Development of (G3-C12)-mediated camptothecin polymeric prodrug targeting to Galectin-3 receptor against androgen-independent prostate cancer.

The development of small molecule anticancer drugs, with low water solubility and high toxicity, into polymeric prodrugs has developed into a promising strategy in clinical application. In this study, we synthesized a novel G3-C12-mediated esterase-sensitive tumor-targeting polymeric prodrug of camptothecin (CPT), P(OEGMA-co-CPT-co-G3-C12), and explored its anticancer activity against androgen-independent prostate cancer in vitro and in vivo. Compared to free CPT, the multifunctional polymeric prodrug demonstrated improved water solubility and stability, higher intracellular uptake, and enhanced cytotoxicity in DU145 cells in vitro. Furthermore, it displayed an improved accumulation in the tumor and an enhanced anticancer activity in vivo. Hence, P(OEGMA-co-CPT-co-G3-C12) could be a promising drug in the treatment of androgen-independent prostate cancer.