Background Our previous studies demonstrated that divalent organic iron(Fe)proteinate sources with higher complexation or chelation strengths as expressed by the greater quotient of formation(Qf)values displayed highe...Background Our previous studies demonstrated that divalent organic iron(Fe)proteinate sources with higher complexation or chelation strengths as expressed by the greater quotient of formation(Qf)values displayed higher Fe bioavailabilities for broilers.Sodium iron ethylenediaminetetraacetate(NaFeEDTA)is a trivalent organic Fe source with the strongest chelating ligand EDTA.However,the bioavailability of Fe when administered as NaFeEDTA in broilers and other agricultural animals remains untested.Herein,the chemical characteristics of 12 NaFeEDTA products were determined.Of these,one feed grade NaFeEDTA(Qf=2.07×10^(8)),one food grade NaFeEDTA(Qf=3.31×10^(8)),and one Fe proteinate with an extremely strong chelation strength(Fe-Prot ES,Qf value=8,590)were selected.Their bioavailabilities relative to Fe sulfate(FeSO_(4)·7H_(2)O)for broilers fed with a conventional corn-soybean meal diet were evaluated during d 1 to 21 by investigating the effects of the above Fe sources and added Fe levels on the growth performance,hematological indices,Fe contents,activities and gene expressions of Fe-containing enzymes in various tissues of broilers.Results NaFeEDTA sources varied greatly in their chemical characteristics.Plasma Fe concentration(PI),transferrin saturation(TS),liver Fe content,succinate dehydrogenase(SDH)activities in liver,heart,and kidney,catalase(CAT)activity in liver,and SDH mRNA expressions in liver and kidney increased linearly(P<0.05)with increasing levels of Fe supplementation.However,differences among Fe sources were detected(P<0.05)only for PI,liver Fe content,CAT activity in liver,SDH activities in heart and kidney,and SDH mRNA expressions in liver and kidney.Based on slope ratios from multiple linear regressions of the above indices on daily dietary analyzed Fe intake,the average bioavailabilities of Fe-Prot ES,feed grade NaFeEDTA,and food grade NaFeEDTA relative to the inorganic FeSO_(4)·7H_(2)O(100%)for broilers were 139%,155%,and 166%,respectively.Conclusions The bioavailabilities of organic Fe sources relative to FeSO_(4)·7H_(2)O were closely related to their Qf values,and NaFeEDTA sources with higher Qf values showed higher Fe bioavailabilities for broilers fed with a conventional corn-soybean meal diet.展开更多
Epilepsy is a devastating neurological condition that affects over 70 million people worldwide.Apart from idiopathic epilepsy,numerous diseases have been reported to cause secondary epilepsy.Polyphenols,ubiquitously e...Epilepsy is a devastating neurological condition that affects over 70 million people worldwide.Apart from idiopathic epilepsy,numerous diseases have been reported to cause secondary epilepsy.Polyphenols,ubiquitously existing in fruits and vegetables,has become a promising neuroprotective candidate against multiple neurological abnormalities due to its interplay with gut microbiome composed of the bacterial population in gastrointestinal system.This bioactive compound is also being tested for the management of epileptogenesis.However,there is still insufficient evidence from mechanistic studies to demonstrate the causal relationship between anti-epileptic effect of polyphenols and microbial alteration.In this review,we provide the brief overview of epilepsy,polyphenols and gut microbiota.We then analysis the association of polyphenols and gut microbiota particularly in the epilepsy and symptomatic seizures-induced by epilepsy related disorders.We also discuss the possibility for the combined application with probiotics to improve the bioavailability and bioaccessibility of polyphenols for expanding its anti-epileptic function.We finally summarize the therapeutic potential of anti-seizure polyphenols through affecting gut microbiome,and propose that the anti-epileptic effect of polyphenols may be tightly relevant to intestinal bacterial flora for overcoming epilepsy and its comorbidities simultaneously.Therefore,the dietary polyphenols targeting specific bacteria may achieve the outcome of‘one stone,two birds’.展开更多
Guava(Psidium guajava L.),a plant belonging to the Myrtaceae family,holds significant medicinal and nutritional values.Leaves of the plant are described to be elliptical with a dark green color and are utilized in the...Guava(Psidium guajava L.),a plant belonging to the Myrtaceae family,holds significant medicinal and nutritional values.Leaves of the plant are described to be elliptical with a dark green color and are utilized in the treatment of gastrointestinal and respiratory issues along with increasing the platelet count in patients suffering from dengue.In this review paper,the nutritional composition and bioactive compounds of guava leaves,including proteins,vitamins,minerals,and polysaccharides,have been reviewed.The methods of extraction of bioactive compounds from guava leaves and their bioactivities,including antioxidant,anti-diabetic,and anti-cancer potential,have been explored.Further,encapsulation techniques for improving the transport of bioactive compounds and living cells into foods have been studied.The application of guava leaves in different food systems such as herbal tea,pork sausage,chocolates,jelly,meals for chickens,functional beverages,and as antibacterial agents in food preservatives has also been investigated.The findings of this review illustrated that the phytochemicals present in guava leaves showed excellent antimicrobial and antioxidant properties.Encapsulation appears to be a promising technique for improving the stability,bioavailability,and controlled release of bioactive chemicals extracted from guava leaves.Different methods for the encapsulation of bioactive compounds employed and applied in distinct food systems showed preservation of phytochemicals,improved bioactivities,and nutritional values.Overall,this review paper demonstrated how guava leaves,an abundant source of bioactive compounds,can be used as a multipurpose component to create functional foods,edible coatings,and active packaging to enhance the nutritional,antioxidant,and antimicrobial properties of various food systems that have qualities that promote health.展开更多
BACKGROUND The rising global burden of liver diseases,such as non-alcoholic fatty liver disease and liver fibrosis,has necessitated innovative therapeutic approaches.Plant-based therapies,recognized for their anti-inf...BACKGROUND The rising global burden of liver diseases,such as non-alcoholic fatty liver disease and liver fibrosis,has necessitated innovative therapeutic approaches.Plant-based therapies,recognized for their anti-inflammatory and antioxidant properties,have shown promising effects.However,poor bioavailability limits their clinical application.AIM To map global research trends,key contributors,and emerging themes in plant-based therapies combined with advanced drug delivery systems for liver health.METHODS Using the Scopus database,645 documents were retrieved and analyzed using bibliometric tools Biblioshiny and VOSviewer.Analysis focused on publication trends,geographical contributions,and advancements in drug delivery technologies,including nanoparticles,liposomes,and polymeric micelles.Metrics such as publication growth rate,authorship collaboration,and thematic clustering were assessed.RESULTS The dataset spans 43 years(1981-2024),with an annual growth rate of 11.09%in the number of publications.Research output is dominated by China(33%),followed by the United States(24%)and India(18%).Collaborative studies accounted for 24.34%of publications,with an average of 5.81 co-authors per document.Key innovations include nanoparticle encapsulation of curcumin and silymarin,improving bioavailability by up to 85%.Highly cited studies demonstrated the antioxidant,anti-inflammatory,and anti-fibrotic properties of these compounds.For instance,curcumin nanoparticles showed a 70%improvement in solubility,and silymarin liposomal formulations enhanced therapeutic efficiency by 62%.Thematic analysis revealed a transition from basic clinical observations to molecular and pharmacokinetic research,with a focus on oxidative stress mitigation and hepatoprotection.CONCLUSION This study highlights the growing synergy between plant-based therapies and advanced drug delivery systems,with significant contributions from Asian and Western countries.Future efforts should prioritize clinical trials,standardization of plant extract formulations,and interdisciplinary approaches to maximize therapeutic outcomes.The findings provide a foundation for integrating plant-derived compounds into evidence-based hepatological therapies,addressing critical challenges in bioavailability and safety.展开更多
