Nanosuspensions study of gossypol: preparation, characterization and in situ single pass perfusion intestinal absorption / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare gossypol nanosuspensions and investigate their physicochemical properties and intestinal absorption behavior in rats. METHODS: Gossypol nanosuspensions were prepared by a high pressure homogenization method. Nanosuspensions' characteristics were investigated from particle size distribution, Zeta potential, particle morphology, crystal physical state, storage stability, saturation solubility, and in vitro release. Nanosuspensions' intestinal absorption characteristics were also observed in rats. RESULTS: The nanosuspensions existed as uniform rods. The mean particle size was (217±23) nm, and Zeta potential was -22.7 mV. Gossypol existed in crystalline form. Long-term stability test showed that gossypol nanosuspensions were stable at 4°C for 3 months. The experiment of intestinal absorption showed that the nanosuspensions could be absorbed through passive diffusion with significant variation at different sections. The experiment also showed that the absorption process was not affected by the efflux of P-glyco-protein (drug efflux pump). CONCLUSION: Gossypol nanosuspensions are successfully developed. The solubility in water and the release in vitro of the nanosuspensions are enhanced compared with the bulk drug of gossypol. This study provides a reference for the further pharmaceutical study of gossypol.