Objective:To explore the effects of a nano-formulation of curcumin(phytosomal curcumin)on the clinical and pathological symptoms of collagen-induced arthritis(CIA)in rats.Methods:Forty male Wistar rats were immunized ...Objective:To explore the effects of a nano-formulation of curcumin(phytosomal curcumin)on the clinical and pathological symptoms of collagen-induced arthritis(CIA)in rats.Methods:Forty male Wistar rats were immunized with an emulsion containing bovine typeⅡcollagen and incomplete Freund's adjuvant and then administered phytosomal curcumin post-immunization.Clinical symptoms and histological analysis of the synovial tissues were performed.The effect of phytosomal curcumin on Th17 and Treg parameters was also evaluated.Results:Phytosomal curcumin reduced the clinical severity and paw swelling in CIA-induced rats,which was accompanied by a reduction in the number of inflammatory cell infiltration in the synovial tissue.Additionally,treatment with phytosomal curcumin significantly inhibited CIA-associated mediators as well as increased the anti-inflammatory mediators in comparison to the control groups.Conclusions:Phytosomal curcumin could improve CIA autoimmune responses and can be considered a potential candidate for the treatment of rheumatoid arthritis.展开更多
Many active constituents from herbal plants have well-established pharmacological effects in vitro. But they demonstrate less or no activities in vivo due to various problems of themselves, which severely restricts th...Many active constituents from herbal plants have well-established pharmacological effects in vitro. But they demonstrate less or no activities in vivo due to various problems of themselves, which severely restricts their clinical applications. After forming phytosomes with phospholipids in aprotic solvent, the active constituents exhibit different physicochemical properties from the free form. In particular, the bioavailability of the active constituent-phytosomes is enhanced greatly due to the improved capacity to cross the biomembrane and reach circulation. Therefore, increasing attention has been attracted to the use of phytosomes in recent years. Based on the published reports, we reviewed the recent progress in the research of phytosomes including preparation, characterization, structure verification and clinical applications.展开更多
Phytosomes(phytophospholipid complex) are dosage forms that have recently been introduced to increase the stability and therapeutic effect of herbal medicine. Currently, bioactive herbs and the phytochemicals they con...Phytosomes(phytophospholipid complex) are dosage forms that have recently been introduced to increase the stability and therapeutic effect of herbal medicine. Currently, bioactive herbs and the phytochemicals they contain are considered to be the best remedies for chronic diseases. One promising approach to increase the efficacy of plant-based therapies is to improve the stability and bioavailability of their bio-active ingredients. Phytosomes employ phospholipids as their active ingredients, and use their amphiphilic properties to solubilize and protect herbal extracts. The unique properties of phospholipids in drug delivery and their use in herbal medicines to improve bioavailability results in significantly enhanced health benefits. The introduction of phytosome nanotechnology can alter and revolutionize the current state of drug delivery. The goal of this review is to explain the application of phytosomes, their future prospects in drug delivery, and their advantages over conventional formulations.展开更多
Across the annals of time,organic molecules sourced from nature have found innumerable uses within the realms of healthcare,pharmaceuticals,and the study of living organisms.This abundant source of natural compounds h...Across the annals of time,organic molecules sourced from nature have found innumerable uses within the realms of healthcare,pharmaceuticals,and the study of living organisms.This abundant source of natural compounds has exhibited immense promise in the cure of diverse ailments,mainly neurodegenerative diseases owing to their minimum toxic and adverse effects.However,different challenges exist with phytocompounds from plants such as poor permeation,poor solubility(water/lipid),unsteadiness under extremely acidic pH conditions,and lack of targeting specificity.Furthermore,as a result of the existence of blood-brain barrier membrane and inconvenient pharmacokinetics characteristics of phytocompounds,their passage into the brain is constrained.In order to address this issue and augment the transportation of medications into the brain at a therapeutically effective level,it is imperative to formulate an innovative and pragmatic strategy.Many papers have shown that nanoformulations containing phytocompounds(resveratrol,quercetin,ferulic acid,curcumin,berberine,etc.)effectively improved many neurodegenerative diseases such as Parkinson’s,Alzheimer’s and Huntington’s diseases.This study provides an overview of phytocompounds that are used in nanosized lipid drug delivery systems.These systems are categorized according to lipid types and preparation techniques used in the formulation.Some studies regarding these systems and phytocompounds are also summarized.展开更多
