Novel polymeric micelles with cinnamic acid as lipophilic moiety for 9-Nitro-20(S)-camptothecin delivery

9-Nitro-20(S)-camptothecin (9-NC) is a broad-spectrum anticancer drug but its application was limited by its poor solubility in aqueous medium. Novel polymeric micelles were developed for 9-NC delivery. The micelles were fabricated from the self-assembly of amphiphiles with cinnamic acid (CIN) as lipohilic moiety and methoxy poly(ethylene glycol) (mPEG) as hydrophilic segment. The micelles were nontoxic to NIH 3T3 fibroblasts. 9-NC was trapped efficiently in mPEG-DCIN micelles. The release of 9-NC from the micelles with one cinnamic acid molecule as lipophilic moiety (mPEG-CIN) was much faster than that from the micelles with two cinnamic acid molecules as lipophilic moiety (mPEG-DCIN). The in vitro anticancer inhibition study demonstrated that the anticancer activity of 9-NC loaded mPEG-DCIN micelles was much better than that of 9-NC loaded mPEG-CIN micelles. Crown Copyright (c) 2013 Published by Elsevier B.V. All rights reserved.