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<p>The antiepileptic drugs gabapentin (GBP) and pregabalin (PGB) act by modulating α2δ-1 calcium channel subunits, which are overexpressed in tumor-initiating cells. Therefore, this study investigates repurposing GBP and PGB in enhancing anticancer efficiency of 5-fluorouracil (5-FU) through a dual-drug-loaded ethyl cellulose nanoparticles (ECNPs) formulation. The ECNPs are prepared using a modified nanoprecipitation method and characterized for particle size, encapsulation and loading efficiencies, and in vitro anticancer efficacy. They exhibited pronounced anticancer efficacy against COLO-205 human colon cancer cell line, with GI<sub>50</sub> value less than 10&#xa0;µg/mL for both the ECNPs. They also exhibited minimal toxicity on MCF-10A non-cancerous breast cell line, suggesting a selective therapeutic window offering new avenues in cancer therapy.</p> Graphical Abstract <p></p>

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Repurposing gabapentin and pregabalin to improve the anticancer efficacy of 5-fluorouracil through development of a dual-drug-loaded nanoformulation

  • 期刊论文

  • 发表日期：

    2026年3月27日

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  • Chandan Raybarman,
  • Surajit Bhattacharjee,
  • Pratap Chandra Acharya

摘要

The antiepileptic drugs gabapentin (GBP) and pregabalin (PGB) act by modulating α2δ-1 calcium channel subunits, which are overexpressed in tumor-initiating cells. Therefore, this study investigates repurposing GBP and PGB in enhancing anticancer efficiency of 5-fluorouracil (5-FU) through a dual-drug-loaded ethyl cellulose nanoparticles (ECNPs) formulation. The ECNPs are prepared using a modified nanoprecipitation method and characterized for particle size, encapsulation and loading efficiencies, and in vitro anticancer efficacy. They exhibited pronounced anticancer efficacy against COLO-205 human colon cancer cell line, with GI50 value less than 10 µg/mL for both the ECNPs. They also exhibited minimal toxicity on MCF-10A non-cancerous breast cell line, suggesting a selective therapeutic window offering new avenues in cancer therapy.

Graphical Abstract