title: Facile fabrication of thermo-responsive and reduction-sensitive polymeric micelles for anticancer drug delivery.
abstract: The development of thermo-responsive and reduction-sensitive polymeric micelles based on an amphiphilic block copolymer poly[(PEG-MEMA)-co-(Boc-Cyst-MMAm)]-block-PEG (denoted PEG-P-SS-HP) for the intracellular delivery of anticancer drugs is reported. PTX, as model drug, was loaded into the PEG-P-SS-HP micelles with an encapsulation efficiency >90%, resulting in a high drug loading content (up to 35 wt%). The PTX-loaded PEG-P-SS-HP micelles show slow drug release in PBS and rapid release after incubation with DTT. The PTX-loaded micelles display a better cytotoxic effect than the free drug, whereas empty micelles are found to be non-toxic. The thermo-responsive and reduction-sensitive polymeric micelles described may serve as promising carriers for cytostatic drugs.
authors.affiliation: Key Laboratory of Biomedical Polymers of Ministry of Education, and Department of Chemistry, Wuhan University, Luojia Hill, Wuhan 430072, China. xljiang@whu.edu.cn
authors.forename: Xulin
authors.initials: X
authors.lastname: Jiang
authors.forename: Lihua
authors.initials: L
authors.lastname: Li
authors.forename: Jia
authors.initials: J
authors.lastname: Liu
authors.forename: Wim E
authors.initials: WE
authors.lastname: Hennink
authors.forename: Renxi
authors.initials: R
authors.lastname: Zhuo
mesh_terms: D000180:Acrylic Resins / Q000138:chemical synthesis* / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D001672:Biocompatible Materials / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004229:Dithiothreitol / Q000737:chemistry; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000494:pharmacology; D004339:Drug Compounding; D056945:Hep G2 Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D010084:Oxidation-Reduction; D017239:Paclitaxel / Q000737:chemistry / Q000494:pharmacology*; D011092:Polyethylene Glycols / Q000138:chemical synthesis* / Q000494:pharmacology; D011108:Polymers / Q000138:chemical synthesis* / Q000494:pharmacology; D013696:Temperature
chemical_list: D000180:Acrylic Resins; D000972:Antineoplastic Agents, Phytogenic; D001672:Biocompatible Materials; D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; C576119:poly((poly(ethylene glycol) methyl methacrylate)-co-(tert-butyloxycarbonylaminoethyldithioethyl methacrylamide)); D011092:Polyethylene Glycols; D017239:Paclitaxel; D004229:Dithiothreitol