A224: Colon specific anticancer activity of vitamin E – quercetin coloaded curcumin nanoemulsion on HCT-116 xenographt nude mice model

Pankaj Dwivedi1,Prabhat Ranjan Mishra1

1CSIR-Central Drug Research Institue, Lucknow, India

Presenting date: Monday 2 November
Presenting time: 13.10-14.00

Background

Dietary polyphenols has emerged as a new concept in modulating human health. These includes common phytocompounds like curcumin (CUR) and quercetin, with antioxidant, antitumorigenic, anti-inflammatory, antibacterial and antifungal properties.

The objective of this study is to develop a nanostructured delivery system for co-delivery of vitamin E- quercetin with curcumin for the assessing anticancer activity invitro and invivo.

Method

To improve the pharmaceutical credentials of CUR it was co-delivered with quercetin in vit E nano delivery systems, overcoming limitations including intrinsically low aqueous solubility, bioavailability and cell uptake by Caco-2 cell line. CUR was incorporated in vitamin E nanoemulsion preloaded with quercetin using high pressure homogenization. The study was extended to anticancer effect on HCT-116 xenographt nude mice model.

Results

The in vitro release studies of optimized nanoemulsion(CUR-F-Nano) (particle size 256 ± 08 nm, polydispersity index (PDI) of 0.120, zeta potential of -41.1 ± 1.2 mV) demonstrated that nanoemulsion was able to sustain the release of CUR for up to 24 h. Minimal hemolysis and cellular toxicity demonstrated its suitability for intravenous administration. Significant induction of caspase dependent apoptosis in Caco-2 cells along with DNA catalating activity. Nanoemulsion CUR-F-Nano resulted in an improvement of plasma concentration (AUC(CUR-F-Nano)/AUC(CUR)= 8.80) of CUR in rats. Therapeutic experiments showed remarkably improved anticancer efficacy of CUR loaded nanoemlsion compare to CUR.

Conclusion

The findings suggest that the therapeutic performance of CUR with quercetin incorporated in vit E nanoemulsion improved to unexpected levels. Also, Vit E nanoemulsion have tremendous potential as a multifunctional colon specific delivery system.

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