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

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.

• Authors: Pu Guo, Chao Pi, Shijie Zhao, Shaozhi Fu, Hongru Yang, Xiaoli Zheng, Xiaomei Zhang, Ling Zhao, Yumeng Wei
• Journal: Expert opinion on drug delivery (Expert Opin Drug Deliv) Vol. 17 Issue 10 Pg. 1473-1484 (10 2020) ISSN: 1744-7593 [Electronic] England
• PMID: 32749895 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Curcumin
• Fluorouracil

Topics

• Animals
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Curcumin (administration & dosage, pharmacology)
• Fluorouracil (administration & dosage)
• Hep G2 Cells
• Humans
• Liver Neoplasms (drug therapy)
• Mice
• Mice, Inbred BALB C
• Mice, Nude
• Rats
• Rats, Sprague-Dawley