In this study,thyme essential oil(TEO)nanoemulsion(tPTNs)was constructed with transglutaminase(TGase)-modified potato protein,and its antibacterial activity and mechanism of action were evaluated and explored.Results ...In this study,thyme essential oil(TEO)nanoemulsion(tPTNs)was constructed with transglutaminase(TGase)-modified potato protein,and its antibacterial activity and mechanism of action were evaluated and explored.Results indicated that tPTNs exhibited great antibacterial activity against both Staphylococcus aureus and Escherichia coli,with minimal inhibitory concentration(MIC)and minimum bactericidal concentration(MBC)of 2.5 and 5.0 mg/mL,respectively.Also,the antibacterial effects of tPTNs were concentration-dependent.We observed a significant decrease in the absolute value of the zeta potential,and significant increases in particle size,cell membrane hydrophobicity,conductivity,the release of metal ions,and the leakage of nucleic acid as the concentration of tPTNs increased from 0 mg/mL to MBC.Furthermore,sodium dodecyl sulphate-polyacrylamide gel electrophoresis(SDS-PAGE)demonstrated that protein synthesis was inhibited or even disrupted.Analysis by liquid chromatography-mass spectrometry(LC-MS)indicated that treatment with tPTNs caused significant changes in bacterial metabolites,1117 and 692 differential metabolites being found for S.aureus and E.coli,respectively.The differential metabolites were involved in nucleotide metabolism,amino acid metabolism,tricarboxylic acid cycle and other metabolic pathways.These findings provide valuable insights for the application of thyme essential oil as an efficient antibacterial agent and for the understanding of its mechanism of action.展开更多
Nanoemulsions have garnered significant attention in the cosmetic industry due to their ability to enhance ingredient dispersion,improve topical absorption,and enable targeted delivery of active compounds within the s...Nanoemulsions have garnered significant attention in the cosmetic industry due to their ability to enhance ingredient dispersion,improve topical absorption,and enable targeted delivery of active compounds within the skin layers.These nano-sized emulsions allow skincare products,like moisturizers,anti-aging creams,and sunscreens,to penetrate the skin more deeply and be absorbed better.They can also release their active ingredients gradually,which enhances the product's effectiveness.Additionally,nanoemulsions are more stable,meaning they protect ingredients from breaking down or losing their effectiveness,which helps extend the shelf life of the products.However,despite their advantages,nanoemulsions come with challenges,such as difficulties in producing them on a large scale,meeting safety regulations,and ensuring they remain stable over time.Future research will likely focus on improving how these formulations are made,making sure they are safe to use,and exploring more environmentally friendly and personalized solutions for skincare.As this technology develops,nanoemulsions have the potential to transform cosmetic formulations by offering more innovative and effective skincare options.展开更多
Encapsulation and protection of hesperidin(HES)in mung bean protein isolate(MPI)-dextran(DX)conjugatestabilized nanoemulsions(MDC NEs)were investigated in this study.The degree of grafting of MDC prepared by a dry-hea...Encapsulation and protection of hesperidin(HES)in mung bean protein isolate(MPI)-dextran(DX)conjugatestabilized nanoemulsions(MDC NEs)were investigated in this study.The degree of grafting of MDC prepared by a dry-heating method reached 39.70%±0.01% under the optimal conditions of MPI/DX mass ratio 1:2.3,reaction temperature 58.8℃,and reaction time 4 d.Moreover,the analyses of Fourier infrared spectroscopy,intrinsic fluorescence spectroscopy,surface hydrophobicity,and thermal stability further confirmed the covalent grafting of dextran onto MPI molecules.When encapsulated in MDC NEs at 80 MPa for three times by highpressure homogenization,the encapsulation efficiency and loading capacity of HES were 63.62%±0.01%and 0.40±0.00 g/g,respectively.The encapsulated HES exhibited higher antioxidant activity and stronger light and storage stability than the free HES.Additionally,the incorporation of HES inhibited the formation of lipid peroxides in the nanoemulsions.The findings suggest that glycosylation combined with high-pressure homogenization is an effective strategy for enhancing the stability of MPI-based emulsions and improving their encapsulation of HES.This study provides a promising approach for the development of innovative food and beverage products based on MPI emulsions or new materials for encapsulating fat-soluble bioactive compounds.展开更多
This study focuses on the preparation,and optimization of the nanoemulsions coorporating with pumpkin seed oil,grape seed oil,and grapefruit essential oil using the phase inversion temperature(PIT)technique.The resear...This study focuses on the preparation,and optimization of the nanoemulsions coorporating with pumpkin seed oil,grape seed oil,and grapefruit essential oil using the phase inversion temperature(PIT)technique.The research investigated the impact of surfactant types and concentrations on critical nanoemulsion properties,including droplet size,polydispersity index(PDI),and zeta potential.Using a Box-Behnken Design(BBD)model,the formulation was optimized containing 6.0%plant oils,10.0%Tween 80,2.0%Span 80,and 1.0%lecithin to achieve nano-sized droplets(33.52 nm),with a low PDI(0.205),and a stable zeta potential(15.49 mV).The antioxidant activity,was evaluated through 2,2-diphenyl-1-picrylhydrazyl(DPPH)radical scavenging assays,demonstrating its outstanding efficacy.And the optimized nanoemulsion showed a radical-scavenging capacity exceeding 2250μg ascorbic acid equivalents/g,significantly outperforming non-nanoemulsified oils.Stability testing under various environmental conditions highlighted exceptional robustness,with refrigerated samples maintaining structural integrity,minimal particle size growth,and consistent physicochemical properties over a 30-day storage period.The results suggest that the plant oil-based nanoemulsions exhibit strong antioxidant potential,offering a promising natural treatment for their application in cosmeceutical and therapeutic formulations.展开更多
Dietary supplementation with plant-derivedα-linolenic acid(ALA)has the potential to alleviate the insufficient intake of global n-3 long-chain polyunsaturated fatty acids(n-3 LCPUFAs),but faces the bottleneck of high...Dietary supplementation with plant-derivedα-linolenic acid(ALA)has the potential to alleviate the insufficient intake of global n-3 long-chain polyunsaturated fatty acids(n-3 LCPUFAs),but faces the bottleneck of highβ-oxidation consumption,oxidative susceptibility,and low conversion efficiency.The current study investigated how flax lignans with different degrees of polymerization and glycosylation affect the conversion of ALA to n-3 LCPUFAs in mice over 35 days of administering sunflower phospholipid-stabilized flaxseed oil nanoemulsions.Results showed that flax lignan macromolecules(FLM)increased hepatic protein expression of elongase of very long chain fatty acid 5(Elovl5,24.2%)and fatty acid desaturase 2(Fads2,44.7%),thereby positively regulating ALA conversion pathways and raising serum eicosapentaenoic acid(EPA)levels(52.7%)via liver lipid re-efflux.Secoisolariciresinol diglucoside(SDG)enhanced ALA desaturation by upregulating hepatic protein expression of Fads1(30.4%)and Fads2(45.6%),increasing serum EPA levels(55.9%)and hepatic docosahexaenoic acid(DHA)levels(10%).Secoisolariciresinol(SECO)elevated hepatic protein expression of Elovl2(30.7%),Elovl5(11.7%),Fads1(37.9%),and Fads2(24.1%),but also increased carnitine palmitoyltransferase 1a(45.2%),leading to decreased ALA,EPA,and DHA levels in serum and liver.Therefore,in comparison,FLM and SDG emerge as the dominant structural units that positively regulate the conversion of ALA.These findings lay a groundwork for designing precise dietary delivery systems to enhance the conversion to n-3 LCPUFAs.展开更多
