Enhanced gastric therapeutic effects of Brucea javanica oil and its gastroretentive drug delivery system compared to commercial products in pharmacokinetics study.

BACKGROUND:Brucea javanica oil (BJO), a traditional Chinese herbal medicine, has a variety of pharmacological activities and several BJO-related patent drugs have been widely used in China. PURPOSE:The objective of this study was to evaluate the gastric therapeutic effects of self-made BJO and its pharmaceutical potential to formulate novel BJO gastroretentive floating bead by comparing with commercial products. METHODS:BJO was extracted from the seeds of B. javanica, and its therapeutic effects were evaluated by comparing with commercial products in the treatment of human gastric cancer and gastric ulcer. Furthermore, the developed gastroretentive drug delivery system was evaluated by in vivo tests. A high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method for detecting the concentration of glycerol trioleate in the pharma-cokinetic study was applied. RESULTS:The antitumor activity of BJO was stronger than that of the marketed preparation; the 50% inhibitory concentration (IC50) values of BJO extracts on HGC27, SGC7901 and BGC823 gastric carcinoma were 0.3091, 1.736 and 2.743 μg/mL, respectively, whereas the values of marked BJO preparation were 15.26, 32.60 and 7.456 μg/mL, respectively. Histopathological studies demonstrated the ability of BJO to locally prevent and treat absolute ethanol-induced gastric ulcer. Developed BJO gastroretentive floating bead showed a satisfactory in vivo study. The highest glycerol trioleate concentration in the stomach after taking BJO gastroretentive floating bead was nearly two times higher when compared to the marketed BJO soft capsule. CONCLUSION:Self-made BJO has a strong therapeutic effect on the stomach, and gastroretentive drug delivery system can be a promising approach to prolong and enhance its therapy ability when treating gastric diseases.