Mechanisms of microemulsion enhancing the oral bioavailability of puerarin: comparison between oil-in-water and water-in-oil microemulsions using the single-pass intestinal perfusion method and a chylomicron flow blocking approach

Abstract

Tian-Tian Tang,1,2,3 Xiong-Bin Hu,1,2,3 De-Hua Liao,1,2,3 Xin-Yi Liu,1,2,3 Da-Xiong Xiang1,2,31Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha, People's Republic of China; 2Institute of Clinical Pharmacy, The Second Xiangya Hospital, Central South University, Changsha, People's Republic of China; 3Key Laboratory for New Technology of Chinese Medicine Preparations of Hunan Province, Changsha, People's Republic of ChinaAbstract: The purpose of the present work was to determine the mechanisms by which microemulsions (MEs) enhance the oral bioavailability of puerarin. The in situ perfusion method was used in rats to study the absorption mechanisms of an oil-in-water (O/W) microemulsion (O/W-ME) and a water-in-oil (W/O) microemulsion (W/O-ME). The possibility of lymphatic transport of the MEs was investigated using a chylomicron flow blocking approach. The results for the absorption mechanisms in the stomach and intestines indicated that the absorption characteristics of the O/W-ME and W/O-ME depend on the segment. The W/O-ME had higher internal membrane permeability than the O/W-ME. The results of the lymphatic transport analyses showed that both the O/W-ME and W/O-ME underwent lymphatic transport and that this pathway was a major contributor to the oral bioavailability of MEs. Furthermore, the type of ME can significantly affect the absorption of puerarin through the lymphatic system due to the oil content and the form of the microemulsion after oral administration. In conclusion, these data indicate that microemulsions are an effective and promising delivery system to enhance the oral bioavailability of poorly water-soluble drugs.Keywords: microemulsion, lymphatic transport, oral bioavailability, chylomicron