[Objective] The aim was to obtain the preparation technology of the pomegranate peel polyphenol nanoemulsion. [Method] The pomegranate peel polyphe- nol nanoemulsion was prepared by the titration methods and the pseud...[Objective] The aim was to obtain the preparation technology of the pomegranate peel polyphenol nanoemulsion. [Method] The pomegranate peel polyphe- nol nanoemulsion was prepared by the titration methods and the pseudo ternary dia- gram. The effect of various elements on the formation of the nanoemulsion was stud- ied. [Results] The optimal prescription of the pomegranate peel polyphenol nanoemul- sion was 4.4%（w/w） of pomegranate peel polyphenol, 34.1%（w/w） of EL-40, 17.1%（w/w） of anhydrous ethanol, 5.7%（w/w） of IPM and 38.7%（w/w） of distilled water. [Conclusion] It is feasible to produce the pomegranate peel polyphenol nanoemulsion by the titration methods and the pseudo ternary diagram. It consists of pomegranate peel polyphe- nol, EL-40, anhydrous ethanol, IPM and distilled water. There is 4.4%（w/w） of the pomegranate peel polyphenol in the nanoemuJsion.展开更多
[ Objective] The paper was to prepare bifenthrin nanoemulsions, and to characterize its property. [ Method ] Oil in water type of bifenthrin nanoemul- sions was prepared using emulsion phase transition method at const...[ Objective] The paper was to prepare bifenthrin nanoemulsions, and to characterize its property. [ Method ] Oil in water type of bifenthrin nanoemul- sions was prepared using emulsion phase transition method at constant temperature of 25℃. The formation mechanism of nanoemulsions was investigated, and the property of bffenthrin nanoemulsions was characterized by dynamic light scattering（DIS）, transmission electron microscopy （TEM）, contact angle meter, interfa- cial tension meter and high performance liquid chromatogTaphy （HPLC）. [ Result ] Phase transition occurred during the formation progress of bifenthrin nanoemul- sions ; the particles of nancomulsions system was spherical, and the particle size was mainly distributed in the range of 25 -30 ran; the contact angle on paraffin was less than 90° with good wetting effect; the surface tension was less than 40 mN/m, and the emulsification effect was also good, so the utilization rate of bifenthrin nancomulsions was improved. HPLC results showed that bffenthrin was not easy to decompose or precipitate with good stability. [ Conclusion] The result provided basis for the preparation of new types of insecticides.展开更多
Salidroside(SAL)is a phenolic substance with high solubility and low permeability,which make it easy to cause the efflux effect of P-glycoprotein and degradation of intestinal flora,resulting in lower bioavailability....Salidroside(SAL)is a phenolic substance with high solubility and low permeability,which make it easy to cause the efflux effect of P-glycoprotein and degradation of intestinal flora,resulting in lower bioavailability.The aim of this study was to develop and optimize a water-in-oil nanoemulsion of SAL(w/o SAL-N)to explore its suitability in oral drug delivery systems.In this work,SAL-N was successfully prepared by water titration method at K_(m)=1 to construct the pseudo-ternary phase diagrams.Physical characterization including the average viscosity,pH,refractive index,particle size,PDI,TEM,DSC,the content of SAL,and stability study were performed.It was evaluated for drug release in vitro and pharmacokinetic studies in vivo.The optimized nanoemulsion formulation consisted of Labrafil M 1944 CS(63%),Span-80/Tween-80/EtOH(27%)and 200 mg·mL^(-1) SAL solution(SAL-SOL)(10%).Low viscosity and suitable pH were expected for the nanoemulsion.The spherical morphology and nanoscale size of SAL-N enhanced the stability of the nanoemulsion system.In vitro drug release showed that SAL-N had a better controlled release property than SAL-SOL at earlier time points.The pharmacokinetic studies exhibited that SAL-N had significantly higher in t_(1/2)(2.11-fold),AUC_(0-48 h)(1.75-fold)and MRT0-48 h(2.63-fold)than SAL-SOL(P<0.01).The w/o SAL-N prepared in this work can be effectively delivered via the oral route.It can be seen w/o nanoemulsion is a strategy for the drug with polyphenols to delay the release,enhance oral absorption and reduce metabolic rate.展开更多
A Hippophae rhamnoides Linn oil nanoemulsion was developed, and its physicochemical properties and in vitro transdermal characteristics were investigated. Then its skin irritation was investigated. The optimum Hippoph...A Hippophae rhamnoides Linn oil nanoemulsion was developed, and its physicochemical properties and in vitro transdermal characteristics were investigated. Then its skin irritation was investigated. The optimum Hippophae rhamnoides Linn oil nanoemulsion prescription was determined using Cremophor EL as an emulsifier, Transcutol P as a co-emulsifier, and isopropyl myristate(IPM) as the oil phase(IPM%: Cremophor EL%: Hippophae rhamnoides Linn oil%= 5:16:20, Km = 4:1). The prepared Hippophae rhamnoides Linn oil nanoemulsion was pale yellow and transparent. Globular droplets were observed under a transmission electron microscope(TEM). The average particle size was 52.2±4.8 nm. The loading capacity was 10.68%, and the oil-in-water(O/W) type nanoemulsion was stable after centrifugation. The CLSM results showed that the fluorescence intensity of the OB Hippophae rhamnoides Linn oil nanoemulsion group was stronger than that of the Hippophae rhamnoides Linn oil cream and Hippophae rhamnoides Linn oil groups in each layer of skin. The study also showed that skin surface treated with the Hippophae rhamnoides Linn oil nanoemulsion had strong fluorescence. The skin depth had weak fluorescence, while the areas near the hair follicle and its appendages had the strongest fluorescence. The skin irritation test showed that the prepared Hippophae rhamnoides Linn oil nanoemulsion was applied to the normal and damaged skin of the rabbit, and there was no apparent redness and swelling. These results suggested that the nanoemulsion coated with Hippophae rhamnoides Linn oil was a potential delivery system for skin disorders.展开更多
