Dodecanol-poly(d,l-lactic acid)-b-poly (ethylene glycol)-folate (Dol-PLA-PEG-FA) nanoparticles: Evaluation of cell cytotoxicity and selecting capability in vitro

Folate-conjugated Dol-poly(d,l-lactic acid)-b-poly (ethylene glycol)-folate (Dol-PLA-PEG-FA), was synthesized from dodecanol-poly(d,l-lactic acid), amino-terminated poly(ethylene glycol) and folate. 1H NMR proved the successful synthesis of Dol-PLA-PEG-FA. Nanoparticles (NPs) were further fabricated from Dol-PLA-PEG-FA by using solvent evaporation-induced interfacial self-assembly method. The size, critical micelle concentration (CMC), cytotoxicity and selecting capability to cancer cells in vitro were examined for Dol-PLA-PEG-FA NPs. The size of NPs showed polymer concentration-dependent phenomenon in the fabrication process, and its polydispersity index (PDI) was very narrow. The CMC was determined as 1.995 × 10−4 g/L in aqueous solution, which is much lower than the reported CMC of block copolymer self-assemble micelles. The cytotoxicity evaluation revealed that the obtained NPs2 are non-toxic to either breast cancer cell or normal endothelial cells, and the cell uptake of NPs indicated that the NPs demonstrated much higher selecting capability to breast cancer cells compared to normal fibroblast cells. The possible receptor-mediated endocytosis pathway mechanism was proposed. Based on the above results, it could be concluded that Dol-PLA-PEG-FA polymer and its nanoparticles can be potentially used as a safe drug carrier with strong tumor cells targeting capability for tumor chemotherapy.

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► We prepared and characterized copolymer Dol-PLA-PEG-FA and its nanoparticles.
► The nanoparticles showed narrow distribution index and low critical micelles concentration.
► Cell proliferation and cytotoxicity test demonstrated that breast cancer cells exhibited slightly better cell proliferation than vascular endothelial cells.
► Breast cancer cells showed higher cellular uptake of nanoparticles compared with normal fibroblast cells.