Transport mechanism of puerarin and the influence of Angelica dahurica extracts on absorption of puerarin in Caco-2 cell model / 中国药学杂志

ABSTRACT

OBJECTIVE: To study the transport properties of puerarin across Caco-2 cell membrane and determine the influence of Radix Angelicae Dahuricae extract on the transport of puerarin using the well-characterized, human-based intestinal Caco-2 cell model as a platform. METHODS: The characteristics of the bidirectional transport of puerarin was investigated. The effects of time, drug concentration, pH, P-gp inhibitor and MRP inhibitor on the absorption of puerarin were observed. Then the influence of the extract of Radix Angelicae Dahuricae on the transport of puerarin was studied. Drug concentration was measured by HPLC and the apparent permeability coefficients (Papp) and apparent permeability ratio (PDR) were calculated. RESULTS: Puerarin was better absorbed in weak acid of pH5.5. The Ka and Papp of puerarin was of concentration-dependent, and the transport showed saturation with increasing time and concentration. When P-gp/MRP inhibitors were added to the model, the Papp AP-BL of puerarin in Caco-2 cell increased and the PappBL-AP/PappAP-BL puerarin reduced. The absorption of puerarin was improved when combined with Radix Angelicae Dahuricae. CONCLUSION The intestinal absorption of puerarin in Caco-2 cell monolayer model is mainly a passive diffusion process, and active transportation mediated by P-gp and MRP transporter is also involved. Radix Angelicae Dahuricae can enhance the intestinal absorption of puerarin.