The assembly of small molecule conjugate amphiphiles into a precise nanomedicine for colon cancer

Abstract

A small molecule conjugate based on a traditional Chinese medicine cantharidin (CTR), which is an anhydride, and the anticancer drug camptothecin (CPT) was designed. This small molecule conjugate is amphiphilic and was found to readily self-assemble into NPs. The NPs were systematically characterized and shown to release drugs in a pH dependent manner. Moreover, we found that cancer cells internalized the NPs via endocytosis. The ester bond could be opened by an esterase to release the two drugs in tumor cells with lower pH values. After that, these two drugs work synergistically to kill the cancer cells. Lastly, mice bearing subcutaneous HT29 colon cancer were i.v. injected with these NPs and great potential for inhibiting colon cancer was found.