通过开发双药载纳米制剂，将加巴喷丁和普瑞巴林重新定位以提高5-氟尿嘧啶的抗癌疗效
Repurposing gabapentin and pregabalin to improve the anticancer efficacy of 5-fluorouracil through development of a dual-drug-loaded nanoformulation.
摘要(中文译文)
抗癫痫药物加巴喷丁（GBP）和普瑞巴林（PGB）通过调节α2δ-1钙通道亚基发挥作用，而该亚基在肿瘤起始细胞中过表达。因此，本研究探讨通过双药负载乙基纤维素纳米粒（ECNPs）制剂将GBP和PGB重新定位用于增强5-氟尿嘧啶（5-FU）的抗癌疗效。采用改良纳米沉淀法制备ECNPs，并对其粒径、包封率和载药率以及体外抗癌疗效进行表征。两种ECNPs对COLO-205人结肠癌细胞系均表现出显著的抗癌疗效，GI值均小于10 µg/mL。它们对MCF-10A非癌性乳腺细胞系也表现出极低的毒性，提示其具有选择性治疗窗口，为癌症治疗提供了新途径。
Abstract
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 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.
如何引用
AMA
Chandan Raybarman, Surajit Bhattacharjee, Pratap Chandra Acharya. Repurposing gabapentin and pregabalin to improve the anticancer efficacy of 5-fluorouracil through development of a dual-drug-loaded nanoformulation.. Naunyn-Schmiedeberg's archives of pharmacology. 2026; doi:10.1007/s00210-026-05238-4.
APA
Chandan Raybarman, Surajit Bhattacharjee, Pratap Chandra Acharya (2026). Repurposing gabapentin and pregabalin to improve the anticancer efficacy of 5-fluorouracil through development of a dual-drug-loaded nanoformulation.. Naunyn-Schmiedeberg's archives of pharmacology. https://doi.org/10.1007/s00210-026-05238-4
GB/T 7714
Chandan Raybarman, Surajit Bhattacharjee, Pratap Chandra Acharya. Repurposing gabapentin and pregabalin to improve the anticancer efficacy of 5-fluorouracil through development of a dual-drug-loaded nanoformulation.[J]. Naunyn-Schmiedeberg's archives of pharmacology, 2026 doi:10.1007/s00210-026-05238-4.
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