The aim of this study was to develop the water compatible form of coconut oil through nanoemulsification. The effect of different types and amounts of surfactants on the physical characteristics of nanoemulsions conta...The aim of this study was to develop the water compatible form of coconut oil through nanoemulsification. The effect of different types and amounts of surfactants on the physical characteristics of nanoemulsions containing coconut oil was investigated. Coconut oil nanoemulsions containing varied amounts of surfactants including polyethylene glycol octyl phenyl ether(PGO), polyoxyethylene sorbitan monostearate(POS), polyethylene glycol hydrogenated castor oil(PHC), sodium lauryl sulfate(SLS) and poloxamer 407(PLX) were formulated and comparatively evaluated for their physical properties. The results showed that the coconut oil nanoemulsions using PGO, POS and PHC as surfactants exhibited low percent creaming index indicating excellent stability, while those containing SLS and PLX demonstrated the higher percent creaming index suggesting lesser physical stability. The droplet sizes of nanoemulsions consisting of 5%(w/w) PGO, POS and PHC were 22.843, 4.458 and 0.162 μm, respectively. Thus, coconut oil nanoemulsions with the smallest size could be obtained when PHC was applied. Furthermore, the droplet size of nanoemulsions decreased from 33 μm to less than 200 nm with an increase in the amount of PHC from 1% to 10%(w/w). Additionally, the properties of coconut oil based nanoemulsions containing PHC were not changed through temperature cycling test. From these results, it was suggested that the fabrication of stable coconut oil nanoemulsions with small particle size could be easily achieved by using 5%(w/w) PHC as a surfactant. The knowledge gained from the study might provide the basic guideline for the fabrication of stable nanoemulsions for food, cosmetic and pharmaceutical fields in the future.展开更多
Nanoemulsions(NEs)and nanosuspensions(NSs)show great potential in enhancing the ocular bioavailability of therapeutics through topical delivery.However,transocular fate of intact NEs and NSs is still inconclusive.In t...Nanoemulsions(NEs)and nanosuspensions(NSs)show great potential in enhancing the ocular bioavailability of therapeutics through topical delivery.However,transocular fate of intact NEs and NSs is still inconclusive.In this study,an aggregation-caused quenching fluorescent probe is used to track precorneal retention and transocular transportation of intact NEs and NSs,while coumarin 6 is used to mimick the cargo.NEs show superior precorneal retention to NSs.Both the two types of nanocarriers can permeate into but not across the cornea.The smaller NEs(100 nm)permeate better into the cornea than the bigger ones(210 nm).Nanocarriers in the cornea serves as depots.The released cargo molecules can penetrate across the cornea and diffuse into the lens.Moreover,the conjunctiva-scleral route may be potential to deliver drugs to the back of the eye,In conclusion,the study provides useful tools and information in the field of transocular transportation of nanoparticles.展开更多
The number of people with Alzheimer’s disease(AD)is increasing annually,with the nidus mainly concentrated in the cortex and hippocampus.Despite of numerous efforts,effective treatment of AD is still facing great cha...The number of people with Alzheimer’s disease(AD)is increasing annually,with the nidus mainly concentrated in the cortex and hippocampus.Despite of numerous efforts,effective treatment of AD is still facing great challenges due to the blood brain barrier(BBB)and limited drug distribution in the AD nidus sites.Thus,in this study,using vinpocetine(VIN)as a model drug,the objective is to explore the feasibility of tackling the above bottleneck via intranasal drug delivery in combination with a brain guider,borneol(BOR),using nanoemulsion(NE)as the carrier.First of all,the NE were prepared and characterized.In vivo behavior of the NE after intranasal administration was investigated.Influence of BOR dose,BOR administration route on drug brain targeting behavior was evaluated,and the influence of BOR addition on drug brain subregion distribution was probed.It was demonstrated that all the NE had comparable size and similar retention behavior after intranasal delivery.Compared to intravenous injection,improved brain targeting effect was observed by intranasal route,and drug targeting index(DTI)of the VIN–NE group was 154.1%,with the nose-to-brain direct transport percentage(DTP)35.1%.Especially,remarkably enhanced brain distribution was achieved after BOR addition in the NE,with the extent depending on BOR dose.VIN brain concentration was the highest in the VIN-1-BOR-NE group at BOR dose of 1 mg/kg,with the DTI reaching 596.1%and the DTP increased to 83.1%.BOR could exert better nose to brain delivery when administrated together with the drug via intranasal route.Notably,BOR can remarkably enhance drug distribution in both hippocampus and cortex,the nidus areas of AD.In conclusion,in combination with intranasal delivery and the intrinsic brain guiding effect of BOR,drug distribution not only in the brain but also in the cortex and hippocampus can be enhanced significantly,providing the perquisite for improved therapeutic efficacy of AD.展开更多
Objective:To characterize a nanoemulsion containing a synergistic combination of curcumin(CUR)and quercetin(QUE)for brain targeting through the nose.Methods:The synergistic activity of the combination of two phytocons...Objective:To characterize a nanoemulsion containing a synergistic combination of curcumin(CUR)and quercetin(QUE)for brain targeting through the nose.Methods:The synergistic activity of the combination of two phytoconstituents,curcumin and quercetin(CUR-QUE)was determined at a 2:1 ratio.Nanoemulsions containing the synergistic combination were prepared using high-pressure homogenization technique.Nanoemulsion formulation was characterized for globule size,drug content,thermodynamic stability,zeta potential measurement,and drug release.Histological studies were performed using isolated nasal mucosa of sheep.Moreover,in vivo studies using allograft model were performed.Results:CUR-QUE in a 2:1 ratio combination showed the lowest combination index values 0.99(combination index<1)for treatment of human glioblastoma U373-MG cell.The combination inhibited the growth of human glioblastoma U373 MG cells.The significant drug targeting efficiency percentage(178.25±2.86 for CUR and 170.54±6.11 for QUE)and nose to brain drug direct transport percentage(44.05±0.93 for CUR and 38.25±0.83 for QUE)of optimized nanoemulsion(F9)indicated effective central nervous system targeting via the intranasal route.In vivo anticancer study using allograft model of nude mice demonstrated potential anticancer activity of the synergistic combination of CUR-QUE as compared to doxorubicin.Conclusions:This study demonstrates that synergistic combination of CUR-QUE was optimal for treatment of human glioblastoma.Moreover,significant site-specific delivery to the brain was achieved by administering nanoemulsion through the nose.The study also reveals that intranasal delivery of nanoemulsion containing synergistic combination of CUR and QUE could be a promising strategy for brain tumor treatment.展开更多
Nanoemulsions have attracted great attention in research, dosage form design and pharmacotherapy. This is as a result of a number of attributes peculiar to nanoemulsions such as optical clarity, ease of preparation, t...Nanoemulsions have attracted great attention in research, dosage form design and pharmacotherapy. This is as a result of a number of attributes peculiar to nanoemulsions such as optical clarity, ease of preparation, thermodynamic stability and increased surface area. Nanoemulsions also known as submicron emulsions serve as vehicles for the delivery of active pharmaceutical ingredients as well as other bioactives. They are designed to address some of the problems associated with conventional drug delivery systems such as low bioavailability and noncompliance. The importance of design and development of emulsion nanocarrier systems aimed at controlling and/or improving required bioavailability levels of therapeutic agents cannot be overemphasized. Reducing droplet sizes to the nanoscale leads to some very interesting physical properties, such as optical transparency and unusual elastic behaviour. This review sheds light on the current state of nanoemulsions in the delivery of drugs and other bioactives. The morphology, formulation, characteristics and characterization of nanoemulsions were also addressed.展开更多
