skin lesions is a challenge that needs to be solved.Herein,we reported a nanotransdermal delivery system composed of all-trans retinoic acid(TRA),triphenylphosphine(TPP)-modified cerium oxide(CeO2)nanoparticles,flexible nanoliposomes and gels(TCeO_(2)-TRA-FNL-Gel).The results revealed that TCeO_(2)synthesized by the anti-micelle method,with a size of approximately 5 nm,possessed excellent mitochondrial targeting ability and valence conversion capability related to scavenging reactive oxygen species(ROS).TCeO_(2)-TRA-FNL prepared by the film dispersion method,with a size of approximately 70 nm,showed high drug encapsulation efficiency(>96%).TCeO_(2)-TRA-FNL-Gel further showed sustained drug release behaviors,great transdermal permeation ability,and greater skin retention than the free TRA.The results of in vitro EGF-induced and H2O2-induced models suggested that TCeO_(2)-TRA-FNL effectively reduced the level of inflammation and alleviated oxidative stress in HaCat cells.The results of in vivo imiquimod(IMQ)-induced model indicated that TCeO_(2)-TRA-FNL-Gel could greatly alleviate the psoriasis symptoms.In summary,the transdermal drug delivery system designed in this study has shown excellent therapeutic effects on psoriasis and is prospective for the safe and accurate therapy of psoriasis.
基金Supported by the National Key R&D Program of China,No.2017YFC1308604
文摘Pancreatic cancer is one of the leading causes of cancer death worldwide.Adjuvant chemotherapy has been developed based on the experiences made with palliative chemotherapy, and advocated to improve long-term survival of patients with this disease. However, the optimal chemotherapeutic regimen remains controversial. Recently, Conroy et al demonstrated the impressive benefits of modified FOLFIRINOX over gemcitabine alone in the multicenter Partenariat de Recherche en Oncologie Digestive 24(PRODIGE-24) trial. The remarkable results mark a new milestone in treating resectable pancreatic cancer and have now changed the standard of care for this patient population. In this commentary, we discuss an issue of difference of tumor grade between the PRODIGE-24 trial and previous phase III trials. We also discuss potential biomarkers predicting therapeutic response to modified FOLFIRINOX. Finally,we summarize several ongoing clinical trials of replacing part of the FOLFIRINOX regimen with Xeloda/S-1/nanoliposomal irinotecan for pancreatic cancer.
基金supported by National Natural Science Foundation of China(31700015)Health Commission of Hunan Province(C202306017634)Changsha Natural Science Foundation(KQ2208092).
文摘Crocetin displays strong antioxidant,anti-inflammatory and anti-depression activity which is promising to relieve symptoms of fatigue.As a carotenoid,crocetin is difficult to dissolve in water and highly unstable against many environmental factors.Nanoliposome is used to encapsulate crocetin to improve its water dispersion.In the present study,the antifatigue activities and potential mechanism of crocetin loaded nanoliposome(CLN)was extensively investigated.The potential antifatigue pathway of CLN was analyzed.Furthermore,impact of CLN on the gut microbiota structure was examined which contributes to its antifatigue functions.CLN significantly increases exhaustive swimming time of fatigue mice,decreases the blood contents of lactic,blood urea nitrogen(BUN)and malondialdehyde(MDA).At the same time,CLN improves the activity of glutathione peroxidase(GSH-Px)and succinate dehydrogenase(SDH)enzyme,attenuates the oxidant stress in mice.CLN activates the adenosine monophosphate-activated kinase(AMPK)/peroxisome proliferator-activated receptor gamma coactivator-1α(PGC-1α)signaling pathway of fatigue mice,increases the mRNA expression of ATP synthase.It also increases mRNA expression of mitochondrial transcription factor A(TFAM)which promotes mitochondrial biogenesis.Additionally,CLN ameliorates the gut microbiota structure by increasing the abundance of genus such as Lactobacillus in fatigue mice.In summary,CLN exerts strong anti-fatigue properties by decreasing the oxidant stress and the contents of harmful metabolites,augmenting the production of ATP,and potentially ameliorating the gut microbiota structure.
文摘Liposome, albumin and polymer polyethylene glycol are nanovector formulations successfully developed for anti-cancer drug delivery. There are significant differences in pharmacokinetics, efficacy and toxicity between pre- and post-nanovector modification. The alteration in clinical pharmacology is instrumental for the future development of nanovector-based anticancer therapeutics. We have reviewed the results of clinical studies and translational research in nanovectorbased anti-cancer therapeutics in advanced pancreatic adenocarcinoma, including nanoparticle albumin-bound paclitaxel and nanoliposomal irinotecan. Furthermore, we have appraised the ongoing studies incorporating novel agents with nanomedicines in the treatment of pancreatic adenocarcinoma.
基金This work was supported by grants from the National Natural Science Foundation of China(No.81770268)the National Basic Research Program of China(No.2015CB932100).
