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载有替莫泊芬的脂质体凝胶:粘弹性特性及体外皮肤渗透

Temoporfin-loaded liposomal gels: viscoelastic properties and in vitro skin penetration.

作者信息

Dragicevic-Curic Nina, Winter Sven, Stupar Mirjana, Milic Jela, Krajisnik Danina, Gitter Burkhard, Fahr Alfred

机构信息

Department of Pharmaceutical Technology, Friedrich Schiller University Jena, Lessingstrasse 8, 07743 Jena, Germany.

出版信息

Int J Pharm. 2009 May 21;373(1-2):77-84. doi: 10.1016/j.ijpharm.2009.02.010. Epub 2009 Feb 24.

DOI:10.1016/j.ijpharm.2009.02.010
PMID:19429291
Abstract

Temoporfin (mTHPC) is a potent second-generation photosensitizer. The primary object of this study was to develop a topical mTHPC-loaded liposomal hydrogel able to deliver mTHPC into the stratum corneum (SC) and deeper skin layers. This study was conducted (1) to determine the effect of carbomer concentration, used as a gelling agent, and the effect of phosphatidylcholine (PC) content of lecithin, used for the liposome preparation, on viscoelastic properties and viscosity of liposomal gels and (2) to determine the relationship between rheological properties of gels and the skin penetration of mTHPC. Liposomal hydrogels revealed plastic flow behaviour. The increase of carbomer concentration induced a domination of elastic over viscous behaviour of gels. There was an inverse relationship between the elasticity of gels and mTHPC-penetration. Viscosity also increased with the increment of carbomer concentration, reducing the mTHPC-penetration. Liposomal gels containing lecithin of smaller PC-content (i.e. smaller purity) exhibited a more elastic solid behaviour than gels containing lecithin with high PC-content, and showed smaller mTHPC-penetration. The gel containing 0.75%, w/w, carbomer and lecithin with high PC-content was considered to be the optimal formulation, since it delivered high amounts of mTHPC to the SC and deeper skin layers, and it possessed desirable rheological properties.

摘要

替莫泊芬(mTHPC)是一种强效的第二代光敏剂。本研究的主要目的是开发一种局部负载mTHPC的脂质体水凝胶,使其能够将mTHPC递送至角质层(SC)和更深的皮肤层。本研究旨在:(1)确定用作胶凝剂的卡波姆浓度以及用于制备脂质体的卵磷脂中磷脂酰胆碱(PC)含量对脂质体凝胶粘弹性和粘度的影响;(2)确定凝胶流变学性质与mTHPC皮肤渗透之间的关系。脂质体水凝胶呈现塑性流动行为。卡波姆浓度的增加导致凝胶的弹性行为超过粘性行为。凝胶弹性与mTHPC渗透之间存在反比关系。粘度也随卡波姆浓度的增加而增加,从而降低了mTHPC的渗透。含有较低PC含量(即较低纯度)卵磷脂的脂质体凝胶比含有高PC含量卵磷脂的凝胶表现出更具弹性的固体行为,并且mTHPC渗透较小。含有0.75%(w/w)卡波姆和高PC含量卵磷脂的凝胶被认为是最佳配方,因为它能将大量的mTHPC递送至SC和更深的皮肤层,并且具有理想的流变学性质。

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