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用于超声调控药物释放的均匀聚合物偏心和核中心空心微胶囊的制备

Generation of uniform polymer eccentric and core-centered hollow microcapsules for ultrasound-regulated drug release.

作者信息

Huang Jingxian, Li Wanbo, Li Yan, Luo Chongdai, Zeng Yecheng, Xu Yuehong, Zhou Jianhua

机构信息

Biomedical Engineering Department, School of Engineering, Sun Yat-sen University, Guangzhou 510006, China.

出版信息

J Mater Chem B. 2014 Oct 21;2(39):6848-6854. doi: 10.1039/c4tb01050g. Epub 2014 Sep 5.

Abstract

In this paper, a strategy was developed for fabricating uniform polydimethylsiloxane (PDMS) microcapsules with eccentric and core-centered internal hollow structures, which can be employed as a novel controlled-release system for site-specific drug delivery under ultrasound regulation. This strategy involves the use of a microfluidic device, through which three phases (i.e., an inner water phase containing drug molecules, a middle oil phase of PDMS solution, and an outer water phase) were delivered at independently adjustable flow rates, allowing the formation of water-in-oil-in-water (W/O/W) emulsion droplets in a microfluidic device. After baking the as-prepared microcapsules, microcapsules with different inner hollow cores were obtained. The sizes of the inner hollow structures could be tuned, leading to a series of microcapsules with different densities. The densities of these microcapsules were all lower than that of water, which showed a long gastric residence time. Most interestingly, eccentric hollow microcapsules with well-controlled sizes and shapes were also prepared using this method. The eccentric and core-centered hollow microcapsules demonstrated triggered and controlled the release of encapsulation under ultrasound, for which the release profiles were consistent with the theoretical simulation. The results showed that the microcapsules had all the properties of a floating drug delivery system and controlled release system, and demonstrated great potential to be used for controlled release, in particular, for the delivery of drugs that are absorbed primarily in the upper segments of the gastrointestinal tract.

摘要

本文开发了一种制备具有偏心和核心居中内部中空结构的均匀聚二甲基硅氧烷(PDMS)微胶囊的策略,该微胶囊可作为一种新型的控释系统,用于在超声调控下进行特定部位的药物递送。该策略涉及使用微流控装置,通过该装置以独立可调的流速输送三相(即含有药物分子的内水相、PDMS溶液的中间油相和外水相),从而在微流控装置中形成水包油包水(W/O/W)乳液滴。对制备的微胶囊进行烘烤后,获得了具有不同内部中空核心的微胶囊。内部中空结构的尺寸可以调节,从而得到一系列具有不同密度的微胶囊。这些微胶囊的密度均低于水,这表明它们在胃中的滞留时间较长。最有趣的是,使用该方法还制备了尺寸和形状得到良好控制的偏心中空微胶囊。偏心和核心居中的中空微胶囊在超声作用下表现出触发和控制包封物释放的特性,其释放曲线与理论模拟结果一致。结果表明,这些微胶囊具备漂浮药物递送系统和控释系统的所有特性,并展现出用于控释的巨大潜力,特别是用于递送主要在胃肠道上段吸收的药物。

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