文摘Nanoliposome is a useful dosage form to increase solubility and absorption of simvastatin(SMV), and consequently improves its therapeutic effects. However, in vivo toxicity of SMV could also be elevated accompanied by the absorption enhancement, which is a decisive factor for the clinical application of SMV nanoliposome(SMV-Lipo), but has not been studied systematically and reported so far. In this study, organ toxicity of SMV-Lipo was evaluated in mice in the presence and absence of isoproterenol and compared to those of free SMV. Results demonstrated that compared to free SMV, the SMV-Lipo administrated at an equal dose of 25 mg/kg/d led to severe myocardiotoxicity, hepatotoxicity at baseline and more pronounced liver injury with elevation of alanine aminotransferase. In addition, muscular adverse effect was also observed in SMV-Lipo treated group but not in SMV group. Pharmacokinetic studies revealed that compared to free SMV, the SMV-Lipo administration significantly improved the plasma SMV concentration, and the oral bioavailability was 6.5 times of free SMV. Notably, when the dosage of free SMV increased to 50 mg/kg/d, yielding the comparable plasma concentration as SMV-Lipo given at 25 mg/kg/d, the myocardiotoxicity was observed in free SMV treated mice as well, which further confirmed that the enhanced absorption of SMV by the nanoliposomal formulation resulted in more severe myocardiotoxicity than the equal dose of free SMV.
文摘Catechin(CTC)is a phenolic active compound with multiple biological activities.However,CTC is relatively unstable,easily oxidized and poorly soluble in water,showing limited bioavailability,which is a challenge for its application in the pharmaceutical and food industry.The purpose of this study was to promote the controlled release of CTC in the simulated gastrointestinal(GI)tract by using biopolymer-coupled nanoliposomes(NL).The nanoliposome was characterized by multifunctional polycrystalline X-ray diffraction(XRD),and Fourier transform infrared spectroscopy(FTIR).The results exhibited that the size of the nanocarrier was in the range of 87-178 nm,the encapsulation efficiency of CTC was 93.5%,and the combination of chitosan(CS)and alginate(ALG)was better than that of monopolymer.In vitro digestion studies showed that ALG-CS-NL significantly controlled the release of CTC by the diffusion,dissolution,and slow release mechanism and retained about 33%-37%of CTC under the GI condition.These results demonstrated that ALG-CS-NL could increase the stability of CTC,which may be important for the development of nutraceutical-enriched functional foods.
基金supported by the Shanghai Rising-Star Program(grant number 24QB2702300)Shanghai Municipal Commission of Science and Technology(Grant No.22N 51900100)Zhejiang Province“Triple Agriculture Nine Aspects Cooperation”Science and Technology Cooperation Program(Grant No.2022SNJF046).
文摘Sanghuangporus vaninii as a valuable edible fungus represents a high source of polyphenols with multidimensional bioactivities.However,the conundrum of the oral bioavailability of polyphenols limits its biological activity.Therefore,a strategy of nanoliposome was employed to enhance oral bioavailability of polyphenols from S.vaninii.In this study,a polyphenol component(PV5)with excellent inhibition of HepG2 cells was isolated and purified from S.vaninii.For enhancing bioavailability and bioactivity of PV5,nanoliposomes-loaded with PV5(PV5-NPs)with an average particle size of(110.17±2.01)nm were prepared,and improved the oral bioavailability of PV5 in vivo.Additionally,PV5-NPs synergistically enhanced the antitumor activity in the H22 tumor bearing mice,reflecting in reducing tumor size and increasing levels of pro-apoptotic factors.The mechanism of PV5-NPs against liver tumor might be attributed to the blocking MEK/ERK pathway.The bioactive agents of PV5 such as Phellibaumin A,Phelligridin_C and Hispidin played a key role in the antitumor activity.Consequently,this study indicated that nanoliposomes could be used as a potential strategy for elevating bioavailability and bioactivity of polyphenols from S.vaninii.
基金supported by the Innovation Team Program of Jinan(202228041)Natural Science Foundation of China(32470132,32000074,42176130)+3 种基金Natural Science Foundation of Shandong Prov-ince(ZR2021MD044)Key Research and Development Program of Shandong Province(2023TZXD047,2023CXPT087,2021TZXD008)Shandong Program of Qingdao Pilot National Laboratory for Marine Science and Technology(2022QNLM030003-1)Key Technology and Industrialization Demonstration Projects of Qingdao(23-1-4-xxgg-20-nsh,23-1-3hysf-1-hy,23-1-4-xxgg-13-nsh,22-3-5-yqpy-10-qy,24-1-3-hygg-24-hy,24-1-8-xdny-28-nsh).
文摘The 6-4 photolyase can specifically repair 6-pyrimidine-4-pyrimidinone(6-4 PP)photoproduct from UVBtriggered DNA damage.However,its application for skin damage hasn’t been reported yet.This study prepared the novel 6-4 photolyase nanoliposomes(6-4 NL),derived from UVB-resistant Antarctic Chlamydomonas sp.ICE-L,which effectively removed 6-4 PPs in UVB-induced skin.The 6-4 NL mitigated oxidative stress by remarkably reducing ROS,MDA and 8-OHdG,and enhancing SOD activity.Anti-inflammatory action was associated with the inhibition of NF-κB pathways by downregulating TNF-α,IL-6,COX-2 and NF-κB.The 6-4 NL regulated mitogen-activated protein kinase pathways via significantly diminishing expression of JNK,ERK and p38,and their phosphorylated forms.Additionally,anti-wrinkle effects were evidenced by significantly reducing the expression of AP-1,MMP-1 and MMP-2,and increasing hydroxyproline levels.These findings provided convincing evidence for the protective mechanisms of 6-4 NL against UVB-induced skin damage,as well as for the potential application in preventing photoaging and skin diseases.
