周围的水凝胶可减缓 PLGA 微颗粒的药物释放速度

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY
L.A. Lefol , P. Bawuah , J.A. Zeitler , J. Verin , F. Danede , J.F. Willart , F. Siepmann , J. Siepmann
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引用次数: 0

摘要

本研究旨在评估和更好地了解周围一层水凝胶(模拟活组织)对 PLGA 微颗粒药物释放的潜在影响。采用乳液溶剂萃取/蒸发法制备了布洛芬负载微颗粒。药物负载量约为 48%。微颗粒表面最初看起来光滑无孔。相比之下,微粒内部的微观结构则呈现出连续的微孔网络。在琼脂糖凝胶和充分搅拌的 pH 值为 7.4 的磷酸盐缓冲液中测量了单个微颗粒的布洛芬释放量。光学显微镜、扫描电子显微镜、差示扫描量热法、X 射线粉末衍射和 X 射线 μCT 成像被用来描述微颗粒在暴露于释放介质前后的特性。重要的是,布洛芬的释放在周围有琼脂糖凝胶的情况下要慢得多,例如,完全释放需要两周时间,而在搅拌良好的磷酸盐缓冲液中只需要几天。这可能是由于水凝胶在立体上阻碍了系统的大幅度膨胀,从而减缓了药物流动性的相关增长。此外,在这种特殊情况下,搅拌的散装液体中的对流可能会破坏微颗粒表面的 PLGA 薄层,使外部水相更快地进入内部连续孔隙网络:一旦与水接触,药物就会溶解,并通过充满水的连续孔道网络迅速扩散出去。如果不能直接进入微粒表面,大部分药物就只能 "等待 "系统发生实质性膨胀时才能释放出来。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Drug release from PLGA microparticles can be slowed down by a surrounding hydrogel

Drug release from PLGA microparticles can be slowed down by a surrounding hydrogel

This study aimed to evaluate and better understand the potential impact that a layer of surrounding hydrogel (mimicking living tissue) can have on the drug release from PLGA microparticles. Ibuprofen-loaded microparticles were prepared with an emulsion solvent extraction/evaporation method. The drug loading was about 48%. The surface of the microparticles appeared initially smooth and non-porous. In contrast, the internal microstructure of the particles exhibited a continuous network of tiny pores. Ibuprofen release from single microparticles was measured into agarose gels and well-agitated phosphate buffer pH 7.4. Optical microscopy, scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction, and X-ray μCT imaging were used to characterize the microparticles before and after exposure to the release media. Importantly, ibuprofen release was much slower in the presence of a surrounding agarose gel, e.g., the complete release took two weeks vs. a few days in well agitated phosphate buffer. This can probably be attributed to the fact that the hydrogel sterically hinders substantial system swelling and, thus, slows down the related increase in drug mobility. In addition, in this particular case, the convective flow in agitated bulk fluid likely damages the thin PLGA layer at the microparticles' surface, giving the outer aqueous phase more rapid access to the inner continuous pore network: Upon contact with water, the drug dissolves and rapidly diffuses out through a continuous network of water-filled channels. Without direct surface access, most of the drug “has to wait” for the onset of substantial system swelling to be released.

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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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