With the aging of the population,the incidence of Alzheimer’s disease(AD)has increased dramatically,causing severe medical,care,and economic burdens on society and families.The efficacy of rivastigmine hydrogen tartr...With the aging of the population,the incidence of Alzheimer’s disease(AD)has increased dramatically,causing severe medical,care,and economic burdens on society and families.The efficacy of rivastigmine hydrogen tartrate(RHT),the first-line clinical treatment,is severely limited by the complex and multiple pathogenesis of AD and low brain bioavailability caused by the blood-brain barrier(BBB).Confronting such two bottlenecks,the development of multi-target agents encapsulated BBB-bypassing drug delivery systems offer tremendous thera-peutics possibilities for AD.In this study,a tailored phytosomes based nose-to-brain drug delivery system with appropriate plume was successfully designed and developed.On the one hand,Ginseng RG3-based phytosomes loaded with RHT was designed for the co-delivery of GRg3 and RHT,achieving the multi-target pharmacology for AD treatment.On the other hand,a tailored nose-to-brain drug delivery system was established for the satisfactory nose-to-brain delivery efficiency,avoiding the obstacle of BBB through bypassing it.In the phar-macodynamic study based on AD rat model,GRg3@RHT exhibited obviously synergic effect,effectively break the vicious cycle of AD progression,ultimately markedly ameliorating learning and memory ability as well as behavioral dysfunctions,and delaying the neurodegenerative process associated with AD.In addition,the strong correlation of viscosity-droplet size-plume geometry-olfactory deposition was also established,and further proved by the in vivo pharmacokinetic study,which is proposed to provide evidence to enhance nose-to-brain delivery efficiency.This study is anticipated to provide novel insights into AD treatment strategies while of-fering innovative ideas for drug delivery approaches targeting nervous system disorders.展开更多
In recent years,there has been extensive research on valorization of food wastes and a growing interest in nano-liposomal systems for food applications.This paper discusses the case of phosphatidylcholine basednanophy...In recent years,there has been extensive research on valorization of food wastes and a growing interest in nano-liposomal systems for food applications.This paper discusses the case of phosphatidylcholine basednanophytosomes loaded with anthocyanins extracted from red onion(RNPs)to overcome the bio-stability during digestion.The characterization of lyophilized RNPs in terms of entrapment efficiency,particle size,poly-dispersity index(PDI),ζ-potential,morphological properties,in vitro bioaccessibility and release kinetics were investigated.Entrapment efficiency was determined as 78.63%with lowest particle size(177.73 nm)and PDI value(0.45)and non-dense spherical microstructure for RNP6(red onion peel anthocyanin extract:soybean phosphatidylcholine at 1:6 ratio).Apart from the particle size,entrapment efficiency was determined higher than 75%,which indicates good entrapment.Additionally,from the cumulative release of RNPs concluded as a successful nano-structure with a two-fold increase in intestinal medium.However,poor Carr index and Hausner ratio suggest some limitations of the current nanoliposomes process which could be further improved.Red onion peel wastes,which are typically discarded,can serve as excellent sources of anthocyanins,and its preparation to nanophytosomes could be used as functional food ingredient or food supplements.展开更多
Nano-phytosomes(NP),lipid-based nano-carriers,were used to encapsulate the phycocyanin.Phycocyanin(Phy)is known for its important biological properties with low bioavailability and low stability.The aim of the study w...Nano-phytosomes(NP),lipid-based nano-carriers,were used to encapsulate the phycocyanin.Phycocyanin(Phy)is known for its important biological properties with low bioavailability and low stability.The aim of the study was to prepare phosphatidylcholine(PC)based Phy loaded NP to overcome the bioavailability and storage stability issues.The characterization of NP such as entrapment efficiency(EE),particle size,poly-dispersity index(PDI),ζ-potential and microstructural properties was conducted and in vitro bioaccessibility and storage stability of bioactive properties were investigated.The highest EE was determined as 81.92%however with a loading capacity(LC)of 58.12%.Phy-NPs showed good characteristics,such as low PDI values(<0.5),low particle size(106.13–134.10 nm),and non-dense spherical shape of microstructure.All NP complexes showed significant bioaccessibility with total phenolic content(TPC)values greater than 50%in intestinal tract.Unfortunately,PC based NP did not show a clear-cut pattern of TPC and color protection of Phy via increased PC content.展开更多