The intricate interplay between natural compounds like curcumin and the gut microbiome has gained significant attention in recent years due to their potential therapeutic implications in various health conditions.Curc...The intricate interplay between natural compounds like curcumin and the gut microbiome has gained significant attention in recent years due to their potential therapeutic implications in various health conditions.Curcumin,a polyphenolic compound derived from turmeric,exhibits diverse pharmacological properties,including anti-inflammatory,antioxidant,and anticancer effects.Understanding how curcumin modulates gut microbiota composition and function is crucial for elucidating its therapeutic mechanisms.This review examines the current literature on the interactions between curcumin and the gut microbiome.A systematic search of relevant databases was conducted to identify studies investigating the effects of curcumin on gut microbial diversity and abundance.Key findings from studies exploring curcumin's efficacy in neurological disorders,gastrointestinal diseases,and metabolic dysfunction are synthesized and discussed.Studies have demonstrated that curcumin supplementation can modulate gut microbiota composition and function,leading to beneficial effects on gut health and homeostasis.Mechanisms underlying curcumin's therapeutic effects include immune modulation,neuroprotection,and inflammation regulation.However,challenges such as poor bioavailability and safety concerns remain significant hurdles to overcome.The interactions between curcumin and the gut microbiome hold promise for therapeutic interventions in a diverse range of health conditions.Further research is needed to optimize curcumin formulations,improve bioavailability,and address safety concerns.展开更多
Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.I...Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.In this work,we studied the impact of phosphate solubilizing bacterial agent(PSBA)on Cd bioavailability,microbial communities in soil and Cd accumulation in lettuce plants with pot experiment and field trial.Results of pot experiment showed that PSBA could decrease the bioavailability of Cd(Cd-acid extractable from 3.30 to 2.34mg/kg,Cd-reducible from 1.94 to 1.56 mg/kg),promote lettuce plants growth(increased by 33.85%height and by 33.65%fresh weight)and reduce the accumulation of Cd(from 5.85 to 3.73 mg/kg)in lettuce plants.High-throughput sequencing identified that PSBA could change the composition and structure of the soil microbial communities.The relative abundances of the three ecologically beneficial bacterial families of Pseudomonadaceae,Burkholderiaceae,and Enterobacteriaceae increased from 2.29%to 5.13%,0.56%to 5.24%,and 1.87%to 16.93%,respectively.And the former two were positively correlated with redox potential(Eh)(R^(2)=0.474,p<0.05,R^(2)=0.590,p<0.01,respectively).The bacterial networks were more complex in PSBA treatment,reflecting through more links(from 1893 to 2185)and a higher average degree(from 38.242 to 45.052)and density(from 0.390 to 0.469).Results of field trial demonstrated that PSBA could also decrease Cd content in lettuce plants and microbial composition in soil.This study indicated that PSBA could be served as an alternative material in bioremediation of Cd contamination in soil.展开更多
Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities an...Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities and is considered a functional source for promoting human health.However,propolis and its bioactive compounds have poor water solubility,rapid and intense metabolism,and low oral bioavailability,which limits their wide application.In this paper,the main bioactive substances in propolis were summarized,and the biological characteristics and therapeutic potential of propolis and its bioactive substances were discussed.In addition,this paper discussed the factors affecting the bioavailability of propolis and its functional ingredients,focusing on the research progress in improving the bioavailability and bioactivity of propolis and its functional ingredients using nanoencapsulation technology.Finally,the current situation of the global propolis market and the applications of propolis products in the pharmaceutical,food,cosmetic and other industrial fields were discussed,providing useful references for promoting the development of the propolis industry.展开更多
The study investigated using rice husk biochar(RHB)to immobilize TNT and RDX explosives in soil at demining sites in Amuru District,Uganda.RHB produced via pyrolysis at 550℃was applied at a rate of 5%w/w to soil samp...The study investigated using rice husk biochar(RHB)to immobilize TNT and RDX explosives in soil at demining sites in Amuru District,Uganda.RHB produced via pyrolysis at 550℃was applied at a rate of 5%w/w to soil samples spiked at 50μg·g^(−1)RDX or TNT.The Liquid chromatography-tandem mass spectrometer(LC-MS/MS)analysis showed that the RHB immobilized 56%-67%of RDX and 55%-69%of TNT.The biochar’s porous structure and surface functional groups facilitated the explosive adsorption,reducing bioavailability.This demonstrates RHB’s effectiveness as an environmentally friendly and cost-effective remediation strategy.展开更多
Utilizing transporter-mediated drug delivery to achieve effective oral absorption emerges as a promising strategy.Researchers have been concentrated on discovering solutions to the issues of low solubility and poor pe...Utilizing transporter-mediated drug delivery to achieve effective oral absorption emerges as a promising strategy.Researchers have been concentrated on discovering solutions to the issues of low solubility and poor permeability of insoluble drugs,whereas,current reports have revealed that drug transporter proteins are abundantly expressed in the mucosa of intestinal epithelial cells,and that their mediated drug absorption effectively improved the bioavailability of orally administered drugs.There are two main categories based on the transporter mechanism,which include the family of ATP-binding cassette(ABC)transporters with efflux effects that reduce drug bioavailability and the family of solute carriers(SLC)transporters with uptake effects that promote drug absorption,respectively.Thus,we review studies of intestinal transporter-mediated delivery of drugs to enhance oral absorption,including the types of intestinal transporters,distribution characteristics,and strategies for enhancing oral absorption using transporter-mediated drug delivery systems are summarized,with the aim of providing important theoretical references for the development of intestinal-targeted delivery system.展开更多
Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu upt...Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu uptake is controlled by natural dissolved organic Cu(DOCu)speciation(i.e.,complexed with the dissolved organic matter)that conventionally could be tested by model prediction or molecular-level characterizations in the lab,while DOCu uptake are hardly directly assessed.Thus,the new chemistrybiology insight into the mechanisms of the Cu uptake process in algae is urgent.The DOCu speciation transformation(organic DOCu to free Cu(II)ions),enzymatic reduction-induced valence change(reduction of free Cu(II)to Cu(I)ions),and algal Cu uptake at the algae-water interface are imitated.Herein,an intelligent system with DOCu colorimetric sensor is developed for real-time monitoring of newly generated Cu(I)ions.Deep learning with whole sample image-based characterization and powerful feature extraction capabilities facilitates colorimetric measurement.In this context,the Cu bioavailability with 7 kinds of organic ligands(e.g.,amino acids,organic acids,carbohydrates)can be predicted by the mimetic intelligent biosensor within 15.0min,i.e.,the DOCu uptake and speciation is successfully predicted and streamlined by the biomimetic approach.展开更多
Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug deli...Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug delivery systems have shown potential to enhance solubility,stability,and therapeutic efficacy.This review examines these advancements,focusing on their mechanisms and applications in improving TCM formulations.Cutting-edge techniques,such as microneedles,iontophoretic patches,and self-orienting applicators,are also discussed for their potential to revolutionize TCM delivery.By bridging traditional wisdom with modern innovations,this review emphasizes the transformative role of these strategies in advancing TCM's integration into contemporary medicine.展开更多
In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and mois...In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and moisture on the phosphorus(P)bioavailability of vegetable soil.Three temperature gradients[T1(15℃),T2(25℃),T3(35℃)]and three humidity gradients[W1(40%),W2(70%),W3(100%)]were set in the test.The results showed that it could improve the contents of HCl-P,Enzyme-P,Citrate-P,and Olsen-P in vegetable soil by increasing soil moisture content;temperature rise was helpful to increase the contents of HCl-P and Olsen-P,but it could reduce the content of Citrate-P.The contents of Enzyme-P and CaCl 2-P were significantly affected by hydrothermal interaction.Within a certain range of soil temperature and humidity,temperature and moisture had a positive coupling effect on soil P bioavailability components,and significantly affected soil P supply capacity.展开更多
Nano ceria(nano-CeO_(2))has been widely applied in various fields of industry and daily life,however,knowledge regarding the biological effects of nano-CeO_(2)with different intrinsic physicochemical properties remain...Nano ceria(nano-CeO_(2))has been widely applied in various fields of industry and daily life,however,knowledge regarding the biological effects of nano-CeO_(2)with different intrinsic physicochemical properties remains limited.In this study,we investigated the impact of nano-CeO_(2)with different properties on the growth of a typical environmental species(romaine lettuce,Lactuca sativa L.)by exposing the plant to four types of CeO_(2)(rod-like nano-CeO_(2)(RNC),cubic nano-CeO_(2)(CNC),spherical nano-CeO_(2)(SNC)and commercial irregular CeO_(2)(CIC))during the germination stage.The results indicated that different types of CeO_(2)exhibited varying inhibitory effects on plant growth.RNC and SNC significantly inhibited the elongation of roots and shoots,while CNC and CIC did not have a significant impact.We further examined the distribution and biotransformation of the four CeO_(2)in plant tissues using transmission electron microscopy(TEM)and synchrotron X-ray absorption near edge structure(XANES).Specifically,the positively charged RNC and SNC were more readily adsorbed onto the root surface,and needle-like nanoclusters were deposited in the intercellular space inside the roots.The absolute content of Ce(III)in the roots romaine lettuce was in the order of RNC>SNC>>CNC>>CIC.The size and shape(i.e.,exposed crystal surface)of the materials affected their reactivity and dissolution ratios,and zeta potentials affected their bioavailability,both of which influenced the overall contents of Ce^(3+)ions in plant tissues.Thus,these characteristics together led to different biological effects.These findings highlight the importance of considering the intrinsic properties of nano-CeO_(2)when assessing their environmental and biological effects.展开更多
Microbial participation in biofortification can improve the availability of selenium(Se)in soil and contribute to the enrichment of Se in crops.In this study,a selenite(Se(IV))reducing strain was isolated from Se-rich...Microbial participation in biofortification can improve the availability of selenium(Se)in soil and contribute to the enrichment of Se in crops.In this study,a selenite(Se(IV))reducing strain was isolated from Se-rich soil,and its Se transformation and bio-enhancement ability were studied.The strain was identified as Bacillus pseudomycoides and could reduce more than 93.48%of 1.0 m M Se(IV)in 54 h.The results of scanning electron microscope(SEM)and energy dispersive Xray spectrometry(EDS)showed that Se(IV)was reduced to Se(0),and Se nanoparticles(Se NPs)were eventually formed.In pot experiments,B.pseudomycoides SA14 could promote the bioavailable Se in soils and the concentration of Se in Brassica chinensis L..The concentrations of watersoluble Se,ion exchange Se and carbonate-binding Se in soil were increased by 23.13%,22.05%and 30.89%,respectively.The Se concentration of Brassica chinensis L.in pot experiments was increased by 145.05%.The relative abundance of Bacillus in soil increased from 0.97%to 2.08%in the pot experiments.As far as we know,this is the first report of Se reduction by B.pseudomycoides.This study might provide a prospective strategy for microbial fortification of Se in crops.展开更多
Vitamin D deficiency is disproportionately prevalent among overweight and obese children,with conventional explanations such as poor dietary intake or reduced sun exposure offering only partial insight.Emerging eviden...Vitamin D deficiency is disproportionately prevalent among overweight and obese children,with conventional explanations such as poor dietary intake or reduced sun exposure offering only partial insight.Emerging evidence reveals a multifactorial pathophysiology,including sequestration of vitamin D in adipose tissue,altered hepatic metabolism,diminished bioavailability,and inflammationinduced resistance at the tissue level.These mechanisms contribute to a functional deficiency,wherein serum 25-hydroxyvitamin D levels may remain suboptimal despite adequate intake or sun exposure.Obesity-related alterations in vitamin Dbinding proteins,receptor expression,and pro-inflammatory signaling further compromise biological activity.Current diagnostic criteria and supplementation guidelines do not fully reflect these physiological complexities,leading to underdiagnosis and insufficient treatment.Personalized approaches-incorporating higher,body composition-adjusted dosing and consideration of inflammatory status-are emerging as promising strategies to restore sufficiency and improve metabolic outcomes.While preliminary evidence supports the safety and efficacy of high-dose supplementation in this population,pediatric-specific clinical trials are lacking.This review synthesizes current understanding of the pathophysiological mechanisms underlying vitamin D deficiency in pediatric obesity and emphasizes the need for individualized,evidence-based interventions to optimize vitamin D status and overall health.展开更多
Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust d...Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust dietary exposure levels of risk factors;however,traditional planar Transwell models have limitations,such as cell dedifferentiation and lack of key intestinal components,necessitating a more physiologically relevant in vitro platform.This study introduces an innovative three-dimensional(3D)intestinal organoid model using a microfluidic chip to evaluate Cd bioavailability in food.Caco-2 cells were cultured on the chip to mimic small intestinal villi's 3D structure,mucus production,and absorption functions.The model's physiological relevance was thoroughly characterized,demonstrating the formation of a confluent epithelial monolayer with well-developed tight junctions(ZO-1),high microvilli density(F-actin),and significant mucus secretion(Alcian blue staining),closely resembling the physiological intestinal epithelium.Fluorescent particle tracking confirmed its ability to simulate intestinal transport and diffusion.The Cd bioavailability in rice measured by the 3D intestinal organoid model((9.07±0.21)%)was comparable to the mouse model((12.82±3.42)%)but significantly lower than the Caco-2 monolayer model((26.97±1.11)%).This 3D intestinal organoid model provides a novel and reliable strategy for in vitro assessment of heavy metal bioavailability in food,with important implications for food safety and risk assessment.展开更多
This paper analyzes challenges encountered during the scale-up production of small molecule inhibitors,focusing on synthesis efficiency,solubility/bioavailability,quality control,stability/storage,and side effect pred...This paper analyzes challenges encountered during the scale-up production of small molecule inhibitors,focusing on synthesis efficiency,solubility/bioavailability,quality control,stability/storage,and side effect prediction/control.To address these issues,targeted solutions leveraging modern technologies are proposed and implemented:synthesis efficiency and purity were significantly enhanced through process optimization,green chemistry principles,and efficient catalysts;solubility and bioavailability were improved utilizing solid dispersion and nano-crystal technologies;process scale-up was optimized with online monitoring systems and continuous flow chemistry,ensuring product quality consistency;computer-aided drug design(CADD)was employed to predict and mitigate potential side effects.These integrated approaches effectively addressed key bottlenecks in the industrial-scale manufacturing of small molecule inhibitors.展开更多
Background:This study focused on developing and optimizing a self-microemulsifying drug delivery system(SMEDDS)to improve Lafutidine’s solubility and bioavailability,thereby enhancing its effectiveness in treating ga...Background:This study focused on developing and optimizing a self-microemulsifying drug delivery system(SMEDDS)to improve Lafutidine’s solubility and bioavailability,thereby enhancing its effectiveness in treating gastric ulcers.Traditional formulations are less effective due to their limited water solubility and bioavailability.Methods:The study used solubility tests,pseudo-ternary phase diagrams,and central composite design(CCD)to optimize.The formulation was optimized by varying the oil concentration(10–40%)and surfactant/cosurfactant ratio(0.33–3.00),and then tested for droplet size,drug content,emulsification,phase stability,and in vitro dissolution.Results:The study found that the optimized formulation contained 14%Capmul PG 8NF oil,62%Labrasol surfactant,and 24%Tween 80 cosurfactant.This combination generated an average droplet size of 111.02 nm and improved drug release properties.Furthermore,the formulation was stable without phase separation,with a drug content of 88.2–99.8%.Conclusion:SMEDDS significantly improves lafutidine delivery by increasing solubility and absorption,thereby overcoming oral administration challenges.The system quickly formed small droplets in water and released the drug in 15 min.Enhancing lafutidine’s bioavailability may improve its efficacy in treating gastric ulcers,resulting in better patient outcomes and potentially lower dosing frequency.展开更多
Recently,the substance P(SP)/neurokinin-1 receptor(NK-1R)system has been found to be involved in various human pathophysiological disorders including the symptoms of coronavirus disease 2019(COVID-19).Besides,studies ...Recently,the substance P(SP)/neurokinin-1 receptor(NK-1R)system has been found to be involved in various human pathophysiological disorders including the symptoms of coronavirus disease 2019(COVID-19).Besides,studies in the oncological field have demonstrated an intricate correlation between the upregulation of NK-1R and the activation of SP/NK-1R system with the progression of multiple carcinoma types and poor clinical prognosis.These findings indicate that the modulation of SP/NK-1R system with NK-1R antagonists can be a potential broad-spectrum antitumor strategy.This review updates the latest potential and applications of NK-1R antagonists in the treatment of human diseases and cancers,as well as the underlying mechanisms.Furthermore,the strategies to improve the bioavailability and efficacy of NK-1R antagonist drugs are summarized,such as solid dispersion systems,nanonization,and nanoencapsulation.As a radiopharmaceutical therapeutic,the NK-1R antagonist aprepitant was originally developed as radioligand receptor to target NK-1R-overexpressing tumors.However,combining NK-1R antagonists with other drugs can produce a synergistic effect,thereby enhancing the therapeutic effect,alleviating the symptoms,and improving patients’quality of life in several diseases and cancers.展开更多
Exosomes as authigenous nanovesicles secreted by living cells represent a significant class of biomaterials.By virtue of their unique roles in intercellular communication,exosomes can mediate intercellular information...Exosomes as authigenous nanovesicles secreted by living cells represent a significant class of biomaterials.By virtue of their unique roles in intercellular communication,exosomes can mediate intercellular information/cargoes exchange as messenger and facilitate drug delivery as smart vehicles.Oral medication is the most clinically relied upon route of administration and can achieve both topical and systemic therapeutic effects after absorption.Exosomes and exosome-derived vectors have shown to be of high value in oral drug delivery,since they enable efficient oral delivery of therapeutic molecules by targeting intestinal epithelial cells.In recent years,exosome-biomimetic nanocarriers have emerged as an important catalyzer in innovating oral drug delivery systems.In this work,we roundly reviewed the biogenesis and functions of exosomes,their extraction and characterization methods,resources available for exosomes harvest,and design philosophy of exosome-derived vehicles,particularly highlighting the oral delivery application of exosome-biomimetic nanocarriers for diverse medicines.Accumulating evidence suggests that exosome-biomimetic nanocarriers hold great promise for oral delivery of intractable drugs with potential biopharmaceutic issues.展开更多
基金funded by Jiangsu Shuang Chuang Tuan Dui program (JSSCTD202147)Jiangsu Shuang Chuang Ren Cai program (JSSCRC2021541)+1 种基金Young Elite Scientists Sponsorship Program by CAST (2022QNRC001)the Initiation Funds of Yangzhou University for Distinguished Scientists
