{"title":"四氢香豆素超变形纳米胶囊乳膏的配方、优化及抗氧化性能评价","authors":"Ankita Kanshide, Malleswara Rao Peram, Nagesh Chandrasekhar, Arzoo Jamadar, Vijay Kumbar, Manohar Kugaji","doi":"10.1007/s12247-022-09696-0","DOIUrl":null,"url":null,"abstract":"<div><h3>Purpose</h3><p>Tetrahydrocurcumin (THC) has excellent anti-inflammatory and antioxidant properties, but its poor aqueous solubility limits its use in pharmaceutical and cosmetic formulations. The present study aimed to develop, optimize, and characterize a nanovesicular cream-loaded tetrahydrocurcumin transfersomes (THC-TFs) to improve its topical delivery and enhance its antioxidant activity.</p><h3>Methodology</h3><p>THC-TFs were prepared using the thin-film hydration technique and characterized for vesicle size, zeta potential, entrapment efficiency, and skin penetration. The optimized transfersomal formulation was incorporated into a cream base and characterized for various parameters.</p><h3>Results</h3><p>The optimized THC-TF (OPT-THC-TF) suspension showed a vesicle size of 212 ± 4.78 nm, a zeta potential of –40.3 mV, and percentage entrapment efficiency of 83.74 ± 0.21. Fluorescence microscopy revealed that transfersomes penetrated the deeper layers of skin. Ex vivo skin permeation demonstrated that OPT-THC-TF cream has better skin permeation and deposition potential compared to the THC conventional cream. The α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging activity assay revealed that the antioxidant potential of THC-TF cream (77%) was comparable to that of pure THC (81%), demonstrating that THC antioxidant activity is unaffected by its encapsulation into transfersomes. The cell viability study revealed that THC-TF cream (***<i>p</i> < 0.001) significantly decreased the cytotoxicity toward normal cells (L-929) compared to pure THC solution.</p><h3>Conclusion</h3><p>Based on these findings, it was concluded that the OPT-THC-TF cream could be a promising strategy for the topical delivery of encapsulated drugs for the effective treatment of various dermatological disorders.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"18 3","pages":"980 - 998"},"PeriodicalIF":2.7000,"publicationDate":"2022-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":"{\"title\":\"Formulation, Optimization, and Antioxidant Evaluation of Tetrahydrocurcumin-Loaded Ultradeformable Nanovesicular Cream\",\"authors\":\"Ankita Kanshide, Malleswara Rao Peram, Nagesh Chandrasekhar, Arzoo Jamadar, Vijay Kumbar, Manohar Kugaji\",\"doi\":\"10.1007/s12247-022-09696-0\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Purpose</h3><p>Tetrahydrocurcumin (THC) has excellent anti-inflammatory and antioxidant properties, but its poor aqueous solubility limits its use in pharmaceutical and cosmetic formulations. The present study aimed to develop, optimize, and characterize a nanovesicular cream-loaded tetrahydrocurcumin transfersomes (THC-TFs) to improve its topical delivery and enhance its antioxidant activity.</p><h3>Methodology</h3><p>THC-TFs were prepared using the thin-film hydration technique and characterized for vesicle size, zeta potential, entrapment efficiency, and skin penetration. The optimized transfersomal formulation was incorporated into a cream base and characterized for various parameters.</p><h3>Results</h3><p>The optimized THC-TF (OPT-THC-TF) suspension showed a vesicle size of 212 ± 4.78 nm, a zeta potential of –40.3 mV, and percentage entrapment efficiency of 83.74 ± 0.21. Fluorescence microscopy revealed that transfersomes penetrated the deeper layers of skin. Ex vivo skin permeation demonstrated that OPT-THC-TF cream has better skin permeation and deposition potential compared to the THC conventional cream. The α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging activity assay revealed that the antioxidant potential of THC-TF cream (77%) was comparable to that of pure THC (81%), demonstrating that THC antioxidant activity is unaffected by its encapsulation into transfersomes. The cell viability study revealed that THC-TF cream (***<i>p</i> < 0.001) significantly decreased the cytotoxicity toward normal cells (L-929) compared to pure THC solution.</p><h3>Conclusion</h3><p>Based on these findings, it was concluded that the OPT-THC-TF cream could be a promising strategy for the topical delivery of encapsulated drugs for the effective treatment of various dermatological disorders.</p></div>\",\"PeriodicalId\":656,\"journal\":{\"name\":\"Journal of Pharmaceutical Innovation\",\"volume\":\"18 3\",\"pages\":\"980 - 998\"},\"PeriodicalIF\":2.7000,\"publicationDate\":\"2022-12-17\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Pharmaceutical Innovation\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s12247-022-09696-0\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Pharmaceutical Innovation","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s12247-022-09696-0","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Formulation, Optimization, and Antioxidant Evaluation of Tetrahydrocurcumin-Loaded Ultradeformable Nanovesicular Cream
Purpose
Tetrahydrocurcumin (THC) has excellent anti-inflammatory and antioxidant properties, but its poor aqueous solubility limits its use in pharmaceutical and cosmetic formulations. The present study aimed to develop, optimize, and characterize a nanovesicular cream-loaded tetrahydrocurcumin transfersomes (THC-TFs) to improve its topical delivery and enhance its antioxidant activity.
Methodology
THC-TFs were prepared using the thin-film hydration technique and characterized for vesicle size, zeta potential, entrapment efficiency, and skin penetration. The optimized transfersomal formulation was incorporated into a cream base and characterized for various parameters.
Results
The optimized THC-TF (OPT-THC-TF) suspension showed a vesicle size of 212 ± 4.78 nm, a zeta potential of –40.3 mV, and percentage entrapment efficiency of 83.74 ± 0.21. Fluorescence microscopy revealed that transfersomes penetrated the deeper layers of skin. Ex vivo skin permeation demonstrated that OPT-THC-TF cream has better skin permeation and deposition potential compared to the THC conventional cream. The α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging activity assay revealed that the antioxidant potential of THC-TF cream (77%) was comparable to that of pure THC (81%), demonstrating that THC antioxidant activity is unaffected by its encapsulation into transfersomes. The cell viability study revealed that THC-TF cream (***p < 0.001) significantly decreased the cytotoxicity toward normal cells (L-929) compared to pure THC solution.
Conclusion
Based on these findings, it was concluded that the OPT-THC-TF cream could be a promising strategy for the topical delivery of encapsulated drugs for the effective treatment of various dermatological disorders.
期刊介绍:
The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories:
Materials science,
Product design,
Process design, optimization, automation and control,
Facilities; Information management,
Regulatory policy and strategy,
Supply chain developments ,
Education and professional development,
Journal of Pharmaceutical Innovation publishes four issues a year.