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基于薄荷醇的新型超可变形囊泡:一种抗真菌药物的配方、优化与评价

Menthol-based Novel Ultra-Deformable Vesicle: Formulation, Optimization and Evaluation of an Antifungal Drug.

作者信息

Manjushree Hema, Nayak Devika, Halagali Praveen, Rathnanand Mahalaxmi, Tawale Roshan, Ananthmurthy Koteshwara, Aranjani Jesil Mathew, Tippavajhala Vamshi Krishna

机构信息

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, 576107, India.

Department of Pharmaceutical Biotechnology, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, 576107, India.

出版信息

AAPS PharmSciTech. 2025 Jan 8;26(1):23. doi: 10.1208/s12249-024-03021-3.

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 2 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.

摘要

当前的研究旨在通过制备载有酮康唑的薄荷醇脂质体,建立一种新型的超可变形囊泡系统,以增强药物透过皮肤的能力。这是通过常规的薄膜蒸发和水合技术实现的。为了研究配方参数对薄荷醇脂质体特性的影响,使用Design-Expert®软件采用2全因子设计。优化后的批次显示出囊泡大小(107.6纳米)、多分散指数(PDI)(0.248)、包封率(%EE)(76.9%)和zeta电位(-33.7毫伏)。体外皮肤渗透研究和体外药物释放结果表明,与其他配方相比,皮肤渗透和药物释放得到了增强。体外抗真菌和体内药效学研究阐明了优化配方对白色念珠菌的增强有效性。总之,薄荷醇脂质体可以作为一种有效的载体,通过皮肤增强药物渗透,以提高其抗真菌活性。

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