ngr-peptide and cholesteryl-succinate

As current tumor chemotherapy faces many challenges, it is important to develop drug delivery systems with increased tumor-targeting ability, enhanced therapeutic effects and reduced side effects. In this study, a pH-sensitive liposome was constructed containing CHEMS-anchored PEG2000 for extended circulation and NGR peptide as the targeting moiety. The NGR-modified docetaxel-loaded pH-sensitive extended-circulation liposomes (DTX/NGR-PLL) prepared possess suitable physiochemical properties, including particle size of approximately 200nm, drug encapsulation efficiency of approximately 70%, and pH-sensitive drug release properties. Experiments performed in vitro and in vivo on human fibrosarcoma cells (HT-1080) and human breast adenocarcinoma cells (MCF-7) verified the specific targeting ability and enhanced antitumor activity to HT-1080 cells. The results of intravenous administration demonstrated that NGR-modified liposomes can significantly and safely accumulate in tumor tissue in xenografted nude mice. In conclusion, the liposomes constructed hold promise as a safe and efficient drug delivery system for specific tumor treatment.

Topics: Animals; Cell Line, Tumor; Cholesterol Esters; Delayed-Action Preparations; Docetaxel; Drug Delivery Systems; Drug Liberation; Humans; Hydrogen-Ion Concentration; Liposomes; MCF-7 Cells; Mice, Inbred BALB C; Mice, Nude; Neoplasms; Oligopeptides; Polyethylene Glycols; Taxoids; Xenograft Model Antitumor Assays