Powder Technology, Vol.301, 641-648, 2016
Enhanced solubility, dissolution, and absorption of lycopene by a solid dispersion technique: The dripping pill delivery system
Lycopene, a natural, hydrophobic compound derived from tomatoes, has attracted considerable attention due to its various benefits such as being an anti-oxidant, anti-cancer, and anti-hyperlipidemic agent. The insolubility of lycopene is a major obstacle that leads to poor bioavailability. We aimed to optimize a straightforward, promising approach utilizing a solid dispersion technique, named the dripping pill delivery system, for improving the absorption of lycopene. The polyethylene glycol 6000-based dripping pills were prepared by the hot melt method with rapid cooling. A 3(2) full factorial design was employed to optimize the effects of the independent variables, Cremophor EL and Tween 80, on the solubility, dissolution, and stability tests. The physicochemical characteristics and interaction were investigated by the disintegration test, scanning electron microscope, differential scanning calorimetry, and Fourier transform infrared spectroscopy. The in vivo experiment was carried out to verify the usefulness of the developed formulae. The optimal dripping pill formulae elevated the solubility and dissolution of lycopene, which was confirmed to be formed in an amorphous state. Furthermore, the optimal dripping pill exhibited an approximate 6-fold improvement in bioavailability. (C) 2016 Elsevier B.V. All rights reserved.