Targeted Delivery of Dual Anticancer Drugs Based on Self-Assembled iRGD-Modified Soluble Drug-Polymer Pattern Conjugate Nanoparticles.

A tumor-penetrating peptide, iRGD (a tumor-homing peptide, CRGDKGPDC), could enhance the penetration of drugs via the specific receptor-binding affinity to αvβ3 and NRP-1 that overexpressed on tumor vasculature and tumor cells. Considering the side effects of traditional chemotherapy, here, poly(ethylene glycol) (PEG, Mw = 7500)-based and iRGD-modified poly(ethylene glycol)-based nanoparticles were successfully prepared. iRGD, as a tumor-targeting and tumor-penetrating agent, was combined with PEG after the esterification reaction between PEG and diosgenin (DGN). After the efficient loading of 10-hydroxycamptothecin (HCPT), the iRGD-PEG-DGN/HCPT NPs of chemotherapy were established. The characteristics of iRGD-PEG-DGN/HCPT NPs were evaluated. This nano-delivery system possessed high drug loading efficiency (∼17.34 wt % HCPT), controlled release rate, good pH response, and iRGD active targeting and passive targeting with an appropriate size (∼140 nm). All these features forcefully indicated that the iRGD-modified drug delivery system could markedly ameliorate the tumor therapy efficacy compared to the nontargeted nanoparticles through enhancing the tumor accumulation and penetration.