ABSTRACT
Objective: To optimize the synthesis of PEGylated puerarin (PEG-PUE) by orthogonal test with multi-index evaluation. Methods: The research has focused on the optimized interacting factors of the synthetic process of PEG-PUE by HPLC, such as ratio of PEG and PUE, catalyst DMAP dosage, and reaction time, using the purity, drug loading, and yield of PEG-PUE as evaluation indexes. Results: The optimum synthesis conditions of PEG-PUE were as follows, PEG-EDC-PUE-DMAP (1 : 1.2 : 1.2 : 0.3) and reaction time 12 h. Conclusion: The optimum synthesis condition of PEG-PUE is reasonable, as well as feasible.
ABSTRACT
Objective: To study the formulation of puerarin (PUE) self-microemulsifying drug delivery system (SMEDDS). Methods: The optimum formulation of PUE SMEDDS was screened by test of solubility, compatibility of oil and surfactant, and pseudo-ternary phase diagram, and the prescription of PUE SMEDDS was optimized by particle size, self-microemulsifying time, and drug loading; The physicochemical characteristics and stability were also determined. Results: The optimum SMEDDS composed of Miglyol 812N (19.0%), oleic acid (19.0%), polysorbate 80 (19.0%), EL-35 (19.0%), 1, 2-propanediol (19.0%), and puerarin (5.0%). The particle size was (17.28 ± 0.24) nm, and self- microemulsifying time was less than 120 s; The appearance, content of PUE, particle size, and self-microemulsifying time had no obvious changes under room temperature storage for six months. Conclusion: The acquired PUE SMEDDS is stable with small particle size, which meets the needs of good SMEDDS formulation.
ABSTRACT
Object To investigate the effect of puerarin (Pue) on renal protein kinase C (PKC) activity, kidney structure and function in diabetic rats. Methods STZ-induced diabetic rats were randomly divided into five groups: Diabetic rats model group (DM), Pue (500, 250, 125 mg/kg) treatment group, and VitE group, in addition, normal rats for control group. All rats were given by ig for 12 weeks. Kidney function and kidney index were determined; The PKC activity was measured by ELISA. The excretion of microalbuminuria (MAU) was measured by radio-immunoassay, and kidney tissue was observed by light-microscope and transmission electron microscope. Results The excretion of MAU, kidney index (kidney weight/body weight) and PKC activity in diabetic rats were significantly increased. The excretion of MAU, and PKC activity were markedly decreased in Pue treatment group, and kidney pathologic changes of diabetic rats in Pue treatment group were improved. Conclusion Pue can ameliorate early kidney hy-perdynamic abnormality in diabetic rats, possess protective effect on kidney of diabetic rats, whose mechanism may be associated partly with a down-regulation of PKC activity.