文摘Background Our previous studies demonstrated that divalent organic iron(Fe)proteinate sources with higher complexation or chelation strengths as expressed by the greater quotient of formation(Qf)values displayed higher Fe bioavailabilities for broilers.Sodium iron ethylenediaminetetraacetate(NaFeEDTA)is a trivalent organic Fe source with the strongest chelating ligand EDTA.However,the bioavailability of Fe when administered as NaFeEDTA in broilers and other agricultural animals remains untested.Herein,the chemical characteristics of 12 NaFeEDTA products were determined.Of these,one feed grade NaFeEDTA(Qf=2.07×10^(8)),one food grade NaFeEDTA(Qf=3.31×10^(8)),and one Fe proteinate with an extremely strong chelation strength(Fe-Prot ES,Qf value=8,590)were selected.Their bioavailabilities relative to Fe sulfate(FeSO_(4)·7H_(2)O)for broilers fed with a conventional corn-soybean meal diet were evaluated during d 1 to 21 by investigating the effects of the above Fe sources and added Fe levels on the growth performance,hematological indices,Fe contents,activities and gene expressions of Fe-containing enzymes in various tissues of broilers.Results NaFeEDTA sources varied greatly in their chemical characteristics.Plasma Fe concentration(PI),transferrin saturation(TS),liver Fe content,succinate dehydrogenase(SDH)activities in liver,heart,and kidney,catalase(CAT)activity in liver,and SDH mRNA expressions in liver and kidney increased linearly(P<0.05)with increasing levels of Fe supplementation.However,differences among Fe sources were detected(P<0.05)only for PI,liver Fe content,CAT activity in liver,SDH activities in heart and kidney,and SDH mRNA expressions in liver and kidney.Based on slope ratios from multiple linear regressions of the above indices on daily dietary analyzed Fe intake,the average bioavailabilities of Fe-Prot ES,feed grade NaFeEDTA,and food grade NaFeEDTA relative to the inorganic FeSO_(4)·7H_(2)O(100%)for broilers were 139%,155%,and 166%,respectively.Conclusions The bioavailabilities of organic Fe sources relative to FeSO_(4)·7H_(2)O were closely related to their Qf values,and NaFeEDTA sources with higher Qf values showed higher Fe bioavailabilities for broilers fed with a conventional corn-soybean meal diet.
基金supported by the National Natural Science Foundation Committee of China(81971212,81601129)Shenyang Young and Middle-aged Technological Innovation Talent Support Program(RC210268)Liaoning Province Natural Science Foundation(2023-MS-153).
文摘Epilepsy is a devastating neurological condition that affects over 70 million people worldwide.Apart from idiopathic epilepsy,numerous diseases have been reported to cause secondary epilepsy.Polyphenols,ubiquitously existing in fruits and vegetables,has become a promising neuroprotective candidate against multiple neurological abnormalities due to its interplay with gut microbiome composed of the bacterial population in gastrointestinal system.This bioactive compound is also being tested for the management of epileptogenesis.However,there is still insufficient evidence from mechanistic studies to demonstrate the causal relationship between anti-epileptic effect of polyphenols and microbial alteration.In this review,we provide the brief overview of epilepsy,polyphenols and gut microbiota.We then analysis the association of polyphenols and gut microbiota particularly in the epilepsy and symptomatic seizures-induced by epilepsy related disorders.We also discuss the possibility for the combined application with probiotics to improve the bioavailability and bioaccessibility of polyphenols for expanding its anti-epileptic function.We finally summarize the therapeutic potential of anti-seizure polyphenols through affecting gut microbiome,and propose that the anti-epileptic effect of polyphenols may be tightly relevant to intestinal bacterial flora for overcoming epilepsy and its comorbidities simultaneously.Therefore,the dietary polyphenols targeting specific bacteria may achieve the outcome of‘one stone,two birds’.
文摘Guava(Psidium guajava L.),a plant belonging to the Myrtaceae family,holds significant medicinal and nutritional values.Leaves of the plant are described to be elliptical with a dark green color and are utilized in the treatment of gastrointestinal and respiratory issues along with increasing the platelet count in patients suffering from dengue.In this review paper,the nutritional composition and bioactive compounds of guava leaves,including proteins,vitamins,minerals,and polysaccharides,have been reviewed.The methods of extraction of bioactive compounds from guava leaves and their bioactivities,including antioxidant,anti-diabetic,and anti-cancer potential,have been explored.Further,encapsulation techniques for improving the transport of bioactive compounds and living cells into foods have been studied.The application of guava leaves in different food systems such as herbal tea,pork sausage,chocolates,jelly,meals for chickens,functional beverages,and as antibacterial agents in food preservatives has also been investigated.The findings of this review illustrated that the phytochemicals present in guava leaves showed excellent antimicrobial and antioxidant properties.Encapsulation appears to be a promising technique for improving the stability,bioavailability,and controlled release of bioactive chemicals extracted from guava leaves.Different methods for the encapsulation of bioactive compounds employed and applied in distinct food systems showed preservation of phytochemicals,improved bioactivities,and nutritional values.Overall,this review paper demonstrated how guava leaves,an abundant source of bioactive compounds,can be used as a multipurpose component to create functional foods,edible coatings,and active packaging to enhance the nutritional,antioxidant,and antimicrobial properties of various food systems that have qualities that promote health.
文摘BACKGROUND The rising global burden of liver diseases,such as non-alcoholic fatty liver disease and liver fibrosis,has necessitated innovative therapeutic approaches.Plant-based therapies,recognized for their anti-inflammatory and antioxidant properties,have shown promising effects.However,poor bioavailability limits their clinical application.AIM To map global research trends,key contributors,and emerging themes in plant-based therapies combined with advanced drug delivery systems for liver health.METHODS Using the Scopus database,645 documents were retrieved and analyzed using bibliometric tools Biblioshiny and VOSviewer.Analysis focused on publication trends,geographical contributions,and advancements in drug delivery technologies,including nanoparticles,liposomes,and polymeric micelles.Metrics such as publication growth rate,authorship collaboration,and thematic clustering were assessed.RESULTS The dataset spans 43 years(1981-2024),with an annual growth rate of 11.09%in the number of publications.Research output is dominated by China(33%),followed by the United States(24%)and India(18%).Collaborative studies accounted for 24.34%of publications,with an average of 5.81 co-authors per document.Key innovations include nanoparticle encapsulation of curcumin and silymarin,improving bioavailability by up to 85%.Highly cited studies demonstrated the antioxidant,anti-inflammatory,and anti-fibrotic properties of these compounds.For instance,curcumin nanoparticles showed a 70%improvement in solubility,and silymarin liposomal formulations enhanced therapeutic efficiency by 62%.Thematic analysis revealed a transition from basic clinical observations to molecular and pharmacokinetic research,with a focus on oxidative stress mitigation and hepatoprotection.CONCLUSION This study highlights the growing synergy between plant-based therapies and advanced drug delivery systems,with significant contributions from Asian and Western countries.Future efforts should prioritize clinical trials,standardization of plant extract formulations,and interdisciplinary approaches to maximize therapeutic outcomes.The findings provide a foundation for integrating plant-derived compounds into evidence-based hepatological therapies,addressing critical challenges in bioavailability and safety.
