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

Glycerosomes: Use of hydrogenated soy phosphatidylcholine mixture and its effect on vesicle features and diclofenac skin penetration
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DOI:
10.1016/j.ijpharm.2016.07.009
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发表时间:
2016-09-10
影响因子:
5.8
通讯作者:
Manconi, Maria
Manconi, Maria
中科院分区:
医学2区
文献类型:
--
作者:
Manca, Maria Letizia;Cencetti, Claudia;Manconi, Maria

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在这项工作中,双氯芬酸以钠盐的形式被包裹在水相中含有10%、20%或30%甘油的甘油微体中,目的是改善其局部疗效。考虑到以前的研究结果,甘油体配方在经济适宜性方面进行了修改,使用了一种廉价且可在市场上买到的氢化大豆磷脂酰胆碱(P90H)混合物。P90H甘油体呈球形和多层状;光子相关光谱显示所获得的囊泡与二棕榈酰磷脂酰胆碱(DPPC)制备的囊泡相似,略大,分散程度更高,但令人惊讶的是,它们能够改善双氯芬酸的局部给药,这比以前的发现有所改善,特别是使用甘油含量较高(20%和30%)的甘油体。最后,该给药系统对人角质形成细胞表现出较高的体外生物相容性。(C)2016爱思唯尔B.V.保留所有权利。
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 similar to 131 nm, 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. (C) 2016 Elsevier B.V. All rights reserved.