title: Lipid composition has significant effect on targeted drug delivery properties of NGR-modified liposomes.
abstract: The Asn-Gly-Arg (NGR) motif has previously been demonstrated to specifically bind to CD13, which is selectively overexpressed in tumor vasculature and some tumor cells (e.g. HT1080). It was reported that NGR-modified stealth liposomes (NGR-SL) could be prepared with different lipid composition, such as 1,2-dipalmitoyl-sn-glycero-phosphatidylcholine (DPPC), hydrogenated soy posphatidylcholine (HSPC) and soy posphatidylcholine (SPC). In the present study, NGR-modified liposomes were prepared with DPPC, HSPC, SPC or the mixture of HSPC and SPC. The resultant liposomes with different lipid composition were compared in terms of cell uptake, antitumor efficacy and targeted drug delivery efficiency using HT1080 tumor model. It was found that NGR-SL composed of the mixture of HSPC and SPC was able to improve targeted drug delivery efficiency to tumor producing the most significant antitumor activity. Collectively, the NGR-modified liposomes composed of the mixture of HSPC and SPC are promising carriers for the treatment of tumor. Besides NGR ligand, lipid composition could also significantly affect the targeted delivery efficiency to the tumor.
authors.affiliation: a Pharmaceutical Research Laboratory, School of Pharmacy, Nanjing University of Chinese Medicine , Nanjing , People's Republic of China .
authors.forename: Jun
authors.initials: J
authors.lastname: Chen
authors.affiliation: b The Second Faculty of Clinical Medicine, Guangzhou University of Chinese Medicine , Guangzhou , People's Republic of China , and.
authors.forename: Aihua
authors.initials: A
authors.lastname: Lin
authors.affiliation: b The Second Faculty of Clinical Medicine, Guangzhou University of Chinese Medicine , Guangzhou , People's Republic of China , and.|c Hubei Collaborative Innovation Center of Targeted Antitumor Drug, Jingchu University of Technology , Jingmen , People's Republic of China.
authors.forename: Pei
authors.initials: P
authors.lastname: Peng
authors.affiliation: a Pharmaceutical Research Laboratory, School of Pharmacy, Nanjing University of Chinese Medicine , Nanjing , People's Republic of China .
authors.forename: Yong
authors.initials: Y
authors.lastname: Wang
authors.affiliation: a Pharmaceutical Research Laboratory, School of Pharmacy, Nanjing University of Chinese Medicine , Nanjing , People's Republic of China .
authors.forename: Wei
authors.initials: W
authors.lastname: Gu
authors.affiliation: b The Second Faculty of Clinical Medicine, Guangzhou University of Chinese Medicine , Guangzhou , People's Republic of China , and.
authors.forename: Yiming
authors.initials: Y
authors.lastname: Liu
mesh_terms: D015060:1,2-Dipalmitoylphosphatidylcholine / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D006801:Humans; D008081:Liposomes; D009842:Oligopeptides / Q000737:chemistry*; D013025:Glycine max / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D008081:Liposomes; C526428:NGR peptide; D009842:Oligopeptides; D015060:1,2-Dipalmitoylphosphatidylcholine
keywords: Active targeting; NGR; lipid composition; liposomes; tumor