iRGD-functionalized PEGylated nanoparticles for enhanced colon tumor accumulation and targeted drug delivery

Abstract

Aim: To enhance the tumor accumulation and targeted drug delivery for colon cancer therapy, iRGD peptide was introduced to the surface of PEGylated camptothecin-loaded nanoparticles (NPs). Methods: Cellular uptake, targeting specificity, biodistribution and antitumor capacity were evaluated. Results: The functionalization of iRGD facilitated tumor accumulation and cellular uptake of NPs by Colon-26 cells. Furthermore, the resultant iRGD-PEG-NPs remarkably improved the therapeutic efficacy of camptothecin in vitro and in vivo by inducing a higher degree of tumor cell apoptosis compared with PEG-NPs. Conclusion: iRGD-PEG-NP is a desired drug delivery system to facilitate the drug accumulation in orthotopic colon tumor tissues and further drug internalization by colon cancer cells.