Targeted folate-conjugated pluronic P85/poly(lactide-co-glycolide) polymersome for the oral delivery of insulin. (11th October 2018)

• Record Type: Journal Article
• Authors: Xie, Shuang; Gong, Yan C; Xiong, Xiang Y; Li, Zi L; Luo, Yue Y; Li, Yu P
• Is Part Of: Nanomedicine. Volume 13:Number 19(2018)
• Page Start: 2527
• Page End: 2544
• Publication Date: 2018-10-11
• Subjects: FA–P85–PLGA -- folate-targeted -- insulin -- oral delivery -- polymersome; Nanotechnology -- Periodicals; Medical technology -- Periodicals; Nanotechnology -- Therapeutic use -- Periodicals; 610.28
• DOI: 10.2217/nnm-2017-0372
• Languages: English
• ISSNs: 1743-5889

Abstract

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.