Berberine chloride (BBR) is a natural isoquinoline alkaloid extracted from medicinal herbs. It has been reported that the intestinal absorption of BBR is very low. In this study, the absolute bioavailability of BBR was studied, and the enhancing effects of D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) on intestinal absorption were investigated in rats. BBR injection was administrated via the femoral vein at a dose of 1.0 mg kg(-1) in intravenous group, and BBR oral formulations were administrated by oral gavage at a dose of 100 mg kg(-1) in BBR control (control) group and BBR-TPGS (test) group, respectively. The result showed that BBR had a very low absolute bioavailability of 0.68%, and TPGS could enhance intestinal absorption of BBR significantly. TPGS at a concentration of 2.5% could improve peak concentration (C(max)) and area under the curve (AUC(0-36)) of BBR by 2.9 and 1.9 times, respectively. The absorption enhancing ability of TPGS may be due to its ability to affect the biological activity of P-glycoprotein and thereby reduce the excretion of absorbed BBR into the intestinal lumen. This study indicated that absolute bioavailability of BBR was 0.68% in rats, and TPGS was a good absorption enhancer capable of enhancing intestinal absorption of BBR significantly.

The incidence of malignant tumours is rising worldwide. Cancer is regarded as the leading cause of death and the most key obstacle to improve life expectancy in every country of the world in the 21st century. 1 Tumour is a new organism formed by the proliferation of local tissue cells under the action of various tumorigenic factors. The development of cancer consists of a number of complex stages of initiation, progression and promotion, in which the stage of progression is invertible which seems to be the phase for the most appropriate drug intervention. Although there are different types therapies targeting cancers, such as surgical resection, radiotherapy, chemotherapy, immunotherapy, biotherapy therapy, molecular-targeted therapy and treatment of TCM, however, not every therapy achieves the expected optimal effect results. For instance, surgical resection can remove the tumour, the risk of advanced cancer is increased, and the survival rate is reduced. Clinical combination of first-line chemotherapy drugs and radiotherapy can prevent the progress of cancer to some extent, but they may cause serious toxic effects, affect the metabolism and proliferation of normal tissues, and reduce the life quality of patients.

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