文摘The intricate interplay between natural compounds like curcumin and the gut microbiome has gained significant attention in recent years due to their potential therapeutic implications in various health conditions.Curcumin,a polyphenolic compound derived from turmeric,exhibits diverse pharmacological properties,including anti-inflammatory,antioxidant,and anticancer effects.Understanding how curcumin modulates gut microbiota composition and function is crucial for elucidating its therapeutic mechanisms.This review examines the current literature on the interactions between curcumin and the gut microbiome.A systematic search of relevant databases was conducted to identify studies investigating the effects of curcumin on gut microbial diversity and abundance.Key findings from studies exploring curcumin's efficacy in neurological disorders,gastrointestinal diseases,and metabolic dysfunction are synthesized and discussed.Studies have demonstrated that curcumin supplementation can modulate gut microbiota composition and function,leading to beneficial effects on gut health and homeostasis.Mechanisms underlying curcumin's therapeutic effects include immune modulation,neuroprotection,and inflammation regulation.However,challenges such as poor bioavailability and safety concerns remain significant hurdles to overcome.The interactions between curcumin and the gut microbiome hold promise for therapeutic interventions in a diverse range of health conditions.Further research is needed to optimize curcumin formulations,improve bioavailability,and address safety concerns.
基金supported by the Science and Technology Programs of Department of Natural Resources of Zhejiang Province,China(No.2020006)the Zhejiang Provincial Natural Science Foundation of China(No.LGF22D030001)the Key R&D Program of Zhejiang Province,China(No.2021C04020)。
文摘Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.In this work,we studied the impact of phosphate solubilizing bacterial agent(PSBA)on Cd bioavailability,microbial communities in soil and Cd accumulation in lettuce plants with pot experiment and field trial.Results of pot experiment showed that PSBA could decrease the bioavailability of Cd(Cd-acid extractable from 3.30 to 2.34mg/kg,Cd-reducible from 1.94 to 1.56 mg/kg),promote lettuce plants growth(increased by 33.85%height and by 33.65%fresh weight)and reduce the accumulation of Cd(from 5.85 to 3.73 mg/kg)in lettuce plants.High-throughput sequencing identified that PSBA could change the composition and structure of the soil microbial communities.The relative abundances of the three ecologically beneficial bacterial families of Pseudomonadaceae,Burkholderiaceae,and Enterobacteriaceae increased from 2.29%to 5.13%,0.56%to 5.24%,and 1.87%to 16.93%,respectively.And the former two were positively correlated with redox potential(Eh)(R^(2)=0.474,p<0.05,R^(2)=0.590,p<0.01,respectively).The bacterial networks were more complex in PSBA treatment,reflecting through more links(from 1893 to 2185)and a higher average degree(from 38.242 to 45.052)and density(from 0.390 to 0.469).Results of field trial demonstrated that PSBA could also decrease Cd content in lettuce plants and microbial composition in soil.This study indicated that PSBA could be served as an alternative material in bioremediation of Cd contamination in soil.
基金supported by the National Natural Science Foundation of China(31972087)the earmarked fund for China Agriculture Research System-Bee(CARS-44-KXJ17)the Science and Technology Innovation Project of Chinese Academy of Agricultural Sciences(CAAS-ASTIP-2021-IAR)。
文摘Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities and is considered a functional source for promoting human health.However,propolis and its bioactive compounds have poor water solubility,rapid and intense metabolism,and low oral bioavailability,which limits their wide application.In this paper,the main bioactive substances in propolis were summarized,and the biological characteristics and therapeutic potential of propolis and its bioactive substances were discussed.In addition,this paper discussed the factors affecting the bioavailability of propolis and its functional ingredients,focusing on the research progress in improving the bioavailability and bioactivity of propolis and its functional ingredients using nanoencapsulation technology.Finally,the current situation of the global propolis market and the applications of propolis products in the pharmaceutical,food,cosmetic and other industrial fields were discussed,providing useful references for promoting the development of the propolis industry.
文摘The study investigated using rice husk biochar(RHB)to immobilize TNT and RDX explosives in soil at demining sites in Amuru District,Uganda.RHB produced via pyrolysis at 550℃was applied at a rate of 5%w/w to soil samples spiked at 50μg·g^(−1)RDX or TNT.The Liquid chromatography-tandem mass spectrometer(LC-MS/MS)analysis showed that the RHB immobilized 56%-67%of RDX and 55%-69%of TNT.The biochar’s porous structure and surface functional groups facilitated the explosive adsorption,reducing bioavailability.This demonstrates RHB’s effectiveness as an environmentally friendly and cost-effective remediation strategy.
基金funded by the National Natural Science Foundation of China(No.82304730)the Project of Academic and Technical Leaders in Major Disciplines in Jiangxi Province(No.20212BCJL23060)+3 种基金the Natural Science Foundation of Jiangxi Province(No.20232BAB216128)the Project of Jiangxi Provincial Department of Education(No.GJJ2200977)the Jiangxi University of Chinese Medicine Science and Technology Innovation Team Development Program(Nos.CXTD-22004,CXTD-22008)the PhD Startup Foundation of Affiliated Hospital of Jiangxi University of Chinese Medicine(No.23KYQDZJ02).
文摘Utilizing transporter-mediated drug delivery to achieve effective oral absorption emerges as a promising strategy.Researchers have been concentrated on discovering solutions to the issues of low solubility and poor permeability of insoluble drugs,whereas,current reports have revealed that drug transporter proteins are abundantly expressed in the mucosa of intestinal epithelial cells,and that their mediated drug absorption effectively improved the bioavailability of orally administered drugs.There are two main categories based on the transporter mechanism,which include the family of ATP-binding cassette(ABC)transporters with efflux effects that reduce drug bioavailability and the family of solute carriers(SLC)transporters with uptake effects that promote drug absorption,respectively.Thus,we review studies of intestinal transporter-mediated delivery of drugs to enhance oral absorption,including the types of intestinal transporters,distribution characteristics,and strategies for enhancing oral absorption using transporter-mediated drug delivery systems are summarized,with the aim of providing important theoretical references for the development of intestinal-targeted delivery system.
