Preeti S Bobade, Ayush S Mishra, Saurabh B Ganorkar, Darshan R Telange, Shailesh S Chalikwar
{"title":"qbd锚定制备和评价经体凝胶增强柠檬酸他莫昔芬的皮肤渗透。","authors":"Preeti S Bobade, Ayush S Mishra, Saurabh B Ganorkar, Darshan R Telange, Shailesh S Chalikwar","doi":"10.2174/0113816128344198250308022732","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>Tamoxifen citrate (TMC), an antiestrogenic drug, is employed in the healing of advanced breast cancer. However, its oral and parenteral route-associated side effects and solubility issues restricted its medical utilization.</p><p><strong>Objective: </strong>The research aimed to prepare a tamoxifen citrate-loaded transethosomal gel (TMC TEsG) to enhance TMC entrapment efficiency, in vitro dissolution, and ex vivo permeation.</p><p><strong>Methods: </strong>TMC TEs were developed employing an HPH method and optimized using 23 factorial designs. The optimized TMC TEs were converted into TMC TEsG by cold dispersion. TMC TEs and TMC TEsG were estimated for particle size, microscopic, functional group interaction, crystalline, in vitro dissolution, ex vivo permeation, spreadability, TMC content, and texture analysis.</p><p><strong>Results: </strong>The optimization study revealed the suitability and validity of 23 designs for developing TMC TE. TMC TEs with particle size ~163.1 nm and zeta potential of ~-26.8 mV improved the physical stability and skin permeation. TMC TEs showed a high entrapment efficiency of ~84.49%. TEM depicts spherical and sealed structure vesicles of TMC TEs. Physical analysis supported the formation of TMC TEs. Vesicles improved the dissolution (~96%) compared to pure TMC (~68%). The TMC TEsG increased the permeation (~82%) compared to TMC gel (~55%). TMC TEsG with pH (~5.61), viscosity (~4077.5 cps), and spreadability (~49.84 g.cm/s) exhibiting safety and easy applicability to the skin.</p><p><strong>Conclusion: </strong>Outcomes suggest the transdermal permeation potential of design-generated flexible TMC TEs and, thus, could be employed to treat skin-related diseases.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6000,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"QbD-Anchored Preparation and Assessment of Transethosomal Gel for Enhanced Skin Permeation of Tamoxifen Citrate.\",\"authors\":\"Preeti S Bobade, Ayush S Mishra, Saurabh B Ganorkar, Darshan R Telange, Shailesh S Chalikwar\",\"doi\":\"10.2174/0113816128344198250308022732\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>Tamoxifen citrate (TMC), an antiestrogenic drug, is employed in the healing of advanced breast cancer. However, its oral and parenteral route-associated side effects and solubility issues restricted its medical utilization.</p><p><strong>Objective: </strong>The research aimed to prepare a tamoxifen citrate-loaded transethosomal gel (TMC TEsG) to enhance TMC entrapment efficiency, in vitro dissolution, and ex vivo permeation.</p><p><strong>Methods: </strong>TMC TEs were developed employing an HPH method and optimized using 23 factorial designs. The optimized TMC TEs were converted into TMC TEsG by cold dispersion. TMC TEs and TMC TEsG were estimated for particle size, microscopic, functional group interaction, crystalline, in vitro dissolution, ex vivo permeation, spreadability, TMC content, and texture analysis.</p><p><strong>Results: </strong>The optimization study revealed the suitability and validity of 23 designs for developing TMC TE. TMC TEs with particle size ~163.1 nm and zeta potential of ~-26.8 mV improved the physical stability and skin permeation. TMC TEs showed a high entrapment efficiency of ~84.49%. TEM depicts spherical and sealed structure vesicles of TMC TEs. Physical analysis supported the formation of TMC TEs. Vesicles improved the dissolution (~96%) compared to pure TMC (~68%). The TMC TEsG increased the permeation (~82%) compared to TMC gel (~55%). TMC TEsG with pH (~5.61), viscosity (~4077.5 cps), and spreadability (~49.84 g.cm/s) exhibiting safety and easy applicability to the skin.</p><p><strong>Conclusion: </strong>Outcomes suggest the transdermal permeation potential of design-generated flexible TMC TEs and, thus, could be employed to treat skin-related diseases.</p>\",\"PeriodicalId\":10845,\"journal\":{\"name\":\"Current pharmaceutical design\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":2.6000,\"publicationDate\":\"2025-03-27\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current pharmaceutical design\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.2174/0113816128344198250308022732\",\"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":"Current pharmaceutical design","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/0113816128344198250308022732","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
QbD-Anchored Preparation and Assessment of Transethosomal Gel for Enhanced Skin Permeation of Tamoxifen Citrate.
Background: Tamoxifen citrate (TMC), an antiestrogenic drug, is employed in the healing of advanced breast cancer. However, its oral and parenteral route-associated side effects and solubility issues restricted its medical utilization.
Objective: The research aimed to prepare a tamoxifen citrate-loaded transethosomal gel (TMC TEsG) to enhance TMC entrapment efficiency, in vitro dissolution, and ex vivo permeation.
Methods: TMC TEs were developed employing an HPH method and optimized using 23 factorial designs. The optimized TMC TEs were converted into TMC TEsG by cold dispersion. TMC TEs and TMC TEsG were estimated for particle size, microscopic, functional group interaction, crystalline, in vitro dissolution, ex vivo permeation, spreadability, TMC content, and texture analysis.
Results: The optimization study revealed the suitability and validity of 23 designs for developing TMC TE. TMC TEs with particle size ~163.1 nm and zeta potential of ~-26.8 mV improved the physical stability and skin permeation. TMC TEs showed a high entrapment efficiency of ~84.49%. TEM depicts spherical and sealed structure vesicles of TMC TEs. Physical analysis supported the formation of TMC TEs. Vesicles improved the dissolution (~96%) compared to pure TMC (~68%). The TMC TEsG increased the permeation (~82%) compared to TMC gel (~55%). TMC TEsG with pH (~5.61), viscosity (~4077.5 cps), and spreadability (~49.84 g.cm/s) exhibiting safety and easy applicability to the skin.
Conclusion: Outcomes suggest the transdermal permeation potential of design-generated flexible TMC TEs and, thus, could be employed to treat skin-related diseases.
期刊介绍：
Current Pharmaceutical Design publishes timely in-depth reviews and research articles from leading pharmaceutical researchers in the field, covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area guest edited by an acknowledged authority in the field.
Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
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