Study on pharmacokinetic profile of PVP-coated norcantharidin-chitosan nanoparticles in rats by HPLC-MS/MS

Objective:To establish an HPLC-MS/MS method for the determination of norcantharidin(NCTD),and to study the bioavailability and pharmaceutical characteristics of PVP-coated NCTD-Chitosan nanoparticles(PVP-NCTD-NP) in SD rats.Methods:Negative electrospray ionization(ESI-) with selected multi reaction monitoring(MRM) mode was used.Perchloric acid was adopted as protein precipitation agent.NCTD concentrations in rat plasma were determined after intravenous injection of PVP-NCTD-NP and NCTD solution.Pharmacokinetic parameters were calculated by 3P97 program.Results:The linear range was 0.1025～10.25μg·mL-1(r=0.9992),and the detection limit was 50ng·mL-1.The concentration-time data was fitted to a two-compartment model,while the relative bioavailability of PVP-NCTD-NP to NCTD was 325.5%.Conclusion:The method is sensitive,accurate,highly selective,and applicable to the pharmacokinetic study of NCTD.PVP-NCTD-NP formulation can promote the absorption of NCTD,and its bioavailability is significantly improved.