Preparation, characterization and pharmacokinetics of puerarin chitosan/sodium alginate oral nanoparticles / 中草药

ABSTRACT

Objective: To prepare and characterize puerarin chitosan/sodium alginate oral nanoparticles (Pur-CS/SA-NPs) and conduct its pharmacokinetics studies. Methods: Pur-CS/SA-NPs were prepared by self-assembly method, the morphology, particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, drug loading and microstructure of Pur-CS/SA-NPs suspension and lyophilized powder were characterized. To determine the concentration of puerarin in plasma after oral administration of nanoparticles to rats, an LC-MS/MS analysis method for puerarin was established, and its pharmacokinetic characteristics were investigated. Results: The morphology, structure and texture of Pur-CS/SA-NPs suspension and lyophilized powder were complete and fine, no new chemical bonds and crystals were formed. The particle size, PDI, Zeta potential, encapsulation efficiency, and drug loading of Pur-CS/ SA-NPs suspension were (208.327 ± 1.870) nm, 0.131 ± 0.006, (89.056 ± 1.680)% and (44.528 ± 0.840)%, respectively. The particle size, Zeta potential, encapsulation efficiency and drug loading of Pur-CS/SA-NPs lyophilized powder were (260.000 ± 0.475) nm, (47.300 ± 0.208) mV, (86.234 ± 0.873)% and (43.117 ± 0.234)%, respectively. The AUC0-24, AUC0-∞, tmax and Cmax of Pur-CS/SA- NPs were (833.067 ± 132.546) mg∙h/L, (844.919 ± 154.768) mg∙h/L, (1.000 ± 0.098) h and (236.318 ± 36.864) mg/L, respectively. The AUC0-24, AUC0-∞, tmax and Cmax of puerarin were (250.087 ± 32.156) mg∙h/L, (250.091 ± 28.398) mg∙h/L, (0.500 ± 0.031) h and (191.830 ± 17.963) mg/L, respectively. The AUC0-24, AUC0-∞, tmax and Cmax of Pur-CS/SA-NPs were 3.331, 3.378, 2.000, and 1.232 times of puerarin, respectively. Conclusion: The structure of Pur-CS/SA-NPs prepared by self-assembly method is stable. After oral administration, the AUC0-24, AUC0-∞ and tmax of the drug in the body are significantly increased, and the circulation time is relatively extended, which significantly improve bioavailability of puerarin.