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Updated: Feb 10, 2026

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Encapsulating GSH/NQO1-responsive SN38 prodrug micelles with Timosaponin AIII-based multifunctional liposomes for

Xu Luo1,2, Ziqiong Yang1,2, Jianqiu Chen3

  • 1School of Pharmacy, Xuzhou Medical University, Xuzhou 221004, China.

International Journal of Pharmaceutics: X
|February 9, 2026
PubMed

Insights

This study developed novel liposomes using Timosaponin AIII (TAIII) to deliver SN38 prodrug micelles for targeted colorectal cancer chemotherapy. The PSSQ@TLP formulation enhanced drug accumulation in tumors and reduced toxicity.

Area of Science:

  • Biomedical Engineering
  • Nanotechnology
  • Oncology

Background:

  • Colorectal cancer (CRC) chemotherapy is limited by poor drug delivery to tumors and significant side effects.
  • Micellar liposome carriers offer potential for improved drug delivery, controlled release, and targeted action against cancer.

Purpose of the Study:

  • To develop a novel tumor-targeted chemotherapy system for colorectal cancer.
  • To encapsulate a glutathione (GSH)/NQO1-responsive SN38 prodrug (PSSQ) into multifunctional liposomes stabilized by Timosaponin AIII (TAIII).

Main Methods:

  • Synthesized an amphiphilic SN38 prodrug (PSSQ) that self-assembles into micelles.
  • Developed TAIII-based liposomes (TLP) using cholesterol replacement for stability and glucose transporter 1 (GLUT1) targeting.
  • Encapsulated PSSQ micelles into TLP to form PSSQ@TLP.
  • Conducted in vitro release studies, cytotoxicity assays (MTT), and in vivo evaluations (biodistribution, anti-tumor efficacy, biosafety) in a CT26.WT mouse model.

Main Results:

  • Molecular docking confirmed TAIII interaction with GLUT1, suggesting enhanced tumor targeting.
  • PSSQ@TLP exhibited controlled GSH/NQO1-responsive drug release in simulated tumor microenvironments.
  • In vitro studies showed significant cytotoxicity against colorectal cancer cell lines.
  • In vivo studies demonstrated superior intratumoral drug accumulation, potent tumor suppression, and reduced systemic toxicity compared to controls.

Conclusions:

  • The developed PSSQ@TLP system shows significant promise as an effective and safer targeted therapeutic strategy for colorectal cancer.
  • TAIII-based liposomes offer a multifunctional platform for enhanced drug delivery and tumor targeting in cancer therapy.
Keywords:
Cholesterol-replacement liposomesColorectal cancerGSH/NQO1-responsive SN38 prodrug micellesMicellar liposome complex carriersTimosaponin AIII

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