Enhancement of the tumour inhibitory activity, in vivo, of diospyrin, a plant-derived quinonoid, through liposomal encapsulation

Diospyrin, a bisnaphthoquinonoid plant product, shows inhibitory activity against murine tumour in vivo and human cancer cell lines in vitro. Efforts have further been made to obtain synthetic derivatives of diospyrin with the objective of improved therapeutic effects. With the goal to reduce the toxicity towards normal cells and enhance the efficacy to tumour cells, diospyrin was encapsulated in liposomal vesicle and its antitumour potential was observed on the growth of Ehrlich ascites tumour in Swiss mice. It was found that the longevity of the tumour-bearing mice was significantly enhanced by treatment with liposomal diospyrin as compared with the free drug. Biochemical assay of liver function enzymes, viz. LDH, AP, GOT and GPT in blood serum of the tumour-bearing mice showed substantial alterations in the activity of these enzymes. These parameters were, however, restored to near normal level when the drug treatment was given encapsulated in a liposome. Histopathological studies on the liver tissues indicated a near normal pathological status in the treated animals despite being challenged by tumour cells. This study on diospyrin has shown, for the first time, an enhancement of its antitumour effect in vivo through liposomal encapsulation.