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Oral co-delivery nanoemulsion of 5-fluorouracil and curcumin for synergistic effects against liver cancer.
Expert Opinion on Drug Delivery ( IF 5.0 ) Pub Date : 2020-08-04 , DOI: 10.1080/17425247.2020.1796629
Pu Guo 1 , Chao Pi 1 , Shijie Zhao 1 , Shaozhi Fu 2 , Hongru Yang 3 , Xiaoli Zheng 4 , Xiaomei Zhang 5 , Ling Zhao 1 , Yumeng Wei 1
Affiliation  

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.



中文翻译:

5-氟尿嘧啶和姜黄素的口服共输送纳米乳剂,具有抗肝癌的协同作用。

摘要

背景

一种新型的纳米乳剂(CU / FU-LN)被开发为口服5-氟尿嘧啶和姜黄素共递送系统,具有抗肝癌的协同功效。

方法

利用MTT法,共聚焦激光扫描显微镜和H&E染色确定CU / FU-LN的有效性和安全性。

结果

CU / FU-LN的AUC (0-t)分别比CU和FU大8.85倍和8.59倍。在HepG2细胞中,CU / FU-LN的IC 50分别比FU和CU低4.6倍和4.9倍。在体内抗肿瘤试验中,CU / FU-LN显着提高了肿瘤抑制率(49.29%),而FU和CU分别为24.84%和4.72%。Ki-67免疫组织化学分析表明,CU / FU-LN具有明显的抗增殖作用。IC 50L02细胞中CU / FU-LN的含量分别比CU和FU高1.51倍和2.60倍。CU / FU-LN组小鼠的某些重要器官的病变明显少于CU,FU和CU + FU组。相对于对照组,CU / FU-LN处理不会引起小鼠体重的显着变化(P > 0.05)。 

结论

我们成功地为肝癌的协同治疗成功地准备了一个有希望的共同交付平台,它具有相对增强的疗效和减轻的毒性。

更新日期:2020-08-04
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