As a kind of stimuli-responsive materials,the disulfide-containing material has received a tremendous amount of interest.A novel functional disulfide-containing waterborne polyurethane(DS-WPU)nanoemulsion was prepared...As a kind of stimuli-responsive materials,the disulfide-containing material has received a tremendous amount of interest.A novel functional disulfide-containing waterborne polyurethane(DS-WPU)nanoemulsion was prepared via a one-step in situ phase inverse emulsification technique and its reducing-responsive prope rty was investigated using dithiothreitol as the reductant.Results showed that the DS-WPU nanoemulsion had a uniform particle size in nanoscale and a good film-forming characteristic,and the DS-WPU latex film exhibited great responsiveness along with a self-assembled behavior in the reducing environment to form WPU emulsion again,including a long-to-short process of the polymer chains.展开更多
For investigating the accelerated blood clearance(ABC) phenomenon of polyglycerin modified nanoemulsions upon cross administration with polyethylene glycol(PEG) covered nanoemulsion, we used the 1,2-distea-royl-sn-gly...For investigating the accelerated blood clearance(ABC) phenomenon of polyglycerin modified nanoemulsions upon cross administration with polyethylene glycol(PEG) covered nanoemulsion, we used the 1,2-distea-royl-sn-glycero-3-phosphoethanolamine-npolyglycerine-610 and the 1,2-distearoyl-n-glycero-3-phosphoethanolamine-n-[methoxy(polyethylene glycol)-2000] as modify materials, the dialkylcarbocyanines as fluorescence indicator. Exhausted macrophages rat model was established and new material containing polycarboxyl structure was synthesized. The microplate reader and the in vivo optical imaging system were applied to measure the concentration of nanoemulsions in tissues.The results show that the first dose of polyglycerin modified nanoemulsion can induce the ABC phenomenon of the second dose of PEGylated nanoemulsion. With the increase in the amount of the surface polyglycerin, the extent of the ABC phenomenon decreases. Liver accumulation has positive relationship with the ABC phenomenon. Furthermore, kupffer cells in liver can get more immune information from polyhydroxy structure than polycarboxyl group in the modify compound. The results of our work imply that the polycarboxyl structure has advantages to eliminate the ABC phenomenon.展开更多
Nanoemulsion as small droplet dispersion allows them to uniformly deposit on substrates,increases the rate of bioavailability,absorption and has a better uptake.Although it is generally accepted that nanoemulsions are...Nanoemulsion as small droplet dispersion allows them to uniformly deposit on substrates,increases the rate of bioavailability,absorption and has a better uptake.Although it is generally accepted that nanoemulsions are stable for years,Oswald ripening which can damage nanoemulsion has been reported[1].In this study,converting nanoemulsion as liquid formulation into solid powders was attempted by using spray drying method.The obtained powders were then characterized,reconstituted and compared to the initial nanoemulsion.展开更多
Nanoemulsions are widely used as advanced pharmaceutical delivery systems in biomedical field, due to their high encapsulation efficiency and good therapy efficacy.Nanoemulsification techniques that produce nanoemulsi...Nanoemulsions are widely used as advanced pharmaceutical delivery systems in biomedical field, due to their high encapsulation efficiency and good therapy efficacy.Nanoemulsification techniques that produce nanoemulsions with controllable sizes and compositions are promising for creating advanced nanoemulsion systems for pharmaceutical delivery.This review summarizes recent advances on low-energy emulsification techniques for producing nanoemulsions, and the use of these nanoemulsions as advanced pharmaceutical delivery systems and as templates to create drug-loaded functional particles for biomedical application.First, nanoemulsification techniques that utilize elaborate interfacial physics/chemistry and micro-/nano-fluidics, featured with relatively-low energy input, to produce nanoemulsions with controllable sizes and compositions, are introduced.Uses of these nanoemulsions to create nanoemulsionincorporated milli-particles, drug-loaded nanoparticles and nanoparticle-incorporated microparticles with sizes ranging from several millimeters to sub-10 nm are emphasized.Flexible and efficient use of the nanoemulsions, functional nanoparticles and milli-/micro-particles integrated with nanoemulsions or nanoparticles for advanced pharmaceutical delivery in biomedical field are highlighted, with focus on how the interplay between their sizes and compositions achieve desired pharmaceutical-delivery performances.Finally, perspectives on further advances on the controllable production of nanoemulsions are provided.展开更多
Spearmint oil(SMO), a commonly used essential oil for oral care products, possesses various interesting functions, especially for anticancer property. However, the application of SMO for cancer treatment is limited du...Spearmint oil(SMO), a commonly used essential oil for oral care products, possesses various interesting functions, especially for anticancer property. However, the application of SMO for cancer treatment is limited due to water insoluble. In the present study, nanoemulsions, which have been widely accepted as dosage forms for poorly water-soluble drugs, were selected as candidate carriers for SMO to inhibit oral cancer cell. The nanoemulsions were fabricated using phase inversion temperature method. The factors affecting formation and properties of nanoemulsions including type and amount of surfactants, oil loading and ratio of SMO to virgin coconut oil(VCO) were investigated. Among the surfactants used, the nanoemulsions containing polyoxyethylene castor oil derivatives(Kolliphor ?EL; PCO35, Cremophor ?RH40; PCO40, Eumulgin ?CO60; PCO60) and polyoxyethylene sorbitan fatty acid esters(PSF80) showed 100% creaming after temperature cycling test indicating excellent physical stability while those containing PCO40 demonstrated more transparency and better physical stability. With an increasing amount of PCO40, the droplet size tended to decrease and was in the nano-size range( < 1000 nm) after increasing to more than 5%(w/w). SMOVCO loading also influenced on the droplet size. At 5%(w/w) PCO40, the maximum SMO-VCO loading of 25%(w/w) to attain nanoemulsions was observed. Moreover, the composition of oils had an impact on size of emulsions. The transparent nanoemulsions were only prepared in the range of SMO-VCO from 40:60 to 80:20, suggesting the optimum ratio of SMO tosurfactant and the composition of oils were the critical factors for formation of nanoemulsions. NMR study disclosed that the interaction between PCO40 with both VCO and SMO should be a possible stabilization mechanism. Furthermore, the SMO-VCO nanoemulsions exhibited significant cytotoxic effect against oral carcinoma(KON) cell line using MTT assay. The finding, therefore, revealed the good feasibility of SMO-VCO nanoemulsions as novel carriers for treating of oral cancer.展开更多
