Preparation, dissolution and bioavailability of lycopene-Poloxamer 188 solid dispersion / 中国药科大学学报

ABSTRACT

Aim: To improve the solubility, dissolution and bioavailability of lycopene by preparing lycopene solid dispersion. Methods: Lycopene solid dispersion was prepared by the solvent method using Poloxamer 188 as car-rier. The physicochemical characteristics of the dispersion were determined by DSC, ultraviolet-visible spectra and the Dissolution Apparatus Ⅱ( Paddle). The oral bioavailability of lycopene was estimated in rat after oral dosing of lycopene solid dispersion or oil preparation. The plasma concentrations of lycopene in rats were determined by HPLC. The pharmacokinetic parameters were estimated by Kinetica software package. Results: In vitro dissolution of lycopene solid dispersion was greater than those of lycopene (raw material), and the physical mixture of lyco-pene and Poloxamer 188, partly due to the existing molecular state of lycopene in the dispersion. It was also found that the relative bioavailability of lycopene solid dispersion to lycopene oil preparation was (312. 2±96. 9) % . The optimal ratio of lycopene to carrier in the dispersion was about 1: 5. Conclusion: Lycopene-Poloxamer 188 solid dispersion could be prepared by the proposed simple, low-costly procedure resulting in improved bioavail-ability of lycopene, which is worthy of further development.