A Novel Microspheres Formulation of Puerarin: Pharmacokinetics Study and In Vivo Pharmacodynamics Evaluations

Abstract EN

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–t of Pue-CCMs, and puerarin were 20.176 mg·h/L, 3.778 μg/mL, 1 h, 4.634 h and 9.474 mg·h/L, 2.618 μg/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.