QbD-Anchored Preparation and Assessment of Transethosomal Gel for Enhanced Skin Permeation of Tamoxifen Citrate.

IF 2.6 4区医学 Q2 PHARMACOLOGY & PHARMACY

Current pharmaceutical design Pub Date : 2025-03-27 DOI:10.2174/0113816128344198250308022732

Preeti S Bobade, Ayush S Mishra, Saurabh B Ganorkar, Darshan R Telange, Shailesh S Chalikwar

{"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":"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.","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}

引用次数: 0

Abstract

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.

查看原文本刊更多论文

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。

背景：柠檬酸他莫昔芬（TMC）是一种抗雌激素药物，用于晚期乳腺癌的治疗。然而，其口服和肠外途径相关的副作用和溶解度问题限制了其医学应用。目的：制备负载柠檬酸他莫昔芬的transthosomal gel (TMC TEsG)，以提高TMC的包封效率、体外溶出度和体外渗透。方法：采用HPH法制备TMC TEs，并采用23因子设计进行优化。通过冷分散将优化后的TMC TEs转化为TMC TEsG。对TMC TEs和TMC TEsG进行粒径、微观、官能团相互作用、结晶、体外溶出、体外渗透、铺展性、TMC含量和织构分析。结果：优化研究表明，23种设计方案对TMC - TE的开发具有适用性和有效性。粒径为~163.1 nm， zeta电位为~-26.8 mV的TMC TEs提高了物理稳定性和透皮性。TMC TEs的捕集效率高达84.49%。透射电镜显示了TMC TEs的球形和密封结构的囊泡。物理分析支持TMC TEs的形成。与纯TMC（~68%）相比，囊泡提高了溶出度（~96%）。与TMC凝胶（~55%）相比，TMC TEsG增加了~82%的通透性。TMC TEsG的pH值（~5.61），粘度（~4077.5 cps），涂抹性（~49.84 g.cm/s），具有良好的安全性和皮肤适用性。结论：实验结果提示设计生成的柔性TMC TEs具有透皮渗透潜能，可用于皮肤相关疾病的治疗。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Current pharmaceutical design 医学-药学

CiteScore

6.30

自引率

0.00%

发文量

302

审稿时长

2 months

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.