Autophagy Inhibition via Functional Liposomal Hydroxychloroquine for Enhanced Antitumor Efficiency of Liposomal Doxorubicin
An autophagy balance exists in the tumor microenvironment.Appropriate disturbance to this balance may have therapeutic potential.Conventional autophagy modulating agents,such as Hydroxychloroquine (HCQ), always functioned at high dosages, which are inconsistently achieved in humans.In this study, we show that loading HCQ into liposomes (HCQ-Lip) decorated with a pH-sensitive TH-RGD targeting peptide (HCQ-TR-Lip) can concentrate HCQ in tumor cells and lysosomes.HCQ-TR-Lip was efficiently internalized as a result of its ability to bind integrin αvβ3 receptors highly expressed on the tumor cell surface and to undergo charge reversal from anionic at pH 7.4 to cationic at pH 6.5.HCQ-TR-Lip thus could significantly inhibit autophagy within tumor microenvironment,improving the ability of liposomal DOX (DOX-Lip)to inhibit tumor growth.
Yang Wang Kairong Shi Yayuan Liu Qin He
Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, 610041, China
国际会议
沈阳
英文
59-61
2016-04-28（万方平台首次上网日期，不代表论文的发表时间）