Enhanced water dispersibility of Curcumin Encapsulated in Alginate-Polysorbate 80 Nano Particles and Bioavailability in Healthy Human volunteers.

Curcumin loaded alginate - polysorbate 80 nanoparticles prepared by ionotropic gelation method, successfully entrapped curcumin, exhibiting higher encapsulation efficiency nearing - 95%. Nano particles Produced were in the size range 105-383 nm and the Zeta potential found to be in the range of 150-200 mV. Formulations exhibited very low dissolution in Simulated Gastric fluid (SGF) & Simulated Intestinal fluid (SIF), but major portion got released in SCF which is attributed to the digestibility of alginate in Simulated Colonic fluid (SCF) under the influence of colonic micro flora which is not present in stomach or small intestine. Based on the physical stability of nanosuspension (number of days of no settling), we have chosen ZC as the optimized formulation. FTIR and DSC observations revealed the successful entrapment of curcumin in alginate polysorbate-80 nanoparticles. The nanoparticles of Zc formulation were more spherical, discrete and homogeneous. Nano particles could be transformed into easily re-dispersible powder form either by freeze drying / vacuum concentration or spray drying for application in nutraceuticals and controlled drug delivery systems. In healthy human volunteers the oral bioavailability (AUC) of curcumin increased 5-fold after the consumption of curcumin nanosuspension compared to curcumin suspension. Maximum plasma concentration Cmax - 636 ± 122 ng / ml was observed at tmax - 2h for nanosuspension, whereas Cmax-87.7 ± 17.9 ng / ml at tmax - 4h for suspension. Elimination rate constant found to be similar for both cur cumin suspension and curcumin nanosuspension which signified unaltered elimination profiles irrespective of formulation design. Both curcumin suspension and curcumin nanosuspension were safe and well tolerated and may thus be useful in the prevention or treatment of various inflammatory diseases of mankind.