关于喷雾干燥PLGA微球的突发释放动力学的新见解
Kyprianos Michaelides1, Mohamad Anas Al Tahan1, Yundong Zhou2
1School of Pharmacy, Aston University, Birmingham B4 7ET, U.K.
Molecular pharmaceutics
|October 25, 2024
概括
聚-乳糖-糖酸) 微球的喷雾干燥会导致活性药物成分 (API) 的突发释放,这是由于蛋白质分布在表面附近. 一个PLGA表面层有助于在注射配方中过早释放API.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 生物技术是生物技术.
背景情况:
- 喷雾干燥是生产活性药物成分 (API) 微球以控制释放的关键方法.
- 基于聚乳糖糖酸 (PLGA) 的注射剂面临着药物过早释放的挑战,称为突发释放.
- 这种突发释放会对长效注射配方的疗效和质量产生负面影响.
研究的目的:
- 为了确定喷雾干燥的PLGA微球中爆破释放的主要来源.
- 为了研究配方变量对爆发释放动力学的影响.
- 了解微球特征在过早的API释放中的作用.
主要方法:
- 喷雾干燥微球的特性 (BSA/PLGA比) 形态,颗粒大小,表面积,热性能和组成.
- 利用X射线光电子光谱 (XPS) 和飞行时间二次离子质谱 (ToF-SIMS) 进行表面和深度分析.
- 研究了微球特性与牛血清白蛋白 (BSA) 释放概况之间的相关性.
主要成果:
- 观察到高初始释放 (85%) 的BSA,归因于蛋白质接近微球表面.
- 表面分析揭示了微球上富含PLGA的层,其中BSA嵌入更深处.
- 虽然颗粒大小和表面积因配方而异,但它们并没有显著改变整体爆破释放配置.
结论:
- 在PLGA微球中爆发释放现象主要是由表面PLGA层的降解和孔隙形成引起的.
- 这一表面层促进了API的快速扩散,导致过早释放.
- 缓解爆破释放的策略需要解决喷雾干燥微球的表面特征.
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