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聚离子复合胶束的制备、表征及药物释放行为

Preparation, characterization and drug release behavior of polyion complex micelles.

作者信息

Luo Yali, Wang Airong, Yuan Jinfang, Gao Qingyu

机构信息

Institute of Fine Chemical and Engineering, Henan University, Kaifeng, PR China.

出版信息

Int J Pharm. 2009 Jun 5;374(1-2):139-44. doi: 10.1016/j.ijpharm.2009.03.019. Epub 2009 Mar 24.

Abstract

Double-hydrophilic block copolymer composed of poly(N-vinylpyrrolidone) (PVP) and poly(styrene-alter-maleic anhydride) (PSMA) has been synthesized by reversible addition-fragmentation chain transfer (RAFT) polymerization. Poly(N-vinylpyrrolidone)-block-poly(styrene-alter-maleic anhydride) (PVP-b-PSMA) thus formed was characterized by gel permeation chromatography (GPC), (1)H nuclear magnetic resonance ((1)H NMR) spectroscopy and FTIR spectroscopy. In acid solution, this block copolymer spontaneously formed polyion complex (PIC) micelles with a cationic polyelectrolyte, chitosan. The PSMA/chitosan polyelectrolyte complex formed an inner core while PVP chains surrounded it as a shell. Transmission electron micrographs (TEMs) and dynamic light scattering (DLS) showed the PIC micelles to be spherically shaped, with mean hydrodynamic diameter around 146 nm. The model drug coenzyme A (CoA) was loaded into the micelles and the in vitro drug release behavior was investigated. We found that by manipulating the pH value and salt concentration of the release solution, it was possible to control the releasing rate of CoA.

摘要

由聚(N-乙烯基吡咯烷酮)(PVP)和聚(苯乙烯-alt-马来酸酐)(PSMA)组成的双亲水嵌段共聚物已通过可逆加成-断裂链转移(RAFT)聚合反应合成。由此形成的聚(N-乙烯基吡咯烷酮)-嵌段-聚(苯乙烯-alt-马来酸酐)(PVP-b-PSMA)通过凝胶渗透色谱(GPC)、氢核磁共振(¹H NMR)光谱和傅里叶变换红外光谱(FTIR)进行表征。在酸性溶液中,这种嵌段共聚物与阳离子聚电解质壳聚糖自发形成聚离子复合物(PIC)胶束。PSMA/壳聚糖聚电解质复合物形成内核,而PVP链作为外壳围绕着它。透射电子显微镜(TEM)和动态光散射(DLS)显示PIC胶束呈球形,平均流体动力学直径约为146 nm。将模型药物辅酶A(CoA)载入胶束并研究其体外药物释放行为。我们发现,通过控制释放溶液的pH值和盐浓度,可以控制CoA的释放速率。

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