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

Abstract

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.

• Authors: Chunxiao Li, Zhenyu Chen, Dan Zheng, Jingyang Zhao, Jiandu Lei
• Journal: ACS applied bio materials (ACS Appl Bio Mater) Vol. 4 Issue 2 Pg. 1499-1507 (02 15 2021) ISSN: 2576-6422 [Electronic] United States
• PMID: 35014499 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Polymers

Topics

• Antineoplastic Agents (pharmacology, therapeutic use)
• Drug Delivery Systems (methods)
• Humans
• Nanoparticles (metabolism)
• Polymers (metabolism)