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Lots of attention has been drawn to targeted nano-drug delivery systems due to their high therapeutic efficacy in cancer treatment. In this work, doxorubicin (DOX) was incorporated into a zwitterionic arginyl-glycyl-aspartic acid (RGD)-conjugated polypeptide by an emulsion solvent evaporation technique with high drug loading content (45%) and high drug loading efficiency (95%). This zwitterionic nano-formulation showed excellent colloidal stability at high dilution and in serum. The pH-induced disintegration and enzyme-induced degradation of the nano-formulation were confirmed by dynamic light scattering (DLS) and gel permeation chromatography (GPC). Efficient internalization of DOX in the cells and high antitumor activity in vitro was observed. Compared with free drug, this nano-formulation showed higher accumulation in tumor and lower systemic toxicity in vivo. The DOX-loaded zwitterionic RGD-conjugated polypeptide vesicles show potential application for targeted drug delivery in the clinic.
PMID: 29933695 [PubMed - as supplied by publisher]