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载他莫昔芬羟丙甲纤维素/聚丙烯腈复合纤维的制备及性能表征。

Preparation and characterization of TAM-loaded HPMC/PAN composite fibers for improving drug-release profiles.

机构信息

College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Songjiang District, Shanghai, P R China.

出版信息

J Biomater Sci Polym Ed. 2011;22(16):2227-40. doi: 10.1163/092050610X538182. Epub 2010 Nov 17.

Abstract

The present paper reports the preparation and characterization of composite hydroxypropyl methylcellulose/polyacrylonitrile (HPMC/PAN)-medicated fibers via a wet spinning technique. Tamoxifen (TAM) was selected as a model drug. Numerous analyses were conducted to characterize the mechanical, structure and morphology properties of the composite fibers. The drug content and in vitro dissolution behavior were also investigated. SEM images showed that the TAM-loaded HPMC/PAN composite fibers had a finger-like outer skin and a porous structure. FT-IR spectra demonstrated that there was a good compatibility between polymer and drug. Results from X-ray diffraction and DSC suggested that most of the incorporated TAM was evenly distributed in the fiber matrix in an amorphous state, except for a minority that aggregated on the surface of fibers. The drug content in the fibers was lower than that in the spinning solution and about 10% of TAM was lost during spinning process. In vitro dissolution results indicated that, compared to TAM-PAN fibers, HPMC/PAN composite systems had weaker initial burst release effects and more drug-loading. The combination of hydrophilic polymer HPMC with PAN could improve the performance of polymer matrix composite fibers in regulating the drug-release profiles.

摘要

本文报道了通过湿法纺丝技术制备和表征羟丙基甲基纤维素/聚丙烯腈(HPMC/PAN)载药复合纤维。选择他莫昔芬(TAM)作为模型药物。对复合纤维的力学、结构和形态性能进行了大量分析。还研究了药物含量和体外释放行为。SEM 图像表明,载 TAM 的 HPMC/PAN 复合纤维具有指状外皮和多孔结构。FT-IR 谱表明聚合物和药物之间具有良好的相容性。X 射线衍射和 DSC 的结果表明,大部分掺入的 TAM 以无定形状态均匀分布在纤维基质中,只有少数聚集在纤维表面。纤维中的药物含量低于纺丝溶液中的药物含量,且在纺丝过程中约有 10%的 TAM 损失。体外释放结果表明,与 TAM-PAN 纤维相比,HPMC/PAN 复合体系具有较弱的初始突释效应和更高的载药量。亲水性聚合物 HPMC 与 PAN 的结合可以改善聚合物基质复合纤维调节药物释放曲线的性能。

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