In the present study,we aimed to formulate,optimize and characterize nanoemulsion-based gel of imiquimod for its topical administration and to improve the drug permeation.Nanoemulsions were prepared by the aqueous pha...In the present study,we aimed to formulate,optimize and characterize nanoemulsion-based gel of imiquimod for its topical administration and to improve the drug permeation.Nanoemulsions were prepared by the aqueous phase titration method and spontaneously formed by mixing specific fractions of oil phase:Smix:water.The nanoemulsion formulations were optimized by response surface methodology(RSM) using mixture design,Scheffe model.The formulated nanoemulsion was incorporated into 0.5% Carbopol 934(w/v) to enhance convenience in superficial application of the drug.The nanoemulsions were characterized in terms of droplet size,zeta potential,TEM,DSC and in vitro drug permeation.The vesicle size was 113.6 nm with polydispersity index of 0.251.The zeta potential was 34 m V.The spherical droplet shape was confirmed by TEM analysis.The drug permeation from the diffusion membrane was 73.67% in 6 h for the optimized formulation.An optimized nanoemulsion gel formulation of imiquimod was successfully developed with improved permeation using experimental design technique.The developed formulation could be further explored as a potential alternate to currently available topical formulations for the treatment of genital warts.展开更多
文摘In this study,thyme essential oil(TEO)nanoemulsion(tPTNs)was constructed with transglutaminase(TGase)-modified potato protein,and its antibacterial activity and mechanism of action were evaluated and explored.Results indicated that tPTNs exhibited great antibacterial activity against both Staphylococcus aureus and Escherichia coli,with minimal inhibitory concentration(MIC)and minimum bactericidal concentration(MBC)of 2.5 and 5.0 mg/mL,respectively.Also,the antibacterial effects of tPTNs were concentration-dependent.We observed a significant decrease in the absolute value of the zeta potential,and significant increases in particle size,cell membrane hydrophobicity,conductivity,the release of metal ions,and the leakage of nucleic acid as the concentration of tPTNs increased from 0 mg/mL to MBC.Furthermore,sodium dodecyl sulphate-polyacrylamide gel electrophoresis(SDS-PAGE)demonstrated that protein synthesis was inhibited or even disrupted.Analysis by liquid chromatography-mass spectrometry(LC-MS)indicated that treatment with tPTNs caused significant changes in bacterial metabolites,1117 and 692 differential metabolites being found for S.aureus and E.coli,respectively.The differential metabolites were involved in nucleotide metabolism,amino acid metabolism,tricarboxylic acid cycle and other metabolic pathways.These findings provide valuable insights for the application of thyme essential oil as an efficient antibacterial agent and for the understanding of its mechanism of action.
文摘Nanoemulsions have garnered significant attention in the cosmetic industry due to their ability to enhance ingredient dispersion,improve topical absorption,and enable targeted delivery of active compounds within the skin layers.These nano-sized emulsions allow skincare products,like moisturizers,anti-aging creams,and sunscreens,to penetrate the skin more deeply and be absorbed better.They can also release their active ingredients gradually,which enhances the product's effectiveness.Additionally,nanoemulsions are more stable,meaning they protect ingredients from breaking down or losing their effectiveness,which helps extend the shelf life of the products.However,despite their advantages,nanoemulsions come with challenges,such as difficulties in producing them on a large scale,meeting safety regulations,and ensuring they remain stable over time.Future research will likely focus on improving how these formulations are made,making sure they are safe to use,and exploring more environmentally friendly and personalized solutions for skincare.As this technology develops,nanoemulsions have the potential to transform cosmetic formulations by offering more innovative and effective skincare options.
基金financially supported by the National Natural Science Foundation of China(Grant No.32101981)the cooperation project between Ya’an city and Sichuan Agricultural University(23ZDF0003)。
文摘Encapsulation and protection of hesperidin(HES)in mung bean protein isolate(MPI)-dextran(DX)conjugatestabilized nanoemulsions(MDC NEs)were investigated in this study.The degree of grafting of MDC prepared by a dry-heating method reached 39.70%±0.01% under the optimal conditions of MPI/DX mass ratio 1:2.3,reaction temperature 58.8℃,and reaction time 4 d.Moreover,the analyses of Fourier infrared spectroscopy,intrinsic fluorescence spectroscopy,surface hydrophobicity,and thermal stability further confirmed the covalent grafting of dextran onto MPI molecules.When encapsulated in MDC NEs at 80 MPa for three times by highpressure homogenization,the encapsulation efficiency and loading capacity of HES were 63.62%±0.01%and 0.40±0.00 g/g,respectively.The encapsulated HES exhibited higher antioxidant activity and stronger light and storage stability than the free HES.Additionally,the incorporation of HES inhibited the formation of lipid peroxides in the nanoemulsions.The findings suggest that glycosylation combined with high-pressure homogenization is an effective strategy for enhancing the stability of MPI-based emulsions and improving their encapsulation of HES.This study provides a promising approach for the development of innovative food and beverage products based on MPI emulsions or new materials for encapsulating fat-soluble bioactive compounds.
基金Ho Chi Minh City University of Technology(HCMUT),VNU-HCM,for supporting this study.
文摘This study focuses on the preparation,and optimization of the nanoemulsions coorporating with pumpkin seed oil,grape seed oil,and grapefruit essential oil using the phase inversion temperature(PIT)technique.The research investigated the impact of surfactant types and concentrations on critical nanoemulsion properties,including droplet size,polydispersity index(PDI),and zeta potential.Using a Box-Behnken Design(BBD)model,the formulation was optimized containing 6.0%plant oils,10.0%Tween 80,2.0%Span 80,and 1.0%lecithin to achieve nano-sized droplets(33.52 nm),with a low PDI(0.205),and a stable zeta potential(15.49 mV).The antioxidant activity,was evaluated through 2,2-diphenyl-1-picrylhydrazyl(DPPH)radical scavenging assays,demonstrating its outstanding efficacy.And the optimized nanoemulsion showed a radical-scavenging capacity exceeding 2250μg ascorbic acid equivalents/g,significantly outperforming non-nanoemulsified oils.Stability testing under various environmental conditions highlighted exceptional robustness,with refrigerated samples maintaining structural integrity,minimal particle size growth,and consistent physicochemical properties over a 30-day storage period.The results suggest that the plant oil-based nanoemulsions exhibit strong antioxidant potential,offering a promising natural treatment for their application in cosmeceutical and therapeutic formulations.
基金supported by grants from the National Natural Science Foundation of China(32072267)China Agriculture Research System(CARS-14)+1 种基金National Key Research and Development Program of China(2023YFD2100404)the Innovation Group Project of Hubei Province(2023AFA042).
