酒石酸长春瑞滨热敏脂质体药效学和组织分布研究

Study on Pharmacodynamics and Biodistribution of Vinorelbine Bitartrate Thermosensitive Liposomes

目的考察酒石酸长春瑞滨热敏脂质体在荷瘤裸鼠体内的分布特征及抑瘤情况。方法建立人卵巢癌SK-OV-3裸鼠移植瘤模型,比较研究酒石酸长春瑞滨热敏脂质体和注射液对移植瘤生长的抑制作用和体内组织分布情况。结果与酒石酸长春瑞滨注射液相比,相同剂量的酒石酸长春瑞滨热敏脂质体可以显著增强其抑瘤效果;同时在局部加热后的肿瘤组织中的药物浓度约为注射液组的4倍。结论酒石酸长春瑞滨热敏脂质体结合温和的热疗可明显的提高肿瘤局部的药物浓度,显著增强其抑瘤效果。

OBJECTIVE To investigate the tissue distribution and pharmacodynamics of viuorelbine bitartrate thermosensi- tive liposomes. METHODS Subcutaneous xenotransplanted tumor model of human ovarian carcinoma SK-OV-3 in nude mice was established. The tumor inhibitory efficacy and biodistribution of drug were evaluated in nude mice by intravenous ad- minstration with vinorelbine bitartrate thermosensitive liposomes and vinorelbine bitartrate injection. RESULTS The inhibi- tion rate of vinorelbine bitartrate thermosensitive liposomes was remarkably higher than that of injection at same dose. Moreo- ver, The drug concentration in heated tumor of mice administrated with vinorelbine bitartrate thermosensitive liposomes was a- bout 4 fold compared with that of mice administrated with injection. CONCLUSION Vinorelbine bitartrate thermosensitive liposomes combined with hyperthermia could significantly increase drug concentration in local tumor tissue and promote tumor inhibitory efficacy.