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甘油脂质体:氢化大豆磷脂酰胆碱混合物的应用及其对囊泡特性和双氯芬酸皮肤渗透的影响。

Glycerosomes: Use of hydrogenated soy phosphatidylcholine mixture and its effect on vesicle features and diclofenac skin penetration.

作者信息

Manca Maria Letizia, Cencetti Claudia, Matricardi Pietro, Castangia Ines, Zaru Marco, Sales Octavio Diez, Nacher Amparo, Valenti Donatella, Maccioni Anna Maria, Fadda Anna Maria, Manconi Maria

机构信息

Dept. Scienze della Vita e dell'Ambiente, Drug Science Division, University of Cagliari, 09124 Cagliari, Italy.

Dept. Chemistry and Drug Technologies, Sapienza, University of Roma, Roma, Italy.

出版信息

Int J Pharm. 2016 Sep 10;511(1):198-204. doi: 10.1016/j.ijpharm.2016.07.009. Epub 2016 Jul 12.

Abstract

In this work, diclofenac was encapsulated, as sodium salt, in glycerosomes containing 10, 20 or 30% of glycerol in the water phase with the aim to ameliorate its topical efficacy. Taking into account previous findings, glycerosome formulation was modified, in terms of economic suitability, using a cheap and commercially available mixture of hydrogenated soy phosphatidylcholine (P90H). P90H glycerosomes were spherical and multilamellar; photon correlation spectroscopy showed that obtained vesicles were ∼131nm, slightly larger and more polydispersed than those made with dipalmitoylphosphatidylcholine (DPPC) but, surprisingly, they were able to ameliorate the local delivery of diclofenac, which was improved with respect to previous findings, in particular using glycerosomes containing high amount of glycerol (20 and 30%). Finally, this drug delivery system showed a high in vitro biocompatibility toward human keratinocytes.

摘要

在这项工作中,双氯芬酸以钠盐形式被包封在水相中甘油含量为10%、20%或30%的脂质体中,目的是改善其局部疗效。考虑到先前的研究结果,从经济适用性方面对脂质体制剂进行了改进,使用了一种廉价且市售的氢化大豆磷脂酰胆碱(P90H)混合物。P90H脂质体呈球形且为多层结构;光子相关光谱显示,所获得的囊泡约为131nm,比用二棕榈酰磷脂酰胆碱(DPPC)制备的囊泡稍大且多分散性更高,但令人惊讶的是,它们能够改善双氯芬酸的局部递送,相对于先前的研究结果有所改善,特别是使用含有大量甘油(20%和30%)的脂质体时。最后,该药物递送系统对人角质形成细胞表现出高度的体外生物相容性。

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