文摘Dietary supplementation with plant-derivedα-linolenic acid(ALA)has the potential to alleviate the insufficient intake of global n-3 long-chain polyunsaturated fatty acids(n-3 LCPUFAs),but faces the bottleneck of highβ-oxidation consumption,oxidative susceptibility,and low conversion efficiency.The current study investigated how flax lignans with different degrees of polymerization and glycosylation affect the conversion of ALA to n-3 LCPUFAs in mice over 35 days of administering sunflower phospholipid-stabilized flaxseed oil nanoemulsions.Results showed that flax lignan macromolecules(FLM)increased hepatic protein expression of elongase of very long chain fatty acid 5(Elovl5,24.2%)and fatty acid desaturase 2(Fads2,44.7%),thereby positively regulating ALA conversion pathways and raising serum eicosapentaenoic acid(EPA)levels(52.7%)via liver lipid re-efflux.Secoisolariciresinol diglucoside(SDG)enhanced ALA desaturation by upregulating hepatic protein expression of Fads1(30.4%)and Fads2(45.6%),increasing serum EPA levels(55.9%)and hepatic docosahexaenoic acid(DHA)levels(10%).Secoisolariciresinol(SECO)elevated hepatic protein expression of Elovl2(30.7%),Elovl5(11.7%),Fads1(37.9%),and Fads2(24.1%),but also increased carnitine palmitoyltransferase 1a(45.2%),leading to decreased ALA,EPA,and DHA levels in serum and liver.Therefore,in comparison,FLM and SDG emerge as the dominant structural units that positively regulate the conversion of ALA.These findings lay a groundwork for designing precise dietary delivery systems to enhance the conversion to n-3 LCPUFAs.
基金Supported by Scientific Research Projects Units of Science and Technology Department of Xinjiang Uygur Autonomous Region for Financial Support(Project No.2013911072)~~
文摘[Objective] The aim was to obtain the preparation technology of the pomegranate peel polyphenol nanoemulsion. [Method] The pomegranate peel polyphe- nol nanoemulsion was prepared by the titration methods and the pseudo ternary dia- gram. The effect of various elements on the formation of the nanoemulsion was stud- ied. [Results] The optimal prescription of the pomegranate peel polyphenol nanoemul- sion was 4.4%（w/w） of pomegranate peel polyphenol, 34.1%（w/w） of EL-40, 17.1%（w/w） of anhydrous ethanol, 5.7%（w/w） of IPM and 38.7%（w/w） of distilled water. [Conclusion] It is feasible to produce the pomegranate peel polyphenol nanoemulsion by the titration methods and the pseudo ternary diagram. It consists of pomegranate peel polyphe- nol, EL-40, anhydrous ethanol, IPM and distilled water. There is 4.4%（w/w） of the pomegranate peel polyphenol in the nanoemuJsion.
基金Supported by Key Project of Science and Technology Plant of Haikou City(2009-043)Research Project of Hainan University (hd09xm78)~~
文摘[ Objective] The paper was to prepare bifenthrin nanoemulsions, and to characterize its property. [ Method ] Oil in water type of bifenthrin nanoemul- sions was prepared using emulsion phase transition method at constant temperature of 25℃. The formation mechanism of nanoemulsions was investigated, and the property of bffenthrin nanoemulsions was characterized by dynamic light scattering（DIS）, transmission electron microscopy （TEM）, contact angle meter, interfa- cial tension meter and high performance liquid chromatogTaphy （HPLC）. [ Result ] Phase transition occurred during the formation progress of bifenthrin nanoemul- sions ; the particles of nancomulsions system was spherical, and the particle size was mainly distributed in the range of 25 -30 ran; the contact angle on paraffin was less than 90° with good wetting effect; the surface tension was less than 40 mN/m, and the emulsification effect was also good, so the utilization rate of bifenthrin nancomulsions was improved. HPLC results showed that bffenthrin was not easy to decompose or precipitate with good stability. [ Conclusion] The result provided basis for the preparation of new types of insecticides.
基金supported by Tianjin City High School Science Technology Fund Planning Project(No.2017KJ134)。
文摘Salidroside(SAL)is a phenolic substance with high solubility and low permeability,which make it easy to cause the efflux effect of P-glycoprotein and degradation of intestinal flora,resulting in lower bioavailability.The aim of this study was to develop and optimize a water-in-oil nanoemulsion of SAL(w/o SAL-N)to explore its suitability in oral drug delivery systems.In this work,SAL-N was successfully prepared by water titration method at K_(m)=1 to construct the pseudo-ternary phase diagrams.Physical characterization including the average viscosity,pH,refractive index,particle size,PDI,TEM,DSC,the content of SAL,and stability study were performed.It was evaluated for drug release in vitro and pharmacokinetic studies in vivo.The optimized nanoemulsion formulation consisted of Labrafil M 1944 CS(63%),Span-80/Tween-80/EtOH(27%)and 200 mg·mL^(-1) SAL solution(SAL-SOL)(10%).Low viscosity and suitable pH were expected for the nanoemulsion.The spherical morphology and nanoscale size of SAL-N enhanced the stability of the nanoemulsion system.In vitro drug release showed that SAL-N had a better controlled release property than SAL-SOL at earlier time points.The pharmacokinetic studies exhibited that SAL-N had significantly higher in t_(1/2)(2.11-fold),AUC_(0-48 h)(1.75-fold)and MRT0-48 h(2.63-fold)than SAL-SOL(P<0.01).The w/o SAL-N prepared in this work can be effectively delivered via the oral route.It can be seen w/o nanoemulsion is a strategy for the drug with polyphenols to delay the release,enhance oral absorption and reduce metabolic rate.
基金National Natural Science Foundation of China(Grant No.81460539)the excellent postgraduate project in Xinjiang Medical University(Grant No.CXCY096)
文摘A Hippophae rhamnoides Linn oil nanoemulsion was developed, and its physicochemical properties and in vitro transdermal characteristics were investigated. Then its skin irritation was investigated. The optimum Hippophae rhamnoides Linn oil nanoemulsion prescription was determined using Cremophor EL as an emulsifier, Transcutol P as a co-emulsifier, and isopropyl myristate(IPM) as the oil phase(IPM%: Cremophor EL%: Hippophae rhamnoides Linn oil%= 5:16:20, Km = 4:1). The prepared Hippophae rhamnoides Linn oil nanoemulsion was pale yellow and transparent. Globular droplets were observed under a transmission electron microscope(TEM). The average particle size was 52.2±4.8 nm. The loading capacity was 10.68%, and the oil-in-water(O/W) type nanoemulsion was stable after centrifugation. The CLSM results showed that the fluorescence intensity of the OB Hippophae rhamnoides Linn oil nanoemulsion group was stronger than that of the Hippophae rhamnoides Linn oil cream and Hippophae rhamnoides Linn oil groups in each layer of skin. The study also showed that skin surface treated with the Hippophae rhamnoides Linn oil nanoemulsion had strong fluorescence. The skin depth had weak fluorescence, while the areas near the hair follicle and its appendages had the strongest fluorescence. The skin irritation test showed that the prepared Hippophae rhamnoides Linn oil nanoemulsion was applied to the normal and damaged skin of the rabbit, and there was no apparent redness and swelling. These results suggested that the nanoemulsion coated with Hippophae rhamnoides Linn oil was a potential delivery system for skin disorders.
