Curcumin-polymeric nanoparticles against colon-26 tumor-bearing mice: cytotoxicity, pharmacokinetic and anticancer efficacy studies

Abstract

Context: Curcumin (CUR), can inhibit proliferation and induce apoptosis of tumor cells, its extreme insolubility and limited bioavailability restricted its clinical application.

Objective: An innovative polymeric nanoparticle of CUR has been developed to enhance the bioavailability and anti-cancer efficacy of CUR, in vitro and in vivo.

Materials and methods: Cationic copolymer Eudragit E 100 was selected as carrier, which can enhance properties of poor bioavailable chemotherapeutic drugs (CUR). The CUR-loaded Eudragit E 100 nanoparticles (CENPs) were prepared by emulsification-diffusion-evaporation method. The in vitro cytotoxicity study of CENPs was carried out using sulphorhodamine B assay. Pharmacokinetic and anti-cancer efficacy of CENPs was investigated in Wister rats as well as colon-26 tumor-bearing mice after oral administration.

Results: CENPs showed acceptable particle size and percent entrapment efficiency. In vitro cytotoxicity studies in terms of 50% cell growth inhibition values demonstrated ∼19-fold reduction when treated with CENPs as compared to pure CUR. ∼91-fold increase in C_max and ∼95-fold increase in AUC_0–12h were observed indicating a significant enhancement in the oral bioavailability of CUR when orally administered as CENPs compared to pure CUR. The in vivo anti-cancer study performed with CENPs showed a significant increase in efficacy compared with pure CUR, as observed by tumor volume, body weight and survival rate.

Conclusions: The results clearly indicate that the developed polymeric nanoparticles offer a great potential to improve bioavailability and anticancer efficacy of hydrophobic chemotherapeutic drug.

• Anti-cancer efficacy
• bioavailability
• colon-26 cells
• cytotoxicity
• polymeric nanoparticles

Acknowledgements

First author acknowledges Tata Memorial Centre for Treatment, Research and Education in Cancer (ACTREC), Mumbai, India, for providing experimental facilities for in vitro cytotoxicity and in vivo anticancer efficacy studies.

Declaration of interest

The authors declare that they have no conflicts of interest to disclose. The first author gratefully acknowledges financial support (DST-INSPIRE Fellowship, IF 110057) from Department of Science and Technology, Govt. of India, New Delhi.