Abstract. We have shown that insulin-loaded Poly(lactic acid)-b-Pluronic-b-poly(lactic acid) nanoparticles (PLA-P85-PLA-NPs) had the hypoglycemic effect after oral administration on diabetic mice. In the present work, free insulin (INS) as controls, the influence of some factors such as time, temperature, pH level, and INS concentration on the uptake efficacy of PLA-P85-PLA-NPs as drug carriers were investigated through a Caco-2 cells. The micrographs of Caco-2 cell model were observed by microscopy. The cytotoxicity of PLA-P85-PLA-NPs in vitro was evaluated by MTT assay. The insulin concentrations in Caco-2 cells were determined by high-performance liquid chromatography (HPLC). Compared with INS groups, PLA-P85-PLA-NPs uptake was not controlled by pH levels. PLA-P85-PLA-NPs can be uptake by Caco-2 cells, and the absorption of PLA-P85-PLA-NPs is dependent on the concentration and incubation time. INS-loaded PLA-P85-PLA-NPs significantly enhanced insulin absorption. These results suggest that PLA-P85-PLA-NPs were more efficient than individual drugs into Caco-2 cells in a short period of time, and PLA-P85-PLA-NPs might be a useful drug carrier for proteins and peptides.
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