基金the Thailand Research Fund,Com-mission on Higher Education(Thailand)Silpakorn University Research and Development Institute+1 种基金Faculty of Pharmacy,Sil-pakorn UniversityFaculty of Pharmacy,Siam University-for research funding
文摘The aim of this study was to develop the water compatible form of coconut oil through nanoemulsification. The effect of different types and amounts of surfactants on the physical characteristics of nanoemulsions containing coconut oil was investigated. Coconut oil nanoemulsions containing varied amounts of surfactants including polyethylene glycol octyl phenyl ether(PGO), polyoxyethylene sorbitan monostearate(POS), polyethylene glycol hydrogenated castor oil(PHC), sodium lauryl sulfate(SLS) and poloxamer 407(PLX) were formulated and comparatively evaluated for their physical properties. The results showed that the coconut oil nanoemulsions using PGO, POS and PHC as surfactants exhibited low percent creaming index indicating excellent stability, while those containing SLS and PLX demonstrated the higher percent creaming index suggesting lesser physical stability. The droplet sizes of nanoemulsions consisting of 5%(w/w) PGO, POS and PHC were 22.843, 4.458 and 0.162 μm, respectively. Thus, coconut oil nanoemulsions with the smallest size could be obtained when PHC was applied. Furthermore, the droplet size of nanoemulsions decreased from 33 μm to less than 200 nm with an increase in the amount of PHC from 1% to 10%(w/w). Additionally, the properties of coconut oil based nanoemulsions containing PHC were not changed through temperature cycling test. From these results, it was suggested that the fabrication of stable coconut oil nanoemulsions with small particle size could be easily achieved by using 5%(w/w) PHC as a surfactant. The knowledge gained from the study might provide the basic guideline for the fabrication of stable nanoemulsions for food, cosmetic and pharmaceutical fields in the future.
基金supported by the National Natural Science Foundation of China(Nos.81872815,81573363,81690263,21372063)the Natural Science Foundation of Shanghai(No.16ZR1403500)
文摘Nanoemulsions(NEs)and nanosuspensions(NSs)show great potential in enhancing the ocular bioavailability of therapeutics through topical delivery.However,transocular fate of intact NEs and NSs is still inconclusive.In this study,an aggregation-caused quenching fluorescent probe is used to track precorneal retention and transocular transportation of intact NEs and NSs,while coumarin 6 is used to mimick the cargo.NEs show superior precorneal retention to NSs.Both the two types of nanocarriers can permeate into but not across the cornea.The smaller NEs(100 nm)permeate better into the cornea than the bigger ones(210 nm).Nanocarriers in the cornea serves as depots.The released cargo molecules can penetrate across the cornea and diffuse into the lens.Moreover,the conjunctiva-scleral route may be potential to deliver drugs to the back of the eye,In conclusion,the study provides useful tools and information in the field of transocular transportation of nanoparticles.
基金supported by the Distinguished Professor Project of Liaoning Province.
文摘The number of people with Alzheimer’s disease(AD)is increasing annually,with the nidus mainly concentrated in the cortex and hippocampus.Despite of numerous efforts,effective treatment of AD is still facing great challenges due to the blood brain barrier(BBB)and limited drug distribution in the AD nidus sites.Thus,in this study,using vinpocetine(VIN)as a model drug,the objective is to explore the feasibility of tackling the above bottleneck via intranasal drug delivery in combination with a brain guider,borneol(BOR),using nanoemulsion(NE)as the carrier.First of all,the NE were prepared and characterized.In vivo behavior of the NE after intranasal administration was investigated.Influence of BOR dose,BOR administration route on drug brain targeting behavior was evaluated,and the influence of BOR addition on drug brain subregion distribution was probed.It was demonstrated that all the NE had comparable size and similar retention behavior after intranasal delivery.Compared to intravenous injection,improved brain targeting effect was observed by intranasal route,and drug targeting index(DTI)of the VIN–NE group was 154.1%,with the nose-to-brain direct transport percentage(DTP)35.1%.Especially,remarkably enhanced brain distribution was achieved after BOR addition in the NE,with the extent depending on BOR dose.VIN brain concentration was the highest in the VIN-1-BOR-NE group at BOR dose of 1 mg/kg,with the DTI reaching 596.1%and the DTP increased to 83.1%.BOR could exert better nose to brain delivery when administrated together with the drug via intranasal route.Notably,BOR can remarkably enhance drug distribution in both hippocampus and cortex,the nidus areas of AD.In conclusion,in combination with intranasal delivery and the intrinsic brain guiding effect of BOR,drug distribution not only in the brain but also in the cortex and hippocampus can be enhanced significantly,providing the perquisite for improved therapeutic efficacy of AD.
文摘Objective:To characterize a nanoemulsion containing a synergistic combination of curcumin(CUR)and quercetin(QUE)for brain targeting through the nose.Methods:The synergistic activity of the combination of two phytoconstituents,curcumin and quercetin(CUR-QUE)was determined at a 2:1 ratio.Nanoemulsions containing the synergistic combination were prepared using high-pressure homogenization technique.Nanoemulsion formulation was characterized for globule size,drug content,thermodynamic stability,zeta potential measurement,and drug release.Histological studies were performed using isolated nasal mucosa of sheep.Moreover,in vivo studies using allograft model were performed.Results:CUR-QUE in a 2:1 ratio combination showed the lowest combination index values 0.99(combination index<1)for treatment of human glioblastoma U373-MG cell.The combination inhibited the growth of human glioblastoma U373 MG cells.The significant drug targeting efficiency percentage(178.25±2.86 for CUR and 170.54±6.11 for QUE)and nose to brain drug direct transport percentage(44.05±0.93 for CUR and 38.25±0.83 for QUE)of optimized nanoemulsion(F9)indicated effective central nervous system targeting via the intranasal route.In vivo anticancer study using allograft model of nude mice demonstrated potential anticancer activity of the synergistic combination of CUR-QUE as compared to doxorubicin.Conclusions:This study demonstrates that synergistic combination of CUR-QUE was optimal for treatment of human glioblastoma.Moreover,significant site-specific delivery to the brain was achieved by administering nanoemulsion through the nose.The study also reveals that intranasal delivery of nanoemulsion containing synergistic combination of CUR and QUE could be a promising strategy for brain tumor treatment.
文摘Nanoemulsions have attracted great attention in research, dosage form design and pharmacotherapy. This is as a result of a number of attributes peculiar to nanoemulsions such as optical clarity, ease of preparation, thermodynamic stability and increased surface area. Nanoemulsions also known as submicron emulsions serve as vehicles for the delivery of active pharmaceutical ingredients as well as other bioactives. They are designed to address some of the problems associated with conventional drug delivery systems such as low bioavailability and noncompliance. The importance of design and development of emulsion nanocarrier systems aimed at controlling and/or improving required bioavailability levels of therapeutic agents cannot be overemphasized. Reducing droplet sizes to the nanoscale leads to some very interesting physical properties, such as optical transparency and unusual elastic behaviour. This review sheds light on the current state of nanoemulsions in the delivery of drugs and other bioactives. The morphology, formulation, characteristics and characterization of nanoemulsions were also addressed.
