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脂质体与皮肤:从药物递送 to 模型膜

Liposomes and skin: from drug delivery to model membranes.

作者信息

El Maghraby G M, Barry B W, Williams A C

机构信息

College of Pharmacy, King Saud University, Riyadh 11451, P.O. Box 2457, Saudi Arabia.

出版信息

Eur J Pharm Sci. 2008 Aug 7;34(4-5):203-22. doi: 10.1016/j.ejps.2008.05.002. Epub 2008 May 8.

Abstract

The early eighties saw the introduction of liposomes as skin drug delivery systems, initially promoted primarily for localised effects with minimal systemic delivery. Subsequently, a novel ultradeformable vesicular system (termed "Transfersomes" by the inventors) was reported for transdermal delivery with an efficiency similar to subcutaneous injection. Further research illustrated that the mechanisms of liposome action depended on the application regime and the vesicle composition and morphology. Ethical, health and supply problems with human skin have encouraged researchers to use skin models. Traditional models involved polymer membranes and animal tissue, but whilst of value for release studies, such models are not always good mimics for the complex human skin barrier, particularly with respect to the stratum corneal intercellular lipid domains. These lipids have a multiply bilayered organization, a composition and organization somewhat similar to liposomes. Consequently researchers have used vesicles as skin model membranes. Early work first employed phospholipid liposomes and tested their interactions with skin penetration enhancers, typically using thermal analysis and spectroscopic analyses. Another approach probed how incorporation of compounds into liposomes led to the loss of entrapped markers, analogous to "fluidization" of stratum corneum lipids on treatment with a penetration enhancer. Subsequently scientists employed liposomes formulated with skin lipids in these types of studies. Following a brief description of the nature of the skin barrier to transdermal drug delivery and the use of liposomes in drug delivery through skin, this article critically reviews the relevance of using different types of vesicles as a model for human skin in permeation enhancement studies, concentrating primarily on liposomes after briefly surveying older models. The validity of different types of liposome is considered and traditional skin models are compared to vesicular model membranes for their precision and accuracy as skin membrane mimics.

摘要

20世纪80年代初,脂质体作为皮肤给药系统被引入,最初主要用于局部效应,全身给药极少。随后,一种新型的超可变形囊泡系统(发明者称之为“传递体”)被报道用于透皮给药,其效率与皮下注射相似。进一步的研究表明,脂质体的作用机制取决于应用方式、囊泡组成和形态。人体皮肤的伦理、健康和供应问题促使研究人员使用皮肤模型。传统模型涉及聚合物膜和动物组织,但尽管对释放研究有价值,但这些模型并不总是能很好地模拟复杂的人体皮肤屏障,特别是在角质层细胞间脂质域方面。这些脂质具有多层双分子层结构,其组成和结构与脂质体有些相似。因此,研究人员将囊泡用作皮肤模型膜。早期工作首先使用磷脂脂质体,并测试它们与皮肤渗透促进剂的相互作用,通常使用热分析和光谱分析。另一种方法探讨了将化合物掺入脂质体如何导致包封标记物的损失,类似于用渗透促进剂处理后角质层脂质的“流化”。随后,科学家们在这类研究中使用了含有皮肤脂质的脂质体。在简要描述了皮肤屏障对透皮给药的性质以及脂质体在皮肤给药中的应用之后,本文批判性地回顾了在渗透增强研究中使用不同类型囊泡作为人体皮肤模型的相关性,在简要调查了早期模型之后,主要集中在脂质体上。考虑了不同类型脂质体的有效性,并将传统皮肤模型与囊泡模型膜作为皮肤膜模拟物的精度和准确性进行了比较。

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