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How to circumvent untoward drug crystallization during emulsion-templated microencapsulation process

机译:在乳液模板微囊化过程中如何避免不良的药物结晶

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Unwanted drug crystals often form on the surface of PLGA microspheres or in an aqueous phase when a hydrophobic drug undergoes emulsion-templated microencapsulation processes. In our study, over 70% of progesterone crystallizes in the aqueous phase when microencapsulation proceeds with a typical oil-in-water solvent evaporation process. During filtration employed for microsphere recovery, unentrapped drug crystals are collected alongside with progesterone-containing microspheres. This phenomenon accompanies unfavorable consequences on the microsphere quality. In contrast, when microspheres are prepared with a new solvent extraction-evaporation hybrid process, it is possible to completely avoid drug crystallization. Consequently, the new microencapsulation technique yields high drug encapsulation efficiencies of >= 90.8%, and the resultant microspheres show a homogeneous size distribution pattern. Also, the microsphere surface is free of drug crystals. For loading hydrophobic drugs into PLGA microspheres, the new microencapsulation process reported in this study has distinct advantages over commonly used emulsion-templated solvent evaporation processes. (C) 2016 Wiley Periodicals, Inc.
机译:当疏水药物经历乳液模板微囊化过程时,有害的药物晶体通常会在PLGA微球表面或水相中形成。在我们的研究中,当微囊化与典型的水包油溶剂蒸发过程一起进行时,超过70%的孕酮在水相中结晶。在用于微球回收的过滤过程中,未捕获的药物晶体与含孕酮的微球一起被收集。这种现象伴随着对微球质量的不利影响。相反,当用新的溶剂萃取-蒸发混合工艺制备微球时,可以完全避免药物结晶。因此,新的微囊化技术可产生> = 90.8%的高药物囊化效率,并且所得微球显示出均一的尺寸分布模式。而且,微球表面没有药物晶体。为了将疏水性药物装载到PLGA微球中,本研究中报道的新微囊化工艺比通常使用的乳液模板溶剂蒸发工艺具有明显优势。 (C)2016威利期刊公司

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