{"title":"Menthol-based Novel Ultra-Deformable Vesicle: Formulation, Optimization and Evaluation of an Antifungal Drug","authors":"Hema Manjushree, Devika Nayak, Praveen Halagali, Mahalaxmi Rathnanand, Roshan Tawale, Koteshwara Ananthmurthy, Jesil Mathew Aranjani, Vamshi Krishna Tippavajhala","doi":"10.1208/s12249-024-03021-3","DOIUrl":null,"url":null,"abstract":"<div><p>The current study aims to establish a novel ultra-deformable vesicular system to enhance the drug penetration across the skin by preparing the ketoconazole-loaded menthosomes. It was achieved through regular thin-film evaporation & hydration techniques. To examine the effect of formulation parameters on menthosome characteristics, a 2<sup>3</sup> full factorial design was used using Design-Expert® software. The optimized batch exhibited a vesicle size (107.6 nm), a polydispersity index (PDI) (0.248), entrapment efficiency (% EE) (76.9%), and a zeta potential (-33.7 mV). Results from <i>ex vivo</i> skin permeation studies and <i>in vitro</i> drug release demonstrated enhanced improved skin permeation and drug release compared to other formulations. An <i>in vitro</i> antifungal and <i>in vivo</i> pharmacodynamic study, elucidated the enhanced effectiveness of the optimized formulation against <i>Candida albicans</i>. In summary, menthosomes could serve as a potent vehicle to enhance drug penetration via the skin to improve its antifungal activity.</p><h3>Graphical Abstract</h3>\n<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 1","pages":""},"PeriodicalIF":3.4000,"publicationDate":"2025-01-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-024-03021-3.pdf","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"AAPS PharmSciTech","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1208/s12249-024-03021-3","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
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Abstract
The current study aims to establish a novel ultra-deformable vesicular system to enhance the drug penetration across the skin by preparing the ketoconazole-loaded menthosomes. It was achieved through regular thin-film evaporation & hydration techniques. To examine the effect of formulation parameters on menthosome characteristics, a 23 full factorial design was used using Design-Expert® software. The optimized batch exhibited a vesicle size (107.6 nm), a polydispersity index (PDI) (0.248), entrapment efficiency (% EE) (76.9%), and a zeta potential (-33.7 mV). Results from ex vivo skin permeation studies and in vitro drug release demonstrated enhanced improved skin permeation and drug release compared to other formulations. An in vitro antifungal and in vivo pharmacodynamic study, elucidated the enhanced effectiveness of the optimized formulation against Candida albicans. In summary, menthosomes could serve as a potent vehicle to enhance drug penetration via the skin to improve its antifungal activity.
期刊介绍：
AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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