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Oral co-delivery nanoemulsion of 5-fluorouracil and curcumin for synergistic effects against liver cancer

Pu Guo, Chao Pi, Shijie Zhao, Shaozhi Fu, Hongru Yang, Xiaoli Zheng, Xiaomei Zhang, Ling Zhao, Yumeng Wei

2020Expert Opinion on Drug Delivery44 citationsDOI

Abstract

Background A novel nanoemulsion (CU/FU-LN) was developed as an oral 5-fluorouracil and curcumin co-delivery system for synergistic efficacy against liver cancer.Methods MTT assay, confocal laser scanning microscope, and H&E staining were utilized to establish the efficacy and safety of CU/FU-LN.Results The AUC(0-t) of CU/FU-LN was 8.85-fold and 8.59-fold greater than those of CU and FU, respectively. The IC50 of CU/FU-LN was 4.6-fold and 4.9-fold lower than those of FU and CU in HepG2 cells, respectively. In vivo anti-tumor trials, the tumor inhibition rate was significantly elevated by CU/FU-LN (49.29%), compared 24.84% and 4.72% for FU and CU, respectively. Ki-67 immunohistochemical analysis revealed that CU/FU-LN had an obvious anti-proliferation effect. The IC50 of CU/FU-LN in L02 cells was 1.51-fold and 2.60-fold higher than those of CU and FU, respectively. Certain vital organs in the mice of the CU/FU-LN group showed markedly fewer lesions than those of the CU, FU, and CU+FU groups. The CU/FU-LN treatment caused no significant change in mouse body weight relative to the control group (P > 0.05). Conclusions We successfully prepared a promising co-delivery platform for the synergistic treatment of liver cancer and it has a comparatively enhanced efficacy and mitigated toxicity.

Topics & Concepts

CurcuminIn vivoFluorouracilPharmacologyIC50MTT assayLiver cancerChemistryToxicityIn vitroMedicineCancerBiochemistryInternal medicineBiologyBiotechnologyCurcumin's Biomedical ApplicationsNatural product bioactivities and synthesisRNA Interference and Gene Delivery