title: Octreotide-modified N-octyl-O, N-carboxymethyl chitosan micelles as potential carriers for targeted antitumor drug delivery.
abstract: Octreotide (OCT) was recently found to have high binding affinity to the positive tumor cells of somatostatin receptors (SSTRs). In this study, octreotide-Phe-polyethylene glycol-stearic acid was first successfully synthesized and used as a targeting molecule for N-octyl-O, N-carboxymethyl chitosan (OCC). Doxorubicin (DOX) was loaded into OCT-modified OCC micelles (DOX-OCC-OCT). The drug-loaded micelles obtained exhibited spherical shape, small particle sizes, and negative zeta potentials. The cytotoxicity of DOX-OCC-OCT micelles against MCF-7 cells (SSTRs expressing) was found to significantly increase with the increased amount of OCT modification, whereas no significant difference was observed against WI-38 cells (no SSTRs expressing). Results of flow cytometry, fluorescence microscopy, and confocal laser scanning microscopy confirmed that DOX-OCC-OCT micelles could remarkably increase the uptake of DOX in MCF-7 cells. All the results indicated that OCC-OCT micelles may be a promising intracellular targeting carrier for efficient delivery of antitumor drugs into tumor cells.
authors.affiliation: Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Aifeng
authors.initials: A
authors.lastname: Zou
authors.forename: Meirong
authors.initials: M
authors.lastname: Huo
authors.forename: Yong
authors.initials: Y
authors.lastname: Zhang
authors.forename: Jianping
authors.initials: J
authors.lastname: Zhou
authors.forename: Xiaoqiang
authors.initials: X
authors.lastname: Yin
authors.forename: Chengli
authors.initials: C
authors.lastname: Yao
authors.forename: Qinnv
authors.initials: Q
authors.lastname: Zhu
authors.forename: Min
authors.initials: M
authors.lastname: Zhang
authors.forename: Jinshan
authors.initials: J
authors.lastname: Ren
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage*; D017209:Apoptosis; D002152:Calorimetry, Differential Scanning; D045744:Cell Line, Tumor; D048271:Chitosan / Q000737:chemistry*; D004317:Doxorubicin / Q000008:administration & dosage*; D004337:Drug Carriers; D005434:Flow Cytometry; D006801:Humans; D008823:Micelles; D018613:Microscopy, Confocal; D008856:Microscopy, Fluorescence; D015282:Octreotide / Q000737:chemistry*; D010316:Particle Size
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D004317:Doxorubicin; D048271:Chitosan; D015282:Octreotide