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了解(透)皮给药中的微乳剂和纳米乳剂。

Understanding Microemulsions and Nanoemulsions in (Trans)Dermal Delivery.

作者信息

Musakhanian Jasmine, Osborne David W

机构信息

, Gattefossé, Paramus, New Jersey, USA.

Consulting, Fort Collins, Colorado, USA.

出版信息

AAPS PharmSciTech. 2025 Jan 10;26(1):31. doi: 10.1208/s12249-024-02997-2.

Abstract

Continuously explored in pharmaceuticals, microemulsions and nanoemulsions offer drug delivery opportunities that are too significant to ignore, namely safe delivery of clinically relevant drug doses across biological membranes. Their effectiveness as drug vehicles in mucosal and (trans)dermal delivery is evident from the volume of published literature. Commonly, their ability to enhance skin permeation is attributed to dispersion size, a characteristic closely related to solubilization capacity. However, the literature falls short on distinctions between microemulsions and nanoemulsions for definitions, behavior, or specific differences in their mechanisms of action in (trans)dermal delivery. The focus is typically on surfactant/cosurfactant ratio and droplet size but the role of mesostructures or the effect of cosolvent (C), oil (O) or water (W) on permeation profile remain poorly explained. Towards a deeper understanding of these vehicles in (trans)dermal drug delivery, this review begins with their conceptual and practical distinctions before delving into the published works for less obvious but potentially important underlying mechanisms; notably composition and the competitive positioning of system constituents in the resulting microstructures and subsequent effect(s) these may have on skin structures and drug permeability. For practical purposes, this review focuses on formulation systems based on ternary diagrams with commonly accepted non-ionic surfactants, cosurfactants, cosolvents, and oils used in pharmaceutical applications.

摘要

在制药领域不断得到探索的微乳剂和纳米乳剂提供了不容忽视的药物递送机会,即能安全递送临床上相关的药物剂量穿过生物膜。从已发表文献的数量来看,它们作为药物载体在黏膜和(经)皮给药方面的有效性是显而易见的。通常,它们增强皮肤渗透的能力归因于分散尺寸,这一特性与增溶能力密切相关。然而,关于微乳剂和纳米乳剂在(经)皮给药中的定义、行为或作用机制的具体差异,文献中缺乏明确区分。重点通常放在表面活性剂/助表面活性剂比例和液滴大小上,但中观结构的作用或助溶剂(C)、油(O)或水(W)对渗透曲线的影响仍解释不足。为了更深入地了解这些载体在(经)皮给药中的作用,本综述首先阐述它们在概念和实际方面的区别,然后深入研究已发表的文献,以探讨不太明显但可能很重要的潜在机制;特别是组成以及体系成分在所得微观结构中的竞争定位,以及这些可能对皮肤结构和药物渗透性产生的后续影响。出于实际目的,本综述重点关注基于三元相图的制剂系统,这些系统使用了制药应用中常用的非离子表面活性剂、助表面活性剂、助溶剂和油。

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