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药物在电纺麦醇溶蛋白纤维中的分布对药物释放行为的影响。

Influence of the drug distribution in electrospun gliadin fibers on drug-release behavior.

作者信息

Xu Ying, Li Jiao-Jiao, Yu Deng-Guang, Williams Gareth R, Yang Jun-He, Wang Xia

机构信息

School of Materials Science & Engineering, University of Shanghai for Science and Technology, Shanghai 200093, China.

School of Materials Science & Engineering, University of Shanghai for Science and Technology, Shanghai 200093, China.

出版信息

Eur J Pharm Sci. 2017 Aug 30;106:422-430. doi: 10.1016/j.ejps.2017.06.017. Epub 2017 Jun 11.

Abstract

Drug distribution within its carrier in a solid dosage form often generates a profound influence on its release profile, particularly when the physicochemical properties of the carrier are exploited to manipulate drug release behavior. In this job, two different types of distributions of a model drug ibuprofen (IBU) within a protein gliadin in their electrospun nanofibers were intentionally created. One was homogeneous distribution in the monolithic fibers fabricated using a modified coaxial process, and the other one was heterogeneous distribution in the core/shell fibers prepared through a traditional coaxial process. SEM observations clearly demonstrated the different distributions of IBU within gliadin in the two kinds of nanofibers although both of them had smooth surfaces and linear morphology. XRD results showed that IBU was amorphously distributed in the monolithic fibers, but that some IBU crystalline lattices presented in the core/shell fibers. FTIR and RM spectra suggested that gliadin had good compatibility with IBU. In vitro dissolution tests verified that the gliadin nanofibers with a heterogeneous drug distribution could provide a better sustained release profile than its counterpart in terms of initial burst release and sustained release time period. Both the fiber formation and drug-controlled release mechanisms are suggested. The present study demonstrated a concept that drug distribution with the medicated nanomaterials can be exploited as a tool to optimize the drug sustained release profile.

摘要

药物在固体剂型载体中的分布通常会对其释放曲线产生深远影响,尤其是当利用载体的物理化学性质来控制药物释放行为时。在本研究中,我们特意在电纺纳米纤维中的麦醇溶蛋白内创建了模型药物布洛芬(IBU)的两种不同分布类型。一种是在采用改进同轴工艺制备的整体纤维中均匀分布,另一种是在通过传统同轴工艺制备的核壳纤维中不均匀分布。扫描电子显微镜(SEM)观察清楚地表明,尽管两种纳米纤维表面均光滑且呈线性形态,但IBU在两种纳米纤维中的麦醇溶蛋白内的分布不同。X射线衍射(XRD)结果显示,IBU在整体纤维中呈无定形分布,但在核壳纤维中存在一些IBU晶格。傅里叶变换红外光谱(FTIR)和拉曼光谱(RM)表明,麦醇溶蛋白与IBU具有良好的相容性。体外溶出试验证实,药物分布不均匀的麦醇溶蛋白纳米纤维在初始突释和缓释时间段方面比其对应物能提供更好的缓释曲线。同时提出了纤维形成和药物控释机制。本研究证明了一个概念,即药物在含药纳米材料中的分布可作为优化药物缓释曲线的一种手段。

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