Methotrexate-loaded biodegradable polymeric micelles: preparation, physicochemical properties and in vitro drug release.
Polymeric micelles based on amphiphilic diblock copolymers methoxy poly(ethylene glycol)-polylactide with various hydrophobic lengths were designed as carriers of poorly water-soluble anticancer drug methotrexate (MTX). Relationship between physicochemical characteristics of micelles and release behavior was explored. The critical micelle concentration was determined by fluorescence spectroscopy using 9-chloromethyl anthracene as fluorescence probe. Core-shell type polymeric micelles were prepared by free-surfactant dialysis technique. The mean size of micelles loaded with MTX was 50-200 nm with narrow polydispersity. Physicochemical properties of drug-loaded micelles were evaluated. In vitro release behavior of MTX was also investigated. MTX was continuously released from micelles and less than 50% MTX was released in 5 days. Release rate was dependent on chemical structures of micelles and enhanced by decreasing polylactide lengths.
Zhang
Ying
Y
School of Pharmacy, Shanghai JiaoTong University, Shanghai 200030, China.
Jin
Tuo
T
Zhuo
Ren-Xi
RX
D000873:Anthracenes / Q000494:pharmacology; D001672:Biocompatible Materials / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000494:pharmacology; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008727:Methotrexate / Q000008:administration & dosage* / Q000494:pharmacology; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D008956:Models, Chemical; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D011208:Powders; D013050:Spectrometry, Fluorescence; D013501:Surface-Active Agents; D013997:Time Factors; D014961:X-Ray Diffraction
D000873:Anthracenes; D001672:Biocompatible Materials; D004337:Drug Carriers; D004791:Enzyme Inhibitors; D008823:Micelles; D011108:Polymers; D011208:Powders; D013501:Surface-Active Agents; C099162:9-chloromethylanthracene; D011092:Polyethylene Glycols; D008727:Methotrexate