3种脂质体-抗肿瘤药复合物的制备及急性毒性  

Preparation of Three Kinds of Antitumor Drugs Liposomes Complex and Their Acute Toxicity

作　　者：陈燕凌[1] 殷凤峙[1] 陈碧芬[2] 高凌云[2] 

机构地区：[1]福建医科大学附属协和医院,福建省肝胆外科研究所福州350001 [2]福建医科大学病理解剖学教研室,福州350004

出　　处：《福建医科大学学报》2001年第1期10-12,15,共4页Journal of Fujian Medical University

摘　　要：目的　筛选较理想的脂质体 -抗肿瘤制品 ,进而应用于 期临床肿瘤患者的治疗。　方法　制备脂质体 ,并包封 3种抗肿瘤药物 (表阿霉素、顺铂和高三尖杉酯碱 ) ,形成脂质体 -抗肿瘤药复合物 ,检测其理化性质、包封率及毒性反应。　结果　脂质体直径为 0 .1～ 0 .4μm的单层膜囊泡 ;3种药物包封率分别为 91.2 8% ,47.7%和47.6 2 %。体外培养细胞经包封药物作用后 2 4h存活率分别为 6 0 % ,70 %和 70 % ,明显高于单纯药物作用。经小鼠尾静脉注射后 L D5 0 值高于无脂质体包封的原药。　结论　制备的脂质体 -抗肿瘤药复合物为较理想的制品 。Objective\ To screen out 3 kinds of liposome\|entrapped antitumor drugs for a later phase Ⅰ clinical trials.Methods\ To prepare liposomes with conjugated lipids as a carrier using a modified skillto form the complex of liposome\|entrapped epirubucin, cisplatin or homoharring tonine.\ The physiochemical properties and the entrappment rate were checked.\ The acute toxicity was determined also.\ Results\ The liposomes were unilamellar vesicles ranged from 0.1~0.4 μm in diameter.\ The entrappment rate for three liposome\|entrapped drugs were 91 28%, 47 7% and 47 62% respectively.\ The acute toxicities for the survival rate of culture cells in 24 h were 60%, 70%, and 70% respectively.\ To compare with free drugs, the survival time of experimental mice prolonged and the toxic reaction decreased.\ Conclusion\ These liposome\|entrapped antitumor drugs are good agents for the patient with tumor in phase Ⅰ clinical chemotherapy.

关 键 词：脂质体 抗肿瘤药 急性毒性 制备 肿瘤 治疗 

分 类 号：R730.5[医药卫生—肿瘤]