To the best of our knowledge, “phytosomal” encapsulation of extracts in edible films has not been applied for enhancing the shelf life of food products by now;as a result, phytosomal encapsulation was used in this r...To the best of our knowledge, “phytosomal” encapsulation of extracts in edible films has not been applied for enhancing the shelf life of food products by now;as a result, phytosomal encapsulation was used in this research to bring about a sustainable release of the extract from the edible film and prompt a significant shelf life enhancement. For this purpose, first, the Alyssum homolocarpum seed gum (AHSG) film was enriched with various levels (1–20% w/w) of Echinacea purpurea (L.) extract-phospholipid phytosome (EEPP) and, then, the structural (FTIR and SEM), thermal, physicochemical, mechanical and radical scavenging properties of the films as well as release kinetics of the extracts from the films were evaluated. Then, the chicken meat was packaged with the developed film and its different parameters including microbial population, chemical indices (TBARS and pH) as well as sensory properties of the meat were compared with those of the control film. Based on the results, as the EEPP percentage increased, water solubility, moisture content, water vapor permeability of AHSG films decreased favorably, and their tensile strength enhanced successfully. Besides, incorporation of EEPP improved the radical scavenging properties and melting point of the base film considerably. Structural surveys revealed that some chemical interactions (hydrogen bonds) occurred between EEPP and AHSG matrix. A two-fold increase in the shelf life of meat was recognized as the microbial and chemical indices of the developed film after 14 days were even better than those indices of the control film after 7 days.展开更多
Background:Carotenoids play important role in delay of aging process.Orange coloured tubular calyx of flowers of Nyctanthes arbor-tristis contains crocin,an apocarotenoid which forms a major component of stigma of saf...Background:Carotenoids play important role in delay of aging process.Orange coloured tubular calyx of flowers of Nyctanthes arbor-tristis contains crocin,an apocarotenoid which forms a major component of stigma of saffron.Due to presence of crocin in orange coloured tubular calyx of Nyctanthes arbor-tristis,it can be used as an economical substitute to saffron for its medicinal and cosmetic utilities.Lutein from flower petals of Tagetes patula L.,is another popular carotenoid which has antioxidant effect and many health benefits.The carotenoids are highly unstable when exposed to atmosphere.One of the ways to improve stability of these phytoconstituents,is their entrapment in phytosomes.Preparation of phytosomes will have dual advantages of improving stability as well as bioavailability of molecule.Objective:In the present study crocin and lutein rich extracts were entrapped into phytosomes to improve stability and efficacy of topical preparation.Methods:The phytosomes of Carotenoid rich extract of tubular calyx of Nyctanthes arbor-tristis L.and the petals of Tagetes patula L.(standardized for crocin and lutein content)were prepared using lipid film hydration technique and these phytosomes were then incorporated into gel base.The gel formulation was evaluated for stability as per ICH guidelines.Efficacy of formulation was evaluated by d-galactose induced aging model.Aging in skin was induced by administration of d-galactose(100 mg/kg bwsc.)to albino mice for 42 days.The gel formulation was applied topically for 42 days.Then the effect of formulation on skin aging was evaluated by estimation of biochemical parameters viz.glutathione and malondialdehyde(MDA)and histopathological studies of treated skin samples.Expression of COL type I and elastin genes in skin samples was also carried out by RT-PCR.Results:Percent entrapment(%w/w)of crocin and lutein in phytosomes were found to be 60.20%and 50.81%,respectively.Accelerated stability studies showed improvement in stability of carotenoids viz.crocin and lutein and the content of crocin and lutein in formulation was found in the range of 99.98%w/w to 99.85%w/w at the end of three months.The formulation containing extract of Phytosomes of carotenoid rich extracts of Nyctanthes arbor-tristis L.and the petals of Tagetes patula L.exhibited potent antiaging activity through significant(P<0.05)increase in dermal and epidermal layers,and increase in GSH levels of skin as compared to the untreated group.The treatment with the gel formulation revealed upregulation of collagen type I and elastin genes.There was significant reduction in lipid peroxidation as revealed through reduction in MDA levels as compared to untreated group.Conclusion:Crocin and lutein have potential to prevent skin aging via upregulation of collagen type I gene and elastin gene.Upregulation of genes resulted into increase in the thickness of epidermal and dermal layer along with reduction in oxidative stress in skin.Entrapment of carotenoid rich extracts of Nyctanthes arbor-tristis and Tagetes patula in phytosomes enhanced the stability and efficacy of the formulation.展开更多
