Abstract

Aim

This study aimed for a detailed understanding of the impact of different process parameters involved during celecoxib-loaded microsphere preparation based on propylene carbonate emulsion-precursors.

Methods

Microspheres were prepared by a modified emulsification-solvent extraction method. Performed investigations included polymer solubility and viscosity, microsphere size, morphology and stability, propylene carbonate content as well as celecoxib solid state, content and release.

Results

Rough-walled round microspheres with sizes between 21 µm and 122 µm and an internal sponge-like structure filled with residual propylene carbonate (content between 1.9 ± 0.1% and 6.7 ± 0.5% w/w) were obtained. Encapsulation efficiencies varied between 28.3 ± 0.1% and 66.8 ± 1.0%. The release rates were affected by the polymer concentration, the emulsion phase ratio and the residual propylene carbonate content (t_50% varied between 2.2 hours and 23.4 hours).

Conclusions

This study identified the most relevant process parameters for this new preparation method for the model drug celecoxib.

中文翻译：

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基于碳酸丙烯酯乳液前驱体的微球制备工艺参数[J].

摘要

目的

本研究旨在详细了解基于碳酸丙烯酯乳液前体的塞来昔布微球制备过程中涉及的不同工艺参数的影响。

方法

采用改良的乳化-溶剂萃取法制备微球。进行的研究包括聚合物溶解度和粘度、微球尺寸、形态和稳定性、碳酸丙烯酯含量以及塞来昔布固态、含量和释放。

结果

获得了尺寸在 21 µm 和 122 µm 之间的粗糙壁圆形微球和填充有残留碳酸亚丙酯（含量在 1.9 ± 0.1% 和 6.7 ± 0.5% w/w 之间）的内部海绵状结构。封装效率在 28.3 ± 0.1% 和 66.8 ± 1.0% 之间变化。释放速率受聚合物浓度、乳液相比和残留碳酸亚丙酯含量的影响（t _50%在 2.2 小时和 23.4 小时之间变化）。

结论

本研究为模型药物塞来昔布的这种新制备方法确定了最相关的工艺参数。