title: A Novel Microspheres Formulation of Puerarin: Pharmacokinetics Study and In Vivo Pharmacodynamics Evaluations.
abstract: The aim of this study was to investigate the pharmacokinetics and pharmacodynamics of puerarin loaded carboxymethyl chitosan microspheres (Pue-CCMs). The differences in pharmacokinetics parameters of rats after intragastric administration of Pue-CCMs and puerarin were investigated using HPLC. To assess the protective effect of Pue-CCMs on myocardial injury in rats, serum levels of creatine kinase (CK), lactate dehydrogenase (LDH), total superoxide dismutase (T-SOD), and malondialdehyde (MDA) were measured, in addition to pathological examinations and immunohistochemical staining. Our present study has shown that the AUC0-t,Cmax,Tmax, MRT0-tof Pue-CCMs, and puerarin were 20.176 mg·h/L, 3.778μg/mL, 1 h, 4.634 h and 9.474 mg·h/L, 2.618μg/mL, 0.542 h, and 3.241 h, respectively. Pue-CCMs alleviated myocardial ischemic injury. Pretreatment with Pue-CCMs could significantly decrease CK, LDH, and MDA levels and increase T-SOD level in the serum. Pue-CCMs downregulated expression of the Bcl-2 associated X protein (Bax) and upregulated B-cell lymphoma-2 (Bcl-2) expression. Compared with puerarin group, the Pue-CCMs group could improve the oral bioavailability of puerarin. The protective effect of Pue-CCMs against myocardial injury was significantly greater than puerarin at the same dose. In summary, Pue-CCMs should be a qualified and promising candidate as a new oral preparation of puerarin.
authors.affiliation: College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an, Shaanxi 712046, China.
authors.forename: Xiao
authors.identifier: 0000-0001-6644-9191
authors.initials: X
authors.lastname: Song
authors.affiliation: College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an, Shaanxi 712046, China.
authors.forename: Xihui
authors.identifier: 0000-0003-0862-4750
authors.initials: X
authors.lastname: Bai
authors.affiliation: College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an, Shaanxi 712046, China.
authors.forename: Shiyu
authors.identifier: 0000-0001-5953-5470
authors.initials: S
authors.lastname: Liu
authors.affiliation: College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an, Shaanxi 712046, China.
authors.forename: Linjuan
authors.identifier: 0000-0003-1103-5607
authors.initials: L
authors.lastname: Dong
authors.affiliation: College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an, Shaanxi 712046, China.
authors.forename: Hui
authors.identifier: 0000-0003-3344-3978
authors.initials: H
authors.lastname: Deng
authors.affiliation: College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an, Shaanxi 712046, China.
authors.forename: Changli
authors.identifier: 0000-0002-9889-6524
authors.initials: C
authors.lastname: Wang