Abstract:To study the pharmacokinetic and bioequivalence of Arparaginase Hyaluronic acid-graft-poly(ethylene glycol) / γ-cyclodextrin nanocapsules (AHRPs) in SD rats. We observed the image of AHRPs under the transmission electron microscopy. The size, zeta potential, entrapment efficiency were detected. The activity of AN was assayed after respectively intravenous injecting AHRPs and free AN in rats. The pharmacokinetic parameters were calculated by software DAS 2.1.1, then the bioequivalence was judged. After calculating, the average particle size was (410.30±3.20) nm, zeta potential was (-31.40±1.65) mV, average entrapment efficiency was (42.80±4.37)%. AUC(0-48h) of AHRPs and free AN was (104.01 ±1.68) U/mL*h and (46.38 ±1.98) U/mL*h, AUC(0-∞) was (131.03 ±19.67) U/mL*h and (51.44 ±3.01) U/mL*h, t1/2 was (4.31±1.53) h and (1.86±0.38Z) h, respectively. Compared with free AN, the AUC(0-48h), AUC(0-∞) and t1/2 of AHRPs increased 2.24, 2.55 and 2.32 times, respectively. The 90% confidential intervals of AUC(0-48h), AUC(0-∞) and Cmax of tested formulation were 77.1%~78.7%，76.7%~78.3%，98.9%~100.5%, respectively. AHRPs can improve the bioavailability and extend the biological half-life of AN in rats. AHRPs and free AN are not bioequivalent.
