Electrospray synthesis and properties of hierarchically structured PLGA TIPS microspheres for use as controlled release technologies
Electrospray synthesis and properties of hierarchically structured PLGA TIPS microspheres for use as controlled release technologies
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DOI：
10.1016/j.jcis.2016.01.021
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发表时间：
2016-04-01
影响因子：
9.9
通讯作者：
Day, Richard M.
中科院分区：
文献类型：
--
作者：
Malik, Salman A.;Ng, Wing H.;Day, Richard M.
基于微球的控释技术已被用于蛋白质、肽和抗生素的长期递送，尽管由于制剂复杂性、缺乏可扩展性和成本，它们的合成带来了巨大的挑战。为了解决这些缺点，我们使用电喷雾工艺作为可再现的合成技术来制造高度多孔（>94%）的微球，同时保持对颗粒结构和尺寸的控制。在这里，我们报告了一个成功的配方用于产生球形聚（乳酸-羟基乙酸）共聚物（PLGA）微球使用电喷雾（ES）结合具有定制液氮（LN 2）收集方案的新型热致相分离（TIPS）过程。我们展示了如何大小，所得微球的形状和孔隙率可以通过明智地改变电喷雾处理参数来控制，其粒度（和孔隙率）影响释放动力学。通过扫描电镜、共聚焦拉曼显微镜、热重分析和压汞法表征了电喷雾处理对颗粒的影响及其物理化学性质。这里制造的微球已经成功地证明了活性剂的长期递送（即1周），使得能够以最小的物理降解持续释放染料，并且已经验证了可扩展的电喷雾技术用于创新的基于TIPS的微球生产方案的潜力。(C)2016年6月，作者。爱思唯尔公司出版这是一篇在CC BY许可证下的开放获取文章（http：//creativecommons.org/licenses/by/4.0/）。
Microsphere-based controlled release technologies have been utilized for the long-term delivery of proteins, peptides and antibiotics, although their synthesis poses substantial challenges owing to formulation complexities, lack of scalability, and cost. To address these shortcomings, we used the electrospray process as a reproducible, synthesis technique to manufacture highly porous (>94%) microspheres while maintaining control over particle structure and size. Here we report a successful formulation recipe used to generate spherical poly(lactic-co-glycolic) acid (PLGA) microspheres using the electrospray (ES) coupled with a novel thermally induced phase separation (TIPS) process with a tailored Liquid Nitrogen (LN2) collection scheme.We show how size, shape and porosity of resulting microspheres can be controlled by judiciously varying electrospray processing parameters and we demonstrate examples in which the particle size (and porosity) affect release kinetics. The effect of electrospray treatment on the particles and their physicochemical properties are characterized by scanning electron microscopy, confocal Raman microscopy, thermogravimetric analysis and mercury intrusion porosimetry. The microspheres manufactured here have successfully demonstrated long-term delivery (i.e. 1 week) of an active agent, enabling sustained release of a dye with minimal physical degradation and have verified the potential of scalable electrospray technologies for an innovative TIPS-based microsphere production protocol. (C) 2016 The Authors. Published by Elsevier Inc. This is an open access article under the CC BY license (http:// creativecommons.org/licenses/by/4.0/).