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用于透皮给药的传递体

Transfersomes for transdermal drug delivery.

作者信息

Benson Heather A E

机构信息

Curtin University of Technology, School of Pharmacy, Perth, WA 6845, Australia.

出版信息

Expert Opin Drug Deliv. 2006 Nov;3(6):727-37. doi: 10.1517/17425247.3.6.727.

Abstract

Transfersomes (Idea AG) are a form of elastic or deformable vesicle, which were first introduced in the early 1990s. Elasticity is generated by incorporation of an edge activator in the lipid bilayer structure. The original composition of these vesicles was soya phosphatidyl choline incorporating sodium cholate and a small concentration of ethanol. Transfersomes are applied in a non-occluded method to the skin and have been shown to permeate through the stratum corneum lipid lamellar regions as a result of the hydration or osmotic force in the skin. They have been used as drug carriers for a range of small molecules, peptides, proteins and vaccines, both in vitro and in vivo. It has been claimed by Idea AG that intact Transfersomes penetrate through the stratum corneum and the underlying viable skin into the blood circulation. However, this has not been substantiated by other research groups who have extensively probed the mechanism of penetration and interaction of elastic vesicles in the skin. Structural changes in the stratum corneum have been identified, and intact elastic vesicles visualised within the stratum corneum lipid lamellar regions, but no intact vesicles have been ascertained in the viable tissues. Using the principle of incorporating an edge-activator agent into a bilayer structure, a number of other elastic vesicle compositions have been evaluated. This review describes the research into the development and evaluation of Transfersomes and elastic vesicles as topical and transdermal delivery systems.

摘要

传递体(Idea AG公司)是一种弹性或可变形囊泡,于20世纪90年代初首次被引入。弹性是通过在脂质双层结构中加入边缘活化剂而产生的。这些囊泡的原始成分是含有胆酸钠和低浓度乙醇的大豆磷脂酰胆碱。传递体以非封闭方式应用于皮肤,并且由于皮肤中的水合作用或渗透力已被证明可透过角质层脂质层区域。它们已被用作一系列小分子、肽、蛋白质和疫苗的药物载体,包括体外和体内应用。Idea AG公司宣称完整的传递体可穿透角质层和下面的活皮肤进入血液循环。然而,其他广泛探究弹性囊泡在皮肤中的渗透和相互作用机制的研究小组并未证实这一点。已确定角质层的结构变化,并在角质层脂质层区域内观察到完整的弹性囊泡,但在活组织中未确定有完整的囊泡。利用将边缘活化剂加入双层结构中的原理,已评估了许多其他弹性囊泡组合物。本综述描述了作为局部和透皮给药系统的传递体和弹性囊泡的开发与评估研究。

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