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用于治疗雄激素性脱发的载有非那雄胺的二甲基亚砜脂质体增强皮肤渗透性:与传统脂质体的比较

Enhanced skin penetration of Finasteride loaded DMSO-liposomes for the treatment of androgenic alopecia: comparison with conventional liposomes.

作者信息

Ramkar Shweta, Kaurav Monika, Sudheesh M S, Pandey Ravi Shankar

机构信息

Department of Pharmacy, Bilaspur, India.

KIET School of Pharmacy, Ghaziabad, India.

出版信息

Drug Dev Ind Pharm. 2023 Jan;49(1):52-61. doi: 10.1080/03639045.2023.2182122. Epub 2023 Feb 23.

Abstract

Long-term treatment with finasteride (FIN) for androgenic alopecia is restricted due to its systemic side effects. To address this problem, DMSO-modified liposomes were prepared in the present study to improve the topical delivery of FIN. DMSO-liposomes were prepared by a modification of the ethanol injection method. It was hypothesized that the permeation-enhancing property of DMSO could promote drug delivery to deeper skin layer where hair follicles are present. Liposomes were optimized by quality by design (QbD) approach and biologically evaluated in a rat model of testosterone-induced alopecia. Optimized DMSO-liposomes were spherical and had mean vesicle size, zeta potential, and entrapment efficiency of 330.1 ± 1.5, -14.52 ± 1.32, and 59.02 ± 1.12%, respectively. Biological evaluation on testosterone-induced alopecia and skin histology shows that follicular density and anagen/telogen (A/T) ratio were increased in rats treated with DMSO-liposomes as compared to FIN-liposomes without DMSO and an alcoholic solution of FIN applied topically. DMSO-liposomes could be promising skin delivery vehicles for FIN or similar drugs.

摘要

由于非那雄胺(FIN)存在全身副作用,其用于雄激素性脱发的长期治疗受到限制。为解决这一问题,本研究制备了二甲基亚砜(DMSO)修饰的脂质体,以改善FIN的局部递送。DMSO脂质体通过改进乙醇注入法制备。据推测,DMSO的渗透增强特性可促进药物递送至存在毛囊的更深皮肤层。采用质量源于设计(QbD)方法对脂质体进行优化,并在睾酮诱导的脱发大鼠模型中进行生物学评价。优化后的DMSO脂质体呈球形,平均囊泡大小、zeta电位和包封率分别为330.1±1.5、-14.52±1.32和59.02±1.12%。对睾酮诱导的脱发和皮肤组织学进行的生物学评价表明,与未添加DMSO的FIN脂质体和局部应用的FIN醇溶液相比,用DMSO脂质体处理的大鼠毛囊密度和生长期/休止期(A/T)比率增加。DMSO脂质体可能是用于FIN或类似药物的有前景的皮肤递送载体。

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