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Three months extended-release microspheres prepared by multi-microchannel microfluidics in beagle dog models
International Journal of Pharmaceutics ( IF 5.8 ) Pub Date : 2021-08-24 , DOI: 10.1016/j.ijpharm.2021.121039
Ju Hee Kim 1 , Choong Ho Ryu 1 , Chan Hee Chon 1 , Seyeon Kim 1 , Sangno Lee 1 , Ravi Maharjan 2 , Nam Ah Kim 2 , Seong Hoon Jeong 2
Affiliation  

To evaluate in vivo drug release profiles in beagle dogs, finasteride-loaded PLGA microspheres were prepared using a novel method of IVL-PPF Microsphere® microfluidic device. Briefly, the dispersed phase (PLGA and finasteride in dichloromethane) was mixed with the continuous phase (0.25% w/v PVA aqueous solution) in the parallelized microchannels. After lyophilization, the diameter of the microspheres was around 40 μm (PLGA 7502A or 5002A) and around 30 µm (PLGA/PLA02A mixture). Their CV and span values suggested a narrow size distribution in repeated batch preparations. The in vivo drug release from the PLGA microspheres exhibited three substantial phases: an initial burst, a moderate release, and then a plateau. The microspheres based on PLGA 7502A (75:25 co-polymer) demonstrated extended drug release for around 1 month with a minimized initial burst release compared to PLGA 5002A (50:50 co-polymer). Moreover, the in vivo drug release profile in beagle dogs was proportionally related to the amount of drug loading. Furthermore, the addition of PLA02A into the fabrication of the microsphere synergistically extended the drug release up to 3 months. These results demonstrated the value of this method to achieve uniform microspheres and extend the drug release properties with interpretative in vivo PK profiles.



中文翻译:

比格犬模型中多微通道微流体制备的三个月缓释微球

为了评估比格犬的体内药物释放曲线,使用 IVL-PPF Microsphere® 微流体装置的新方法制备了负载非那雄胺的 PLGA 微球。简而言之,分散相(PLGA 和非那雄胺在二氯甲烷中)与连续相(0.25% w/v PVA 水溶液)在平行微通道中混合。冻干后,微球的直径约为 40 μm(PLGA 7502A 或 5002A)和约 30 μm(PLGA/PLA02A 混合物)。它们的 CV 和跨度值表明在重复批次制备中粒径分布较窄。在体内PLGA 微球的药物释放表现出三个基本阶段:初始爆发、适度释放和平台期。与 PLGA 5002A(50:50 共聚物)相比,基于 PLGA 7502A(75:25 共聚物)的微球表现出持续约 1 个月的药物缓释,并具有最小的初始突释。此外,比格犬的体内药物释放曲线与载药量成正比。此外,在微球的制造中加入 PLA02A 协同延长药物释放长达 3 个月。这些结果证明了该方法在获得均匀的微球和扩展具有解释性体内PK 曲线的药物释放特性方面的价值。

更新日期:2021-09-13
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