Objective: To investigate pharmacokinetics and tissue distribution of gossypol nanosuspensions(GP-NS) in mice. Method: HPLC was established to determine the concentration of gossypol in serum and different tissues of mice.After tail administration of GP-NS and gossypol solution

their pharmacokinetics and tissue distribution differences were compared. Result: After administration of GP-NS

area under plasma concentration time curve (AUC0-∞) was (18 792.56±2 304.43) μg · L-1 · h-1

in vivo residence time (MRT0-∞) was (21.82±1.60)h

apparent volume of distribution (V) was (0.75±0.16) L · kg-1

clearance(CL) was (1.37±0.37) L · kg-1 · h-1and maximum plasma concentration (Cmax) was (17 589.81±3 034.14) μg · L-1.Values of relative uptake rate (Re)in the liver

heart

spleen

lung and kidneywere 1.44

3.21

12.19

1.88 and 6.54

respectively. Conclusion: GP-NS can significantly increase the level of gossypol concentration in mice and improve its bioavailability.GP-NS is helpful for gossypol to reach a long circulation time and is hopeful to be its novel drug delivery system.