Abstract

Colon cancer (CC) is one of the major causes of death worldwide. Insufficient drug concentration, non-specificity, or serious adverse effects of the conventional chemotherapeutic agents necessitate application of more effective treatment options. Herein, poly-ursolic acid, a polymer with anticancer effect, has been self-assembled for producing nanoparticles (NPs) for delivery of irinotecan (IRN) which is usually associated with poor solubility and severe adverse effects. NPs showed therapeutic efficiency by themselves in vivo and in vitro. IRN-loaded NPs with appropriate physicochemical characteristics, released IRN in a controlled fashion and demonstrated more efficient cytotoxicity, lower clearance rate and distribution volume, higher Cmax and AUC, prolonged t1/2, increased accumulation in tumor, and therapeutic effects in vivo as compared to free drug. There was no significant alteration of body weight or damage to the major organs. The prepared bioactive nanoplatform via improvement of IRN efficiency could be applied for inducing synergistic toxicity against CC.

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