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。
Abstract
OBJECTIVE To investigate the tissue distribution and pharmacodynamics of vinorelbine bitartrate thermosensitive 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 adminstration with vinorelbine bitartrate thermosensitive liposomes and vinorelbine bitartrate injection. RESULTS The inhibition rate of vinorelbine bitartrate thermosensitive liposomes was remarkably higher than that of injection at same dose. Moreover, The drug concentration in heated tumor of mice administrated with vinorelbine bitartrate thermosensitive liposomes was about 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.
关键词
酒石酸长春瑞滨 /
热敏脂质体 /
温和热疗 /
卵巢癌
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Key words
vinorelbine bitartrate /
thermosensitive liposomes /
hyperthermia /
ovarian carcinoma
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中图分类号：
R965
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参考文献
HUANG H S, GONG W, ZHANG H, et al. Preparation and entrapment efficiency of vinorelbine tartrate thermo-sensitive liposomes . Chin Pharm J(中国药学杂志), 2010, 45(16):1250-1254. YATIVIN M B, WEINSTEIN J N, DENNIS W H, et al. Design of liposomes for enhanced local release of drugs by hyperthermia. Science, 1978, 202(4374):1290-1293. KONING G A, EGGERMONT A M, LINDNER L H, et al. Hyperthermia and thermosensitive liposomes for improved delivery of chemotherapeutic drugs to solid tumors. Pharm Res, 2010, 27(8):1750-1754. KONO K, OZAWA T, YOSHIDA T, et al.Highly temperature-sensitive liposomes based on a thermosensitive block copolymer for tumor-specific chemotherapy. Biomaterials, 2010, 31(27):7096-7105. KARINO T, KOGA S, MAETA M. Experimental studies of the effects of local hyperthermia on blood flow, oxygen pressure and pH in tumors. Jpn J Surg, 1988, 18(3):276-283. HUANG S K, STAUFFER P R, HONG K, et al. Liposomes and hyperthermia in mice:Increased tumor uptake and therapeutic efficacy of doxorubicin in sterically stabilized liposomes. Cancer Res, 1994, 54 (8):2186-2191. GONG W, WANG Z Y, LIU N, et al. Improving efficiency of adriamycin crossing blood brain barrier by combination of thermosensitive liposomes and hyperthermia. Biol Pharm Bull, 2011, 34(7):1058-1064.
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脚注
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基金
国家十二五重大专项资助项目(2012ZX09301003-001-009)
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