title: Lanreotide-conjugated PEG-DSPE micelles: an efficient nanocarrier targeting to somatostatin receptor positive tumors.
abstract: Lanreotide is an octapeptide analog of endogenous somatostatin, specifically binding with tumors over-express somatostatin receptor 2 (SSTR2). In this study, we conjugated lanreotide to 1, 2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy (poly-(ethylene glycol))-2000] (PEG-DSPE), constructed active targeted micelles (lanreotide-PM), characterized their in vitro and in vivo targeting effect, and explored the receptor mediated transportion. The uptake of lanreotide-PM was found to be related to the expression level of SSTR2 in different cell lines and the competitive inhibition phenomenon indicated that the cellular uptake of lanreotide-PM was via a receptor meditated mechanism. In vivo, more lanreotide-PM accumulated in SSTR2 high expression tumor xenografts, endocytosed by the tumor cells, induced more apoptosis of tumor cells, and suppressed tumor growth efficiently. In conclusion, lanreotide-modified micelles containing antitumor drugs provide a promising strategy for the treatment of SSTR-expressing tumors.
authors.affiliation: Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Good Clinical Practice Center, Peking University Cancer Hospital & Institute , Beijing , People's Republic of China and.
authors.forename: Nan
authors.initials: N
authors.lastname: Zheng
authors.forename: Wenbing
authors.initials: W
authors.lastname: Dai
authors.forename: Hua
authors.initials: H
authors.lastname: Zhang
authors.forename: Xueqing
authors.initials: X
authors.lastname: Wang
authors.forename: Jiancheng
authors.initials: J
authors.lastname: Wang
authors.forename: Xuan
authors.initials: X
authors.lastname: Zhang
authors.forename: Kun
authors.initials: K
authors.lastname: Wang
authors.forename: Jian
authors.initials: J
authors.lastname: Li
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D006224:Cricetinae; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D004705:Endocytosis; D005456:Fluorescent Dyes / Q000737:chemistry; D006801:Humans; D008297:Male; D008823:Micelles; D009369:Neoplasms / Q000378:metabolism*; D017239:Paclitaxel / Q000737:chemistry / Q000494:pharmacology; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000378:metabolism* / Q000493:pharmacokinetics; D010714:Phosphatidylethanolamines / Q000737:chemistry* / Q000493:pharmacokinetics; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017481:Receptors, Somatostatin / Q000378:metabolism*; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics; D013050:Spectrometry, Fluorescence; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D005456:Fluorescent Dyes; D008823:Micelles; D010456:Peptides, Cyclic; D010714:Phosphatidylethanolamines; D017481:Receptors, Somatostatin; C107570:polyethylene glycol-distearoylphosphatidylethanolamine; C060347:lanreotide; D011092:Polyethylene Glycols; D013004:Somatostatin; C093733:somatostatin receptor 2; D017239:Paclitaxel
keywords: Antitumor; PEG-DSPE micelles; lanreotide; paclitaxel; receptor-mediated delivery; somatostatin receptor 2