基金supported by the National Natural Science Foundation of China(No.22074058,S.Li).
文摘Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu uptake is controlled by natural dissolved organic Cu(DOCu)speciation(i.e.,complexed with the dissolved organic matter)that conventionally could be tested by model prediction or molecular-level characterizations in the lab,while DOCu uptake are hardly directly assessed.Thus,the new chemistrybiology insight into the mechanisms of the Cu uptake process in algae is urgent.The DOCu speciation transformation(organic DOCu to free Cu(II)ions),enzymatic reduction-induced valence change(reduction of free Cu(II)to Cu(I)ions),and algal Cu uptake at the algae-water interface are imitated.Herein,an intelligent system with DOCu colorimetric sensor is developed for real-time monitoring of newly generated Cu(I)ions.Deep learning with whole sample image-based characterization and powerful feature extraction capabilities facilitates colorimetric measurement.In this context,the Cu bioavailability with 7 kinds of organic ligands(e.g.,amino acids,organic acids,carbohydrates)can be predicted by the mimetic intelligent biosensor within 15.0min,i.e.,the DOCu uptake and speciation is successfully predicted and streamlined by the biomimetic approach.
文摘Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug delivery systems have shown potential to enhance solubility,stability,and therapeutic efficacy.This review examines these advancements,focusing on their mechanisms and applications in improving TCM formulations.Cutting-edge techniques,such as microneedles,iontophoretic patches,and self-orienting applicators,are also discussed for their potential to revolutionize TCM delivery.By bridging traditional wisdom with modern innovations,this review emphasizes the transformative role of these strategies in advancing TCM's integration into contemporary medicine.
基金Supported by Open Fund of Engineering Research Center of Ministry of Education for Wetland Ecology and Agricultural Utilization(KF202015).
文摘In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and moisture on the phosphorus(P)bioavailability of vegetable soil.Three temperature gradients[T1(15℃),T2(25℃),T3(35℃)]and three humidity gradients[W1(40%),W2(70%),W3(100%)]were set in the test.The results showed that it could improve the contents of HCl-P,Enzyme-P,Citrate-P,and Olsen-P in vegetable soil by increasing soil moisture content;temperature rise was helpful to increase the contents of HCl-P and Olsen-P,but it could reduce the content of Citrate-P.The contents of Enzyme-P and CaCl 2-P were significantly affected by hydrothermal interaction.Within a certain range of soil temperature and humidity,temperature and moisture had a positive coupling effect on soil P bioavailability components,and significantly affected soil P supply capacity.
基金funded by National Key R&D Program of China(2022YFA1207600)the National Natural Science Foundation of China(12175263,11875267,and 12075262).
文摘Nano ceria(nano-CeO_(2))has been widely applied in various fields of industry and daily life,however,knowledge regarding the biological effects of nano-CeO_(2)with different intrinsic physicochemical properties remains limited.In this study,we investigated the impact of nano-CeO_(2)with different properties on the growth of a typical environmental species(romaine lettuce,Lactuca sativa L.)by exposing the plant to four types of CeO_(2)(rod-like nano-CeO_(2)(RNC),cubic nano-CeO_(2)(CNC),spherical nano-CeO_(2)(SNC)and commercial irregular CeO_(2)(CIC))during the germination stage.The results indicated that different types of CeO_(2)exhibited varying inhibitory effects on plant growth.RNC and SNC significantly inhibited the elongation of roots and shoots,while CNC and CIC did not have a significant impact.We further examined the distribution and biotransformation of the four CeO_(2)in plant tissues using transmission electron microscopy(TEM)and synchrotron X-ray absorption near edge structure(XANES).Specifically,the positively charged RNC and SNC were more readily adsorbed onto the root surface,and needle-like nanoclusters were deposited in the intercellular space inside the roots.The absolute content of Ce(III)in the roots romaine lettuce was in the order of RNC>SNC>>CNC>>CIC.The size and shape(i.e.,exposed crystal surface)of the materials affected their reactivity and dissolution ratios,and zeta potentials affected their bioavailability,both of which influenced the overall contents of Ce^(3+)ions in plant tissues.Thus,these characteristics together led to different biological effects.These findings highlight the importance of considering the intrinsic properties of nano-CeO_(2)when assessing their environmental and biological effects.
基金supported by the Open Project of Technology Innovation Center for Ecological Evaluation and Remediation of Agricultural Land in Plain Area,MNR(No.ZJGCJ202001)Basic Public Welfare Research Program of Zhejiang Province(No.LGF22D030001)Jiande City(No.HX2022B-011)。
文摘Microbial participation in biofortification can improve the availability of selenium(Se)in soil and contribute to the enrichment of Se in crops.In this study,a selenite(Se(IV))reducing strain was isolated from Se-rich soil,and its Se transformation and bio-enhancement ability were studied.The strain was identified as Bacillus pseudomycoides and could reduce more than 93.48%of 1.0 m M Se(IV)in 54 h.The results of scanning electron microscope(SEM)and energy dispersive Xray spectrometry(EDS)showed that Se(IV)was reduced to Se(0),and Se nanoparticles(Se NPs)were eventually formed.In pot experiments,B.pseudomycoides SA14 could promote the bioavailable Se in soils and the concentration of Se in Brassica chinensis L..The concentrations of watersoluble Se,ion exchange Se and carbonate-binding Se in soil were increased by 23.13%,22.05%and 30.89%,respectively.The Se concentration of Brassica chinensis L.in pot experiments was increased by 145.05%.The relative abundance of Bacillus in soil increased from 0.97%to 2.08%in the pot experiments.As far as we know,this is the first report of Se reduction by B.pseudomycoides.This study might provide a prospective strategy for microbial fortification of Se in crops.
