Synthesis and Characterization of Poly(ε-caprolactone)-block-polyN-(2-hydroxypropyl)methacrylamide Micelles for Drug Delivery

摘要

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 IC50 dose was 1.96 μM after 72 h of incubation, whereas the micelles without drug showed no cytotoxicity.