聚合物囊泡
PLGA公司
内吞作用
泊洛沙姆
化学
胰岛素
胞饮病
内化
生物物理学
药理学
体外
细胞生物学
生物化学
受体
医学
内分泌学
生物
共聚物
两亲性
聚合物
有机化学
作者
Shuang Xie,Yan Gong,Xiangyuan Xiong,Zi L Li,Yue Luo,Yu P Li
出处
期刊:Nanomedicine
日期:2018-10-01
卷期号:13 (19): 2527-2544
被引量:23
标识
DOI:10.2217/nnm-2017-0372
摘要
Aim: To explore the better efficacy of targeted folic acid (FA)-Pluronic 85-poly(lactide-co-glycolide) (FA–P85–PLGA) polymersome in oral insulin delivery. Materials & methods: The cytotoxicity of the polymers, in vitro qualitative and quantitative cellular uptake and the internalization mechanism of insulin-loaded FA–P85–PLGA and PLGA–P85–PLGA polymersomes were studied with the human colon adenocarcinoma cells (Caco-2 cells). Their pharmacodynamics and pharmacokinetics properties were also studied with diabetic rats. Results & conclusion: Polymersomes have shown good biocompatibility. Polymersomes are mainly localized within the cytoplasm of Caco-2 cells from fluorescence microscopy images. FA–P85–PLGA exhibited higher cellular uptake than PLGA–P85–PLGA polymersomes and free fluorescein isothiocyanate-labeled insulin (FITC–insulin) did. The uptake process of targeted polymersomes included clathrin- and caveolae-mediated endocytosis, macropinocytosis and the folate receptor-mediated endocytosis. Insulin-loaded FA–P85–PLGA showed better hypoglycemic effects than insulin-loaded PLGA–P85–PLGA.
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