BACKGROUND: Studies on transdermal administration have shown that puerarin can permeate rat skin rapidly with long-term drug delivery, but there are no reports demonstrating whether topical use of puerarin can provide a steady plasma concentration to produce therapeutic effects. The aim of the study is to evaluate the percutaneous penetration and plasma concentration of puerarin after transdermal administration in experimental rats. METHODS: The skin and plasma concentration of puerarin was quantified by microdialysis, and the recovery was determined by retrodialysis. Puerarin microdialysate concentrations were measured by on-line high-performance liquid chromatography (HPLC). Puerarin release from gels was determined by analysis of the amount of remaining drug after dermal application to hairless skin. RESULTS: The average recoveries of puerarin in the skin and plasma over an 8-hour period were 31.49% and 15.5%. Puerarin was rapidly absorbed with transdermal administration, with the C(max) values of 30.64 μg/mL and 3.53 μg/mL, the AUC0 t-values of 11.60 and 1.48 μg/mL per minute, for skin and plasma, respectively. CONCLUSIONS: The results indicate that the automated on-line microdialysis technique can be used to detect the skin and plasma pharmacokinetics of puerarin and that the use of skin gel can provide an effective means of puerarin administration.
BACKGROUND: Studies on transdermal administration have shown that puerarin can permeate rat skin rapidly with long-term drug delivery, but there are no reports demonstrating whether topical use of puerarin can provide a steady plasma concentration to produce therapeutic effects. The aim of the study is to evaluate the percutaneous penetration and plasma concentration of puerarin after transdermal administration in experimental rats. METHODS: The skin and plasma concentration of puerarin was quantified by microdialysis, and the recovery was determined by retrodialysis. Puerarin microdialysate concentrations were measured by on-line high-performance liquid chromatography (HPLC). Puerarin release from gels was determined by analysis of the amount of remaining drug after dermal application to hairless skin. RESULTS: The average recoveries of puerarin in the skin and plasma over an 8-hour period were 31.49% and 15.5%. Puerarin was rapidly absorbed with transdermal administration, with the C(max) values of 30.64 μg/mL and 3.53 μg/mL, the AUC0 t-values of 11.60 and 1.48 μg/mL per minute, for skin and plasma, respectively. CONCLUSIONS: The results indicate that the automated on-line microdialysis technique can be used to detect the skin and plasma pharmacokinetics of puerarin and that the use of skin gel can provide an effective means of puerarin administration.