Issue 15, 2022

Self-boosting stimulus activation of a polyprodrug with cascade amplification for enhanced antitumor efficacy

Abstract

The use of polyprodrugs, which bind drugs to polymer chains through responsive linkers, is a potential technique for cancer therapy; however, a lack of endogenous triggering factors limits drug activation in tumor tissue. Herein, we rationally created a reactive oxygen species (ROS)-sensitive polyprodrug (TSCA/DOX) with cascade amplification of triggering agents and drug activation by incorporating both an ROS signal amplifier (TACA) and a drug activation amplifier (SIPDOX) into a delivery system. Endogenous ROS as a triggering mechanism kicked off the initial circulation phase to increase intracellular ROS signals. Subsequently, the enhanced ROS initiated the second degradation step, allowing the polyprodrug SIPDOX to fracture spontaneously in a domino-like fashion, resulting in self-accelerated drug activation in tumor tissue. Therefore, the polyprodrug created in this study with cascade amplification of drug activation holds great promise for effective cancer treatment.

Graphical abstract: Self-boosting stimulus activation of a polyprodrug with cascade amplification for enhanced antitumor efficacy

Supplementary files

Article information

Article type
Paper
Submitted
27 Apr 2022
Accepted
15 Jun 2022
First published
16 Jun 2022

Biomater. Sci., 2022,10, 4228-4234

Self-boosting stimulus activation of a polyprodrug with cascade amplification for enhanced antitumor efficacy

Q. Zong, X. Xiao, J. Li and Y. Yuan, Biomater. Sci., 2022, 10, 4228 DOI: 10.1039/D2BM00647B

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