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.

► New polymeirc amphiphiles with one and two cinnamic acid as lipophilic moieties were synthesized and self-assembled into micelles. ► The number of cinnamic acid in the amphiphiles affected the drug release behavior seriously. ► The micelles with two cinnamic acid molecules showed better anti-tumor inhibition activity to HepG2 cancer cells. ► We report a new strategy for fabricating polymeric micelles for anti-tumor drug delivery.