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胆固醇封端的聚(丙烯酸)的易掺入化用于脂质体的简易表面修饰。

Labile Incorporation of Cholesterol-Terminated Poly(acrylic acid) for the Facile Surface-Modification of Lipid Vesicles.

机构信息

Department of Chemistry, The Catholic University of Korea , Bucheon, Gyeonggi-do 14662, Korea.

出版信息

Langmuir. 2017 Jul 11;33(27):6751-6759. doi: 10.1021/acs.langmuir.7b00670. Epub 2017 Jun 26.

Abstract

An amphiphilic cholesterol-terminated poly[acrylic acid] (Chol-PAA) that can be self-aggregated into nanoscale micelles in aqueous media has been prepared via nitroxide-mediated radical polymerization for the facile postformation modification of lipid vesicles. By varying the amount of Chol-PAA addition, the incorporation of Chol-PAA on the liposome templates was verified with zeta potential while the dynamic light scattering measurements revealed the polymer length of Chol-PAA dictated the hydrodynamic diameter of the resulting polymer-grafted vesicles (PGVs). The membrane incorporation process of Chol-PAA was monitored through the fluorescence resonance energy transfer (FRET) study, which showed the relatively labile incorporation property of Chol-PAA, compared to the cholesterol-free PAA and the native cholesterol. Additionally, the postmodification of liposomes with such labile Chol-PAA exhibited a negligible leakage of calcein payloads, which can be attributed to the partial modification of the external membrane. These results indicated that our Chol-PAA can be exploited for the facile construction of functional polymer-decorated liposomal delivery systems.

摘要

一种两亲性的胆固醇封端的聚(丙烯酸)(Chol-PAA)可以通过氮氧自由基聚合在水介质中自组装成纳米级胶束,便于脂质体的后期形成修饰。通过改变 Chol-PAA 的添加量,通过电泳测量证实了 Chol-PAA 在脂质体模板上的掺入,而动态光散射测量则揭示了 Chol-PAA 的聚合物长度决定了所得聚合物接枝囊泡(PGV)的水动力直径。通过荧光共振能量转移(FRET)研究监测 Chol-PAA 的膜掺入过程,结果表明与无胆固醇的 PAA 和天然胆固醇相比,Chol-PAA 的掺入性质相对不稳定。此外,这种不稳定的 Chol-PAA 对脂质体的后期修饰表现出几乎没有 calcein 有效负载的泄漏,这可以归因于外膜的部分修饰。这些结果表明,我们的 Chol-PAA 可以用于简便地构建功能性聚合物修饰的脂质体给药系统。

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