Core/shell PLGA microspheres with controllable in vivo release profile via rational core phase design

作者：Meiling Yu, Qing Yao, Yan Zhang, Huilin Chen, Haibing He, Yu Zhang, Tian Yin, Xing Tang, Hui Xu · 发表于：Artificial Cells Nanomedicine and Biotechnology · 年份：2018 · DOI：10.1080/21691401.2018.1443940 · 被引用次数：24 · 研究领域：Advanced Drug Delivery Systems、Drug Solubulity and Delivery Systems、Nanoparticle-Based Drug Delivery

Highly soluble drugs tend to release from preparations at high speeds, which make them need to be taken at frequent intervals. Additionally, some drugs need to be controlled to release in vivo at certain periods, so as to achieve therapeutic effects. Thus, the objective of this study is to design injectable microparticulate systems with controllable in vivo release profile. Biodegradable PLGA was used as the matrix material to fabricate microspheres using the traditional double emulsification-solvent evaporation method as well as improved techniques, with gel (5% gelatine or 25% F127) or LP powders as the inner phases. Their physicochemical properties were systemically investigated. Microspheres prepared by modified methods had an increase in drug loading (15.50, 16.72, 15.66%, respectively) and encapsulation efficiencies (73.46, 79.42, 74.40%, respectively) when compared with traditional methods (12.01 and 57.06%). The morphology of the particles was characterized by optical microscope (OM) and scanning electron microscopy (SEM), and the amorphous nature of the encapsulated drug was confirmed by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. To evaluate their release behaviour, the in vitro degradation, in vitro release and in vivo pharmacodynamics were subsequently studied. Traditional microspheres prepared in this study with water as the inner phase had a relatively short release period within 16 d when compared with modified microspheres wit...