A novel GSH-triggered polymeric nanomicelles for reversing MDR and enhancing antitumor efficiency of Hydroxycamptothecin

Int J Pharm. 2021 Mar 26:120528. doi: 10.1016/j.ijpharm.2021.120528. Online ahead of print.


Tumor multidrug resistance (MDR) is one of the main reasons for the failure of clinical chemotherapy. Here, a bio-responsive anti-drug-resistant polymer micelle that can respond to the reductive GSH in the tumor microenvironment (TME) for delivery of HCPT was designed. A new type of with anti-drug resistance and anti-tumor effect was synthesized and used to encapsulated HCPT to form reduction-sensitive micelles (PDSAH) by a thin-film dispersion method. It is demonstrated that the micelle formulation improves the anti-tumor activity and biosafety of HCPT, and also plays a significant role in reversing the drug resistance, which contributes to inhibiting the tumor growth and prolonging the survival time of H22 tumor-bearing mice. The results indicate that this nanoplatform can serve as a flexible and powerful system for delivery of other drugs that are tolerated by tumors or bacteria.

PMID:33781880 | DOI:10.1016/j.ijpharm.2021.120528