文摘Objective:To explore the effects of a nano-formulation of curcumin(phytosomal curcumin)on the clinical and pathological symptoms of collagen-induced arthritis(CIA)in rats.Methods:Forty male Wistar rats were immunized with an emulsion containing bovine typeⅡcollagen and incomplete Freund's adjuvant and then administered phytosomal curcumin post-immunization.Clinical symptoms and histological analysis of the synovial tissues were performed.The effect of phytosomal curcumin on Th17 and Treg parameters was also evaluated.Results:Phytosomal curcumin reduced the clinical severity and paw swelling in CIA-induced rats,which was accompanied by a reduction in the number of inflammatory cell infiltration in the synovial tissue.Additionally,treatment with phytosomal curcumin significantly inhibited CIA-associated mediators as well as increased the anti-inflammatory mediators in comparison to the control groups.Conclusions:Phytosomal curcumin could improve CIA autoimmune responses and can be considered a potential candidate for the treatment of rheumatoid arthritis.
基金The National Science and Technology Major Projects"Major New Drugs Innovation and Development"(Grant No.2009ZX09103-007)
文摘Many active constituents from herbal plants have well-established pharmacological effects in vitro. But they demonstrate less or no activities in vivo due to various problems of themselves, which severely restricts their clinical applications. After forming phytosomes with phospholipids in aprotic solvent, the active constituents exhibit different physicochemical properties from the free form. In particular, the bioavailability of the active constituent-phytosomes is enhanced greatly due to the improved capacity to cross the biomembrane and reach circulation. Therefore, increasing attention has been attracted to the use of phytosomes in recent years. Based on the published reports, we reviewed the recent progress in the research of phytosomes including preparation, characterization, structure verification and clinical applications.
文摘Phytosomes(phytophospholipid complex) are dosage forms that have recently been introduced to increase the stability and therapeutic effect of herbal medicine. Currently, bioactive herbs and the phytochemicals they contain are considered to be the best remedies for chronic diseases. One promising approach to increase the efficacy of plant-based therapies is to improve the stability and bioavailability of their bio-active ingredients. Phytosomes employ phospholipids as their active ingredients, and use their amphiphilic properties to solubilize and protect herbal extracts. The unique properties of phospholipids in drug delivery and their use in herbal medicines to improve bioavailability results in significantly enhanced health benefits. The introduction of phytosome nanotechnology can alter and revolutionize the current state of drug delivery. The goal of this review is to explain the application of phytosomes, their future prospects in drug delivery, and their advantages over conventional formulations.
文摘Across the annals of time,organic molecules sourced from nature have found innumerable uses within the realms of healthcare,pharmaceuticals,and the study of living organisms.This abundant source of natural compounds has exhibited immense promise in the cure of diverse ailments,mainly neurodegenerative diseases owing to their minimum toxic and adverse effects.However,different challenges exist with phytocompounds from plants such as poor permeation,poor solubility(water/lipid),unsteadiness under extremely acidic pH conditions,and lack of targeting specificity.Furthermore,as a result of the existence of blood-brain barrier membrane and inconvenient pharmacokinetics characteristics of phytocompounds,their passage into the brain is constrained.In order to address this issue and augment the transportation of medications into the brain at a therapeutically effective level,it is imperative to formulate an innovative and pragmatic strategy.Many papers have shown that nanoformulations containing phytocompounds(resveratrol,quercetin,ferulic acid,curcumin,berberine,etc.)effectively improved many neurodegenerative diseases such as Parkinson’s,Alzheimer’s and Huntington’s diseases.This study provides an overview of phytocompounds that are used in nanosized lipid drug delivery systems.These systems are categorized according to lipid types and preparation techniques used in the formulation.Some studies regarding these systems and phytocompounds are also summarized.
