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.
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Acrylamides / chemical synthesis*
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Acrylamides / pharmacology
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Biocompatible Materials / chemical synthesis*
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Biocompatible Materials / pharmacology
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Cell Line, Tumor
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Cell Survival / drug effects*
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Drug Compounding
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Drug Delivery Systems / methods*
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Humans
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Inhibitory Concentration 50
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Kinetics
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Magnetic Resonance Spectroscopy
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Male
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Micelles
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Microscopy, Electron, Transmission
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Particle Size
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Polyesters / chemical synthesis*
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Polyesters / pharmacology
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Polyethylene Glycols / chemistry
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Polymerization
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Polymers / chemical synthesis*
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Polymers / pharmacology
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Prostatic Neoplasms / drug therapy
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Prostatic Neoplasms / pathology
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Retinoids / metabolism
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Retinoids / pharmacology*
Substances
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Acrylamides
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Biocompatible Materials
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Micelles
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Polyesters
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Polymers
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Retinoids
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polycaprolactone
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Polyethylene Glycols
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N-(2-hydroxypropyl)methacrylamide