标题：NGR-modified pH-sensitive liposomes for controlled release and tumor target delivery of docetaxel
作者：Gu, Zili; Chang, Minglu; Fan, Yang; Shi, Yanbin; Lin, Guimei
作者机构：[Gu, Zili; Chang, Minglu; Fan, Yang; Lin, Guimei] Shandong Univ, Sch Pharmaceut Sci, 44 West Wenhua Rd, Jinan 250012, Shandong, Peoples R China.; [S 更多
通讯作者地址：[Lin, GM]Shandong Univ, Sch Pharmaceut Sci, 44 West Wenhua Rd, Jinan 250012, Shandong, Peoples R China.
来源：COLLOIDS AND SURFACES B-BIOINTERFACES
关键词：Docetaxel; Long circulation; NGR; pH-sensitive liposomes; Tumor; targeting
摘要：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 200 nm, 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. (C) 2017 Elsevier B.V. All rights reserved.