title: RGD(Arg-Gly-Asp) internalized docetaxel-loaded pH sensitive liposomes: Preparation, characterization and antitumor efficacy in vivo and in vitro.
abstract: The goal of this research was to formulate dual-targeting liposomes (RGD/DTX-PSL) that can selectively release loaded contents in a low pH level environment and to actively target to the tumor using liposomes that had surface arginine-glycine-aspartic (RGD) tripeptides. We investigated whether RGD/DTX-PSL could serve as an effective tumor-targeted nanoparticle that is capable of suppressing tumor growth. The results suggest that DTX is released from liposomes faster at pH 5.0 than pH 7.4, demonstrating their pH sensitivity. RGD/DTX-PSL has a longer blood circulation than Duopafei(®) in rats. The RGD/DTX-PSL formulation displayed stronger antiproliferative effects than DTX alone and the strongest inhibition of tumor growth of the formulations tested, thus expanding therapeutic window of DTX. In conclusion, we established a novel, promising and easy-to-handle liposome formulation that has a considerable antitumor activity in vitro and in vivo. This study provides important prerequisite for the clinical application of dual-targeting liposomes in delivering therapies.
authors: School of Pharmaceutical Science, Shandong University, 44 Wenhuaxi Road, Jinan, 250012,China; School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, China.
authors: Tiantian
authors: T
authors: Zuo
authors: School of Pharmaceutical Science, Shandong University, 44 Wenhuaxi Road, Jinan, 250012,China.
authors: Yuanyuan
authors: Y
authors: Guan
authors: School of Pharmaceutical Science, Shandong University, 44 Wenhuaxi Road, Jinan, 250012,China.
authors: Minglu
authors: M
authors: Chang
authors: School of Pharmaceutical Science, Shandong University, 44 Wenhuaxi Road, Jinan, 250012,China.
authors: Fang
authors: F
authors: Zhang
authors: School of Pharmaceutical Science, Shandong University, 44 Wenhuaxi Road, Jinan, 250012,China.
authors: Shanshan
authors: S
authors: Lu
authors: School of Pharmaceutical Science, Shandong University, 44 Wenhuaxi Road, Jinan, 250012,China.
authors: Ting
authors: T
authors: Wei
authors: School of Pharmaceutical Science, Shandong University, 44 Wenhuaxi Road, Jinan, 250012,China.
authors: Wei
authors: W
authors: Shao
authors: School of Pharmaceutical Science, Shandong University, 44 Wenhuaxi Road, Jinan, 250012,China. Electronic address: guimeilin@sdu.edu.cn.
authors: Guimei
authors: G
authors: Lin
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology*; D002470:Cell Survival / Q000187:drug effects; D000077143:Docetaxel; D005260:Female; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D008081:Liposomes / Q000737:chemistry*; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D009842:Oligopeptides / Q000737:chemistry*; D051381:Rats; D043823:Taxoids / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D008081:Liposomes; D009842:Oligopeptides; D043823:Taxoids; D000077143:Docetaxel; C047981:arginyl-glycyl-aspartic acid
keywords: Antitumor efficacy; Docetaxel; RGD; pH-sensitive liposomes