ABSTRACT
Objective: To develop adriamycin liposome (AL) , adriamycin long circulating liposome (ALCL) and adriamycin long circulating temprerature-sensitive liposome ( ALTSL) and to study their anti-tumor effects on tumor-bearing mice. Methods: The antitumor activity was observed using the tumor weight as index. The life prolongation rate of mice was calculated according to the tumor-bearing mice survival time. The tissue distribution of adriamycin was determined by HPLC method. Tumor, heart, liver and kidney tissue of the tumor-bearing mice, were sliced and prepared to observe the tissue pathology differences. Results: Compared with free adriamycin, the anti-tumor effects of ALCL and ALTSL were remarkably increased. Their tumor growth inhibitory rates were 57. 8% and 67. 0% respectively. The study of pharmacoki-netics indicated that the adriamycin concentrations were remarkably higher in tumor tissue and blood,lower in heart and lung tissue of ALCL and ALTSL groups when compared with the free ADM group; The pathology slices indicated that tumor cells in the ALTSL group with hyperthermia were mostly destroyed; the cardiac muscle cells in the ALTSL group were similar to the normal cardiac muscle. Conclusion: ALCL and ALTSL remarkably increased the adriamycin concentration on the tumor site, significantly enhanced the anti-tumor effects, decreased the side-effects (such as cytotoxicity) when compared with free ADM, they also significantly prolonged the survival time of the tumor-bearing mice.
ABSTRACT
Aim To study the effects of dipfluzine (Dip) on cell apoptosis after focal cerebral ischemia-reperfusion injury in rats. Methods Endothelin-1 induced focal cerebral ischemia-reperfusion model in rat was used in experiment. The cell apoptosis, the expressions of Bcl-2 and Bax proteins were observed by flow cytometric analysis. Results The tissues from the solvent group showed remarkably high apoptotic percentages with(9.34?1.22)% in cortex and(10.58?1.44)% in striatum, respectively, in contrast with(1.26?0.15)% in cortex and(2.50?0.35)% in striatum in sham group. Dipfluzine could decrease the cell apoptosis in cortex and striatum and showed a close correlation with the dose increment, which were (7.92?0.76)% in 10mg?kg -1 group, (6.78?0.77)% in 20 mg?kg -1 group, and (6.00?0.71)% in 40 mg?kg -1 group in cortex (r=0.9559, P0.05). The determination of Bcl-2 and Bax by flow cytometric analysis indicated that sham group showed high expression of Bcl-2 both in cortex and striatum and the ratio of Bcl-2 and Bax were the highest,they were 1.30?0.08 in cortex and 1.64?0.10 in striatum, respectively. The expression of Bax in solvent group was increased and the the ratio of Bcl-2 and Bax were 1.03?0.12 in cortex and 1.00?0.04 in striatum, significantly lower than those in sham group (P
