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Antitumor Activity of a Novel Double-Targeted System for Folate Receptor-Mediated Delivery of Mitomycin C

Yan Xu1, Xiangmei Jin2, Jun Zhang1

  • 1Center of Morphological Experiment, Yanbian University, Yanji 133002, Jilin, China.

ACS Omega
|October 28, 2020
PubMed

Insights

A novel double-targeted drug delivery system using folic acid (FA) and glycine-phenylalanine-leucine-glycine (GFLG) effectively delivered mitomycin C (MMC) to cancer cells, enhancing antitumor activity and reducing toxicity to normal cells.

Area of Science:

  • Biotechnology and Pharmaceutical Sciences
  • Oncology and Cancer Research
  • Drug Delivery Systems

Background:

  • Cancer cells often overexpress folate receptors (FR), presenting a target for selective drug delivery.
  • Conventional chemotherapy drugs like mitomycin C (MMC) exhibit significant toxicity to both cancerous and normal cells.
  • Developing targeted drug delivery systems can improve therapeutic efficacy and minimize side effects.

Purpose of the Study:

  • To design and formulate a novel double-targeted drug delivery system for enhanced antitumor activity.
  • To investigate the FR-mediated delivery and cytotoxic effects of the FA-GFLG-MMC system.
  • To compare the antitumor efficacy and toxicity profile of the targeted system versus free MMC.

Main Methods:

  • A drug delivery system was formulated using folic acid (FA) as the FR-targeting ligand and glycine-phenylalanine-leucine-glycine (GFLG) for cathepsin B-specific cleavage.
  • The anticancer drug mitomycin C (MMC) was conjugated to the FA-GFLG system (FA-GFLG-MMC).
  • Cytotoxicity was assessed using the MTT assay on cell lines with high (HeLa, SiHa, PC9) and low (16HBE, A549) FR expression. Apoptosis was evaluated by Western blotting for BAX and BCL-2 expression.

Main Results:

  • FA-GFLG-MMC demonstrated significantly higher inhibitory effects on cancer cells (HeLa, SiHa, PC9) compared to cells with low FR expression (16HBE, A549).
  • The drug delivery system inhibited cancer cell proliferation in a dose-dependent manner, with reduced toxicity to normal cells compared to free MMC.
  • FA-GFLG-MMC treatment increased the BAX/BCL-2 ratio in targeted cancer cells, indicating enhanced apoptosis induction.

Conclusions:

  • The developed FA-GFLG-MMC system effectively targets cancer cells via FR-mediated endocytosis and cathepsin B cleavage.
  • This targeted delivery enhances the induction of apoptosis in cancer cells, leading to effective tumor cell proliferation inhibition.
  • The system shows potential for improving anticancer drug delivery, increasing therapeutic efficacy while minimizing systemic toxicity.

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