基金the National Key Research and Development Program of China (No.2017YFD0200704)the National Basic Research Program of China (973 Program,No. 2014CB932202) for the financial supports
文摘As a kind of stimuli-responsive materials,the disulfide-containing material has received a tremendous amount of interest.A novel functional disulfide-containing waterborne polyurethane(DS-WPU)nanoemulsion was prepared via a one-step in situ phase inverse emulsification technique and its reducing-responsive prope rty was investigated using dithiothreitol as the reductant.Results showed that the DS-WPU nanoemulsion had a uniform particle size in nanoscale and a good film-forming characteristic,and the DS-WPU latex film exhibited great responsiveness along with a self-assembled behavior in the reducing environment to form WPU emulsion again,including a long-to-short process of the polymer chains.
基金supported by the National Natural Science Foundation of China (Grant Nos.81072602,81373334)
文摘For investigating the accelerated blood clearance(ABC) phenomenon of polyglycerin modified nanoemulsions upon cross administration with polyethylene glycol(PEG) covered nanoemulsion, we used the 1,2-distea-royl-sn-glycero-3-phosphoethanolamine-npolyglycerine-610 and the 1,2-distearoyl-n-glycero-3-phosphoethanolamine-n-[methoxy(polyethylene glycol)-2000] as modify materials, the dialkylcarbocyanines as fluorescence indicator. Exhausted macrophages rat model was established and new material containing polycarboxyl structure was synthesized. The microplate reader and the in vivo optical imaging system were applied to measure the concentration of nanoemulsions in tissues.The results show that the first dose of polyglycerin modified nanoemulsion can induce the ABC phenomenon of the second dose of PEGylated nanoemulsion. With the increase in the amount of the surface polyglycerin, the extent of the ABC phenomenon decreases. Liver accumulation has positive relationship with the ABC phenomenon. Furthermore, kupffer cells in liver can get more immune information from polyhydroxy structure than polycarboxyl group in the modify compound. The results of our work imply that the polycarboxyl structure has advantages to eliminate the ABC phenomenon.
文摘Nanoemulsion as small droplet dispersion allows them to uniformly deposit on substrates,increases the rate of bioavailability,absorption and has a better uptake.Although it is generally accepted that nanoemulsions are stable for years,Oswald ripening which can damage nanoemulsion has been reported[1].In this study,converting nanoemulsion as liquid formulation into solid powders was attempted by using spray drying method.The obtained powders were then characterized,reconstituted and compared to the initial nanoemulsion.
基金gratefully acknowledge support from the National Natural Science Foundation of China(Nos.22108186,21922809,21991101)Sichuan University(No.2020SCUNG112).
文摘Nanoemulsions are widely used as advanced pharmaceutical delivery systems in biomedical field, due to their high encapsulation efficiency and good therapy efficacy.Nanoemulsification techniques that produce nanoemulsions with controllable sizes and compositions are promising for creating advanced nanoemulsion systems for pharmaceutical delivery.This review summarizes recent advances on low-energy emulsification techniques for producing nanoemulsions, and the use of these nanoemulsions as advanced pharmaceutical delivery systems and as templates to create drug-loaded functional particles for biomedical application.First, nanoemulsification techniques that utilize elaborate interfacial physics/chemistry and micro-/nano-fluidics, featured with relatively-low energy input, to produce nanoemulsions with controllable sizes and compositions, are introduced.Uses of these nanoemulsions to create nanoemulsionincorporated milli-particles, drug-loaded nanoparticles and nanoparticle-incorporated microparticles with sizes ranging from several millimeters to sub-10 nm are emphasized.Flexible and efficient use of the nanoemulsions, functional nanoparticles and milli-/micro-particles integrated with nanoemulsions or nanoparticles for advanced pharmaceutical delivery in biomedical field are highlighted, with focus on how the interplay between their sizes and compositions achieve desired pharmaceutical-delivery performances.Finally, perspectives on further advances on the controllable production of nanoemulsions are provided.
基金the financial support received from Silpakorn University Research and Development Institutesupported by Faculty of Pharmacy,Sil-pakorn University
文摘Spearmint oil(SMO), a commonly used essential oil for oral care products, possesses various interesting functions, especially for anticancer property. However, the application of SMO for cancer treatment is limited due to water insoluble. In the present study, nanoemulsions, which have been widely accepted as dosage forms for poorly water-soluble drugs, were selected as candidate carriers for SMO to inhibit oral cancer cell. The nanoemulsions were fabricated using phase inversion temperature method. The factors affecting formation and properties of nanoemulsions including type and amount of surfactants, oil loading and ratio of SMO to virgin coconut oil(VCO) were investigated. Among the surfactants used, the nanoemulsions containing polyoxyethylene castor oil derivatives(Kolliphor ?EL; PCO35, Cremophor ?RH40; PCO40, Eumulgin ?CO60; PCO60) and polyoxyethylene sorbitan fatty acid esters(PSF80) showed 100% creaming after temperature cycling test indicating excellent physical stability while those containing PCO40 demonstrated more transparency and better physical stability. With an increasing amount of PCO40, the droplet size tended to decrease and was in the nano-size range( < 1000 nm) after increasing to more than 5%(w/w). SMOVCO loading also influenced on the droplet size. At 5%(w/w) PCO40, the maximum SMO-VCO loading of 25%(w/w) to attain nanoemulsions was observed. Moreover, the composition of oils had an impact on size of emulsions. The transparent nanoemulsions were only prepared in the range of SMO-VCO from 40:60 to 80:20, suggesting the optimum ratio of SMO tosurfactant and the composition of oils were the critical factors for formation of nanoemulsions. NMR study disclosed that the interaction between PCO40 with both VCO and SMO should be a possible stabilization mechanism. Furthermore, the SMO-VCO nanoemulsions exhibited significant cytotoxic effect against oral carcinoma(KON) cell line using MTT assay. The finding, therefore, revealed the good feasibility of SMO-VCO nanoemulsions as novel carriers for treating of oral cancer.
文摘In the present study,we aimed to formulate,optimize and characterize nanoemulsion-based gel of imiquimod for its topical administration and to improve the drug permeation.Nanoemulsions were prepared by the aqueous phase titration method and spontaneously formed by mixing specific fractions of oil phase:Smix:water.The nanoemulsion formulations were optimized by response surface methodology(RSM) using mixture design,Scheffe model.The formulated nanoemulsion was incorporated into 0.5% Carbopol 934(w/v) to enhance convenience in superficial application of the drug.The nanoemulsions were characterized in terms of droplet size,zeta potential,TEM,DSC and in vitro drug permeation.The vesicle size was 113.6 nm with polydispersity index of 0.251.The zeta potential was 34 m V.The spherical droplet shape was confirmed by TEM analysis.The drug permeation from the diffusion membrane was 73.67% in 6 h for the optimized formulation.An optimized nanoemulsion gel formulation of imiquimod was successfully developed with improved permeation using experimental design technique.The developed formulation could be further explored as a potential alternate to currently available topical formulations for the treatment of genital warts.