基金supported by the National Natural Science Foundation of China(No.82104072 and 82373800,China)Guangdong Natural Science Foundation(No.2024A1515010896,China)。
文摘With the aging of the population,the incidence of Alzheimer’s disease(AD)has increased dramatically,causing severe medical,care,and economic burdens on society and families.The efficacy of rivastigmine hydrogen tartrate(RHT),the first-line clinical treatment,is severely limited by the complex and multiple pathogenesis of AD and low brain bioavailability caused by the blood-brain barrier(BBB).Confronting such two bottlenecks,the development of multi-target agents encapsulated BBB-bypassing drug delivery systems offer tremendous thera-peutics possibilities for AD.In this study,a tailored phytosomes based nose-to-brain drug delivery system with appropriate plume was successfully designed and developed.On the one hand,Ginseng RG3-based phytosomes loaded with RHT was designed for the co-delivery of GRg3 and RHT,achieving the multi-target pharmacology for AD treatment.On the other hand,a tailored nose-to-brain drug delivery system was established for the satisfactory nose-to-brain delivery efficiency,avoiding the obstacle of BBB through bypassing it.In the phar-macodynamic study based on AD rat model,GRg3@RHT exhibited obviously synergic effect,effectively break the vicious cycle of AD progression,ultimately markedly ameliorating learning and memory ability as well as behavioral dysfunctions,and delaying the neurodegenerative process associated with AD.In addition,the strong correlation of viscosity-droplet size-plume geometry-olfactory deposition was also established,and further proved by the in vivo pharmacokinetic study,which is proposed to provide evidence to enhance nose-to-brain delivery efficiency.This study is anticipated to provide novel insights into AD treatment strategies while of-fering innovative ideas for drug delivery approaches targeting nervous system disorders.
文摘In recent years,there has been extensive research on valorization of food wastes and a growing interest in nano-liposomal systems for food applications.This paper discusses the case of phosphatidylcholine basednanophytosomes loaded with anthocyanins extracted from red onion(RNPs)to overcome the bio-stability during digestion.The characterization of lyophilized RNPs in terms of entrapment efficiency,particle size,poly-dispersity index(PDI),ζ-potential,morphological properties,in vitro bioaccessibility and release kinetics were investigated.Entrapment efficiency was determined as 78.63%with lowest particle size(177.73 nm)and PDI value(0.45)and non-dense spherical microstructure for RNP6(red onion peel anthocyanin extract:soybean phosphatidylcholine at 1:6 ratio).Apart from the particle size,entrapment efficiency was determined higher than 75%,which indicates good entrapment.Additionally,from the cumulative release of RNPs concluded as a successful nano-structure with a two-fold increase in intestinal medium.However,poor Carr index and Hausner ratio suggest some limitations of the current nanoliposomes process which could be further improved.Red onion peel wastes,which are typically discarded,can serve as excellent sources of anthocyanins,and its preparation to nanophytosomes could be used as functional food ingredient or food supplements.
文摘Nano-phytosomes(NP),lipid-based nano-carriers,were used to encapsulate the phycocyanin.Phycocyanin(Phy)is known for its important biological properties with low bioavailability and low stability.The aim of the study was to prepare phosphatidylcholine(PC)based Phy loaded NP to overcome the bioavailability and storage stability issues.The characterization of NP such as entrapment efficiency(EE),particle size,poly-dispersity index(PDI),ζ-potential and microstructural properties was conducted and in vitro bioaccessibility and storage stability of bioactive properties were investigated.The highest EE was determined as 81.92%however with a loading capacity(LC)of 58.12%.Phy-NPs showed good characteristics,such as low PDI values(<0.5),low particle size(106.13–134.10 nm),and non-dense spherical shape of microstructure.All NP complexes showed significant bioaccessibility with total phenolic content(TPC)values greater than 50%in intestinal tract.Unfortunately,PC based NP did not show a clear-cut pattern of TPC and color protection of Phy via increased PC content.
