In-Vivo Pharmacokinetics Study Of Curcumin Benzathiazole Analog And Apoptosis Assay In Mda-Mb 231 Cell Line For Its Nanoparticle

Abstract

Objectives

Background

Curcumin is a popular natural compound with numerous pharmacological benefits, including showing activity against several cancers. Despite its anticancer potential, it is less desirable due to two major issues relating to its poor bioavailability, and rapid metabolism. To overcome these drawbacks and boost efficacy, we prepared a curcumin analogue (BEN) that was loaded with chitosan nanoparticles and evaluated for anti-breast cancer activity.

Methods

The oral bioavailability of BEN was determined in rabbits. The nanoparticles were prepared with chitosan and sodium tripolyphosphate using the ionic gelation method. The prepared nanoparticles were evaluated by UV, FTIR, particle size analyzer, zeta potential, morphology of particles, drug release and drug entrapment efficiency. MTT assay and apoptosis study were carried out to find its efficacy towards MDA-MB-231(breast cancer) cell line.

Results

The pharmacokinetic parameters such as Cmax, Tmax, T1/2, AUC0–t, AUC0–∞, and MRT were determined from the plasma concentration-time profile of the curcumin benzothiazole. The nano formulated BEN has particle size in the range of 50 to 200 nm and  the zeta potential ranges from -30 to +30 mV. Drug release was about 70 % at pH 5.5 and ~45 % at pH 7.4. Nano-BEN exhibited anti-cancer activity in MDA-MB cell line.

Conclusion

This study suggested that the synthesis of a curcumin analogue and its incorporation into chitosan nanoparticles could enhance drug release and provide a practical solution to curcumin’s poor bioavailability, and which will be confirmed by in vivo studies.