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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >In situ-forming PLGA implants loaded with leuprolide acetate/-cyclodextrin complexes: mathematical modelling and degradation
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In situ-forming PLGA implants loaded with leuprolide acetate/-cyclodextrin complexes: mathematical modelling and degradation

机译：负载醋酸亮丙瑞林/环糊精复合物的原位形成PLGA植入物：数学建模和降解

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摘要

Drug release mechanism of in situ-forming implants (ISIs) based on poly(lactic acid-co-glycolic acid) (PLGA) loaded with leuprolide acetate/-cyclodextrin (LA/-CD) complexes via fitting with four diffusion-based semi-empirical models were studied. The release rate constants and release exponent of ISIs were calculated. The main drug release mechanism was Fickian diffusion. The LA diffusion coefficient and release constant were decreased via increasing the portion of -CD in complexes. The release curve was parabolic, with a higher initial slope and then consistent with the exponential. All ISIs containing LA/-CD complexes better fitted with the Korsmeyer-Peppas, Weibull and Peppas-Sahlin models rather than first-order model. Furthermore, the effect of LA/-CD complexation on the degradation of ISIs was studied through scanning electron microscopy (SEM). Results showed that hydrophilic nature of -CD facilitated the surface erosion of PLGA chains, however after 18 d, ISI-1/10 had still a proper structural strength, due to no hydrolytic degradation of -CD in this implant.
机译：基于聚乳酸-乙醇酸共聚物（PLGA）的原位形成植入物（ISI）的药物释放机理，通过配合四个基于扩散的半固态化合物，从而负载醋酸亮丙瑞林/环糊精（LA / -CD）复​​合物研究了经验模型。计算ISI的释放速率常数和释放指数。主要的药物释放机制是菲克扩散。通过增加复合物中-CD的比例，可降低LA扩散系数和释放常数。释放曲线是抛物线的，具有较高的初始斜率，然后与指数一致。所有包含LA / CD复合物的ISI都更适合Korsmeyer-Peppas，Weibull和Peppas-Sahlin模型，而不是一阶模型。此外，通过扫描电子显微镜（SEM）研究了LA / CD复合物对ISI降解的影响。结果表明，-CD的亲水性促进了PLGA链的表面腐蚀，但是在18 d后，由于该植入物中-CD没有水解降解，ISI-1 / 10仍具有适当的结构强度。

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