文摘To the best of our knowledge, “phytosomal” encapsulation of extracts in edible films has not been applied for enhancing the shelf life of food products by now;as a result, phytosomal encapsulation was used in this research to bring about a sustainable release of the extract from the edible film and prompt a significant shelf life enhancement. For this purpose, first, the Alyssum homolocarpum seed gum (AHSG) film was enriched with various levels (1–20% w/w) of Echinacea purpurea (L.) extract-phospholipid phytosome (EEPP) and, then, the structural (FTIR and SEM), thermal, physicochemical, mechanical and radical scavenging properties of the films as well as release kinetics of the extracts from the films were evaluated. Then, the chicken meat was packaged with the developed film and its different parameters including microbial population, chemical indices (TBARS and pH) as well as sensory properties of the meat were compared with those of the control film. Based on the results, as the EEPP percentage increased, water solubility, moisture content, water vapor permeability of AHSG films decreased favorably, and their tensile strength enhanced successfully. Besides, incorporation of EEPP improved the radical scavenging properties and melting point of the base film considerably. Structural surveys revealed that some chemical interactions (hydrogen bonds) occurred between EEPP and AHSG matrix. A two-fold increase in the shelf life of meat was recognized as the microbial and chemical indices of the developed film after 14 days were even better than those indices of the control film after 7 days.
基金supported by National Medicinal Plant Board(NMPB),Dept.of Ayush,Government of India.(Project No.R&D/MS 04/2010).
文摘Background:Carotenoids play important role in delay of aging process.Orange coloured tubular calyx of flowers of Nyctanthes arbor-tristis contains crocin,an apocarotenoid which forms a major component of stigma of saffron.Due to presence of crocin in orange coloured tubular calyx of Nyctanthes arbor-tristis,it can be used as an economical substitute to saffron for its medicinal and cosmetic utilities.Lutein from flower petals of Tagetes patula L.,is another popular carotenoid which has antioxidant effect and many health benefits.The carotenoids are highly unstable when exposed to atmosphere.One of the ways to improve stability of these phytoconstituents,is their entrapment in phytosomes.Preparation of phytosomes will have dual advantages of improving stability as well as bioavailability of molecule.Objective:In the present study crocin and lutein rich extracts were entrapped into phytosomes to improve stability and efficacy of topical preparation.Methods:The phytosomes of Carotenoid rich extract of tubular calyx of Nyctanthes arbor-tristis L.and the petals of Tagetes patula L.(standardized for crocin and lutein content)were prepared using lipid film hydration technique and these phytosomes were then incorporated into gel base.The gel formulation was evaluated for stability as per ICH guidelines.Efficacy of formulation was evaluated by d-galactose induced aging model.Aging in skin was induced by administration of d-galactose(100 mg/kg bwsc.)to albino mice for 42 days.The gel formulation was applied topically for 42 days.Then the effect of formulation on skin aging was evaluated by estimation of biochemical parameters viz.glutathione and malondialdehyde(MDA)and histopathological studies of treated skin samples.Expression of COL type I and elastin genes in skin samples was also carried out by RT-PCR.Results:Percent entrapment(%w/w)of crocin and lutein in phytosomes were found to be 60.20%and 50.81%,respectively.Accelerated stability studies showed improvement in stability of carotenoids viz.crocin and lutein and the content of crocin and lutein in formulation was found in the range of 99.98%w/w to 99.85%w/w at the end of three months.The formulation containing extract of Phytosomes of carotenoid rich extracts of Nyctanthes arbor-tristis L.and the petals of Tagetes patula L.exhibited potent antiaging activity through significant(P<0.05)increase in dermal and epidermal layers,and increase in GSH levels of skin as compared to the untreated group.The treatment with the gel formulation revealed upregulation of collagen type I and elastin genes.There was significant reduction in lipid peroxidation as revealed through reduction in MDA levels as compared to untreated group.Conclusion:Crocin and lutein have potential to prevent skin aging via upregulation of collagen type I gene and elastin gene.Upregulation of genes resulted into increase in the thickness of epidermal and dermal layer along with reduction in oxidative stress in skin.Entrapment of carotenoid rich extracts of Nyctanthes arbor-tristis and Tagetes patula in phytosomes enhanced the stability and efficacy of the formulation.
