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. 2025 Jan 22;42(2):53.
doi: 10.1007/s12032-025-02603-w.

Enhanced antitumor efficacy of nanostructured lipid carrier co-loaded with docetaxel and 5-fluorouracil for targeted gastric cancer therapy

Hanan Alyami  1 , Sitah Alharthi  2 , Ali Jaber Alqahtani  3 , Hasan Ebrahimi Shahmabadi  4 , Seyed Ebrahim Alavi  5
Affiliations

Enhanced antitumor efficacy of nanostructured lipid carrier co-loaded with docetaxel and 5-fluorouracil for targeted gastric cancer therapy

Hanan Alyami et al. Med Oncol. .

Abstract

This study presents nanostructured lipid carrier (NLC) co-loaded with Docetaxel (DCT) and 5-Fluorouracil (5-FU) as a targeted therapeutic approach for gastric cancer (GC). Using nanoprecipitation, NLC-DCT/5-FU were synthesized and exhibited an average particle size of 215.3 ± 10.4 nm, a polydispersity index (PDI) of 0.29, and a zeta potential of - 17.1 mV. Encapsulation efficiency reached 95.9% for DCT and 5-FU, with a loading efficiency of 11.2%. In vitro release studies demonstrated a biphasic release profile, with an initial burst and sustained release, achieving 85.6% DCT and 75.8% 5-FU release over 72 h. Cytotoxicity assays in MKN45 cells showed a significantly lower half-maximal inhibitory concentration (IC50) for NLC-DCT/5-FU (0.3 µM) compared to free DCT (3.9 µM) and free 5-FU (19.5 µM), indicating enhanced efficacy. In vivo evaluation in a GC mouse model confirmed substantial tumor volume reduction to 213 mm3 with NLC-DCT/5-FU treatment, compared to 432 mm3 with the free-drug combination. Systemic safety assessment showed minimal adverse effects, suggesting the nanoparticles' enhanced therapeutic index. These results demonstrate that NLC-based co-delivery systems could substantially improve the clinical outcomes of GC therapy.

Keywords: 5-Fluorouracil; Docetaxel; Drug delivery; Gastric cancer; Nanoparticles; Nanostructured lipid carrier.

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Conflict of interest statement

Declarations. Competing interests: The authors declare no competing interests.

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