| Title | Lanreotide-conjugated PEG-DSPE micelles: an efficient nanocarrier targeting to somatostatin receptor positive tumors |
| Authors | Zheng, Nan Dai, Wenbing Zhang, Hua Wang, Xueqing Wang, Jiancheng Zhang, Xuan Wang, Kun Li, Jian Zhang, Qiang |
| Affiliation | Peking Univ, Canc Hosp & Inst, Good Clin Practice Ctr, Key Lab Carcinogenesis & Translat Res,Minist Educ, Beijing 100191, Peoples R China. Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China. Peking Univ, Sch Pharmaceut Sci, 38 Xueyuan Rd, Beijing 100191, Peoples R China. |
| Keywords | Antitumor lanreotide paclitaxel PEG-DSPE micelles receptor-mediated delivery somatostatin receptor 2 POORLY SOLUBLE DRUGS LIQUID-CHROMATOGRAPHY CREMOPHOR EL MOUSE PLASMA IN-VITRO PACLITAXEL DELIVERY THERAPY CANCER PHARMACOKINETICS |
| Issue Date | 2015 |
| Publisher | journal of drug targeting |
| Citation | JOURNAL OF DRUG TARGETING.2015,23,(1),67-78. |
| 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. |
| URI | http://hdl.handle.net/20.500.11897/188570 |
| ISSN | 1061-186X |
| DOI | 10.3109/1061186X.2014.954118 |
| Indexed | SCI(E) PubMed |
| Appears in Collections: | 北京肿瘤医院 药学院 天然药物与仿生药物国家重点实验室 |
