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.