Release mechanisms of tacrolimus-loaded PLGA and PLA microspheres and immunosuppressive effects of the microspheres in a rat heart transplantation model
作者： Ryo Kojima , Takatsune Yoshida , Hiroaki Tasaki , Hiroyuki Umejima , Masashi Maeda
DOI: 10.1016/J.IJPHARM.2015.07.004
关键词: Polylactic acid 、 Transplantation 、 Absorption (skin) 、 Drug 、 Tacrolimus 、 Chemistry 、 Pharmacology 、 Controlled release 、 PLGA 、 Pharmacokinetics
摘要: The objective of this study was to elucidate the release and absorption mechanisms tacrolimus loaded into microspheres composed poly(lactic-co-glycolic acid) (PLGA) and/or polylactic acid (PLA). Tacrolimus-loaded were prepared by o/w emulsion solvent evaporation method. entrapment efficiency correlated with molecular weight PLGA, glass transition temperature PLGA not decreased addition tacrolimus. These results indicate that intermolecular interaction between polymer would affect in microspheres. Tacrolimus released loss microspheres, dominant mechanism considered be erosion rather than diffusion drug. whole-blood concentration rats maintained for at least 2 weeks after a single subcutaneous administration pharmacokinetic profile following similar intramuscular administration, suggesting dissolution tacrolimus, dissolved rate-limiting steps. Graft-survival time heart transplantation rat model prolonged tacrolimus-loaded microsphere formulation expected precisely control blood while maintaining immunosuppressive effect
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