Effect of perillyl alcohol-loaded mitochondria-targeted liposomes(POH/DPT-LN)on breast cancer MDA-MB-231 cells
Objective:To prepare perillyl alcohol(POH)-loaded distearoyl phosphoethanolamine(DSPE)-poly-ethylene glycol(PEG)-(3-carboxy propyl)triphenyl phosph-onium bromide(TPP)-liposomes(POH/DPT-LN),and to investigate the physicochemical characteristics,mitochondrial targeting and the inhibitory effect on breast cancer MDA-MB-231 cells.Methods:POH/DPT-LN was prepared by thin film dispersion method.Cell counting kit-8(CCK-8)assay,cell scratch experiment,Transwell,apoptosis experiment,JC-1 staining experiment and western blotting were used to evaluate the mitochondrial targeting and tumor-inhibitory effects of drug-loading systems.Results:POH/DPT-LN was uniform and round,with an average particle size of(141.0±0.8)nm,zeta po-tential of(29.5±2.8)mV,PDI of(0.185±0.006),encapsulation efficiency and drug loading capacity of(88.6±1.8)%and(17.7±0.3)%,respectively.The IC50 of POH/DPT-LN was 63.32µg/mL,and it had a good inhibitory effect on the growth of MDA-MB-231 cells.Compared with the POH monotherapy group,the migration ability of MDA-MB-231 cells in the POH/DPT-LN group was significantly weakened,and the effect on inhibiting cell invasion was obvious(P＜0.01).POH/DPT-LN group increased the accumulation concentration of POH in the mitochondria and enhanced the cell killing effect(P＜0.01).POH/DPT-LN can significantly increase the protein expression of pro-apoptotic P53,Bax,Caspase-3 and reduce the protein expression of anti-apoptotic Bcl-2.Con-clusion:POH/DPT-LN has good encapsulation efficiency and drug loading capacity.It can target POH drugs into mitochondria,more effectively inhibit the proliferation of MDA-MB-231 breast cancer cells,and enhance the an-ti-tumor effect of drugs.
万方数据
维普
