title: Synthesis and characterization of poly(ε-caprolactone)-block-poly[N-(2-hydroxypropyl)methacrylamide] micelles for drug delivery.
abstract: Amphiphilic block copolymers based on HPMA and ε-CL were synthesized by ring-opening polymerization of ε-CL followed by RAFT polymerization of HPMA. A copolymer composed of 34 kDa PHPMA and 8.5 kDa PCL associated into micelles with CMC of 5.4 µg · mL(-1) . A novel retinoid, 3-Cl-AHPC-OMe, was incorporated into micelles with 25 wt.-% loading by dialysis method. The effective diameter of drug loading micelles was 117 nm. Incubation of micelles in PBS at 37 °C indicated 86 wt.-% of the drug was released after 96 h. Cytotoxicity studies performed with C4-2 prostate cancer cells showed the IC(50) dose was 1.96 µM after 72 h of incubation, whereas the micelles without drug showed no cytotoxicity.
authors.affiliation: Department of Pharmaceutics and Pharmaceutical Chemistry, University of Utah, Salt Lake City, UT 84112, USA.
authors.forename: Stefan G
authors.initials: SG
authors.lastname: Krimmer
authors.forename: Huaizhong
authors.initials: H
authors.lastname: Pan
authors.forename: Jihua
authors.initials: J
authors.lastname: Liu
authors.forename: Jiyuan
authors.initials: J
authors.lastname: Yang
authors.forename: Jindřich
authors.initials: J
authors.lastname: Kopeček
mesh_terms: D000178:Acrylamides / Q000138:chemical synthesis* / Q000494:pharmacology; D001672:Biocompatible Materials / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects*; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D011091:Polyesters / Q000138:chemical synthesis* / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry; D058105:Polymerization; D011108:Polymers / Q000138:chemical synthesis* / Q000494:pharmacology; D011471:Prostatic Neoplasms / Q000188:drug therapy / Q000473:pathology; D012176:Retinoids / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D000178:Acrylamides; D001672:Biocompatible Materials; D008823:Micelles; D011091:Polyesters; D011108:Polymers; D012176:Retinoids; C016240:polycaprolactone; D011092:Polyethylene Glycols; C032976:N-(2-hydroxypropyl)methacrylamide