Comparative studies on the properties of glycyrrhetinic acid-loaded PLGA microparticles prepared by emulsion and template methods.
Comparative studies on the properties of glycyrrhetinic acid-loaded PLGA microparticles prepared by emulsion and template methods.
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乳液法与模板法制备的甘草次酸PLGA微粒性能对比研究
DOI：
10.1016/j.ijpharm.2015.11.018
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发表时间：
2015
影响因子：
5.8
通讯作者：
Wang,Wenping
中科院分区：
文献类型：
--
作者：
Wang,Hong;Zhang,Guangxing;Sui,Hong;Liu,Yanhua;Park,Kinam;Wang,Wenping
O/W乳液法已被广泛用于生产聚（丙交酯-共-乙交酯）（PLGA）微粒。最近，模板方法已被用于制备具有预定尺寸和形状的均匀微粒，并显示出可用于包封不同类型的活性化合物。然而，模板法和乳液法之间的差异尚未得到检验。本研究以大黄酸为模型药物，采用两种方法制备PLGA微粒。对所得微粒的药物分布、体外释放和降解性能进行了表征和比较。两种方法的包封率均在70%以上，平均粒径约为40 μm。DSC热分析和XRPD衍射图表明GA在微粒基体中高度分散或以无定形状态存在。乳液方法产生具有核-壳型结构和每个微粒内的许多富含药物的域的宽尺寸分布的微粒。其药物释放和基质降解在50天前缓慢，然后加速。相比之下，模板法形成的微粒具有窄的尺寸分布和药物分布，没有明显的药物富集域。载药率为85%的模板微球在突释26.7%后3个月内仍保持零级释放，并有稳定的表面溶蚀过程。由两种不同方法制备的相同微粒显示出两种不同的药物释放曲线。这两种不同的方法可以相互补充，优化药物制剂，以实现预定的药物释放模式。
The O/W emulsion method has been widely used for the production of poly (lactide-co-glycolide) (PLGA) microparticles. Recently, a template method has been used to make homogeneous microparticles with predefined size and shape, and shown to be useful in encapsulating different types of active compounds. However, differences between the template method and emulsion method have not been examined. In the current study, PLGA microparticles were prepared by the two methods using glycyrrhetinic acid (GA) as a model drug. The properties of obtained microparticles were characterized and compared on drug distribution,in vitrorelease, and degradation. An encapsulation efficiency of over 70% and a mean particle size of about 40 μm were found for both methods. DSC thermograms and XRPD diffractograms indicated that GA was highly dispersed or in the amorphous state in the matrix of microparticles. The emulsion method produced microparticles of a broad size distribution with a core–shell type structure and many drug-rich domains inside each microparticle. Its drug release and matrix degradation was slow before Day 50 and then accelerated. In contrast, the template method formed microparticles with narrow size distribution and drug distribution without apparent drug-rich domains. The template microparticles with a loading efficiency of 85% exhibited a zero-order release profile for 3 months after the initial burst release of 26.7%, and a steady surface erosion process as well. The same microparticles made by two different methods showed two distinguished drug release profiles. The two different methods can be supplementary with each other in optimization of drug formulation for achieving predetermined drug release patterns.