文摘Vitamin D deficiency is disproportionately prevalent among overweight and obese children,with conventional explanations such as poor dietary intake or reduced sun exposure offering only partial insight.Emerging evidence reveals a multifactorial pathophysiology,including sequestration of vitamin D in adipose tissue,altered hepatic metabolism,diminished bioavailability,and inflammationinduced resistance at the tissue level.These mechanisms contribute to a functional deficiency,wherein serum 25-hydroxyvitamin D levels may remain suboptimal despite adequate intake or sun exposure.Obesity-related alterations in vitamin Dbinding proteins,receptor expression,and pro-inflammatory signaling further compromise biological activity.Current diagnostic criteria and supplementation guidelines do not fully reflect these physiological complexities,leading to underdiagnosis and insufficient treatment.Personalized approaches-incorporating higher,body composition-adjusted dosing and consideration of inflammatory status-are emerging as promising strategies to restore sufficiency and improve metabolic outcomes.While preliminary evidence supports the safety and efficacy of high-dose supplementation in this population,pediatric-specific clinical trials are lacking.This review synthesizes current understanding of the pathophysiological mechanisms underlying vitamin D deficiency in pediatric obesity and emphasizes the need for individualized,evidence-based interventions to optimize vitamin D status and overall health.
基金supported by National key research and development program of China(2022YFF1102500)。
文摘Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust dietary exposure levels of risk factors;however,traditional planar Transwell models have limitations,such as cell dedifferentiation and lack of key intestinal components,necessitating a more physiologically relevant in vitro platform.This study introduces an innovative three-dimensional(3D)intestinal organoid model using a microfluidic chip to evaluate Cd bioavailability in food.Caco-2 cells were cultured on the chip to mimic small intestinal villi's 3D structure,mucus production,and absorption functions.The model's physiological relevance was thoroughly characterized,demonstrating the formation of a confluent epithelial monolayer with well-developed tight junctions(ZO-1),high microvilli density(F-actin),and significant mucus secretion(Alcian blue staining),closely resembling the physiological intestinal epithelium.Fluorescent particle tracking confirmed its ability to simulate intestinal transport and diffusion.The Cd bioavailability in rice measured by the 3D intestinal organoid model((9.07±0.21)%)was comparable to the mouse model((12.82±3.42)%)but significantly lower than the Caco-2 monolayer model((26.97±1.11)%).This 3D intestinal organoid model provides a novel and reliable strategy for in vitro assessment of heavy metal bioavailability in food,with important implications for food safety and risk assessment.
文摘This paper analyzes challenges encountered during the scale-up production of small molecule inhibitors,focusing on synthesis efficiency,solubility/bioavailability,quality control,stability/storage,and side effect prediction/control.To address these issues,targeted solutions leveraging modern technologies are proposed and implemented:synthesis efficiency and purity were significantly enhanced through process optimization,green chemistry principles,and efficient catalysts;solubility and bioavailability were improved utilizing solid dispersion and nano-crystal technologies;process scale-up was optimized with online monitoring systems and continuous flow chemistry,ensuring product quality consistency;computer-aided drug design(CADD)was employed to predict and mitigate potential side effects.These integrated approaches effectively addressed key bottlenecks in the industrial-scale manufacturing of small molecule inhibitors.
文摘Background:This study focused on developing and optimizing a self-microemulsifying drug delivery system(SMEDDS)to improve Lafutidine’s solubility and bioavailability,thereby enhancing its effectiveness in treating gastric ulcers.Traditional formulations are less effective due to their limited water solubility and bioavailability.Methods:The study used solubility tests,pseudo-ternary phase diagrams,and central composite design(CCD)to optimize.The formulation was optimized by varying the oil concentration(10–40%)and surfactant/cosurfactant ratio(0.33–3.00),and then tested for droplet size,drug content,emulsification,phase stability,and in vitro dissolution.Results:The study found that the optimized formulation contained 14%Capmul PG 8NF oil,62%Labrasol surfactant,and 24%Tween 80 cosurfactant.This combination generated an average droplet size of 111.02 nm and improved drug release properties.Furthermore,the formulation was stable without phase separation,with a drug content of 88.2–99.8%.Conclusion:SMEDDS significantly improves lafutidine delivery by increasing solubility and absorption,thereby overcoming oral administration challenges.The system quickly formed small droplets in water and released the drug in 15 min.Enhancing lafutidine’s bioavailability may improve its efficacy in treating gastric ulcers,resulting in better patient outcomes and potentially lower dosing frequency.
基金This work was supported by the Zhejiang Provincial Natural Science Foundation of China(No.LD22H310004)the“Pioneer”and“Leading Goose”R&D Program of Zhejiang(No.2022C03005),China.
文摘Recently,the substance P(SP)/neurokinin-1 receptor(NK-1R)system has been found to be involved in various human pathophysiological disorders including the symptoms of coronavirus disease 2019(COVID-19).Besides,studies in the oncological field have demonstrated an intricate correlation between the upregulation of NK-1R and the activation of SP/NK-1R system with the progression of multiple carcinoma types and poor clinical prognosis.These findings indicate that the modulation of SP/NK-1R system with NK-1R antagonists can be a potential broad-spectrum antitumor strategy.This review updates the latest potential and applications of NK-1R antagonists in the treatment of human diseases and cancers,as well as the underlying mechanisms.Furthermore,the strategies to improve the bioavailability and efficacy of NK-1R antagonist drugs are summarized,such as solid dispersion systems,nanonization,and nanoencapsulation.As a radiopharmaceutical therapeutic,the NK-1R antagonist aprepitant was originally developed as radioligand receptor to target NK-1R-overexpressing tumors.However,combining NK-1R antagonists with other drugs can produce a synergistic effect,thereby enhancing the therapeutic effect,alleviating the symptoms,and improving patients’quality of life in several diseases and cancers.
基金supported by Guangdong Basic and Applied Basic Research Foundation(No.2023A1515012326)Major International(Regional)Joint Research Project of National Natural Science Foundation of China(No.82020108033)+1 种基金Science and Technology Projects in Guangzhou(No.202103000091)Sanming Project of Medicine in Shenzhen(No.202211003)。
文摘Exosomes as authigenous nanovesicles secreted by living cells represent a significant class of biomaterials.By virtue of their unique roles in intercellular communication,exosomes can mediate intercellular information/cargoes exchange as messenger and facilitate drug delivery as smart vehicles.Oral medication is the most clinically relied upon route of administration and can achieve both topical and systemic therapeutic effects after absorption.Exosomes and exosome-derived vectors have shown to be of high value in oral drug delivery,since they enable efficient oral delivery of therapeutic molecules by targeting intestinal epithelial cells.In recent years,exosome-biomimetic nanocarriers have emerged as an important catalyzer in innovating oral drug delivery systems.In this work,we roundly reviewed the biogenesis and functions of exosomes,their extraction and characterization methods,resources available for exosomes harvest,and design philosophy of exosome-derived vehicles,particularly highlighting the oral delivery application of exosome-biomimetic nanocarriers for diverse medicines.Accumulating evidence suggests that exosome-biomimetic nanocarriers hold great promise for oral delivery of intractable drugs with potential biopharmaceutic issues.
