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一种刚性非磷脂脂质体药物递送系统的药理功效。

The pharmacological efficacy of a rigid non-phospholipid liposome drug delivery system.

作者信息

Patel K R, Li M P, Schuh J R, Baldeschwieler J D

出版信息

Biochim Biophys Acta. 1984 Jan 24;797(1):20-6. doi: 10.1016/0304-4165(84)90377-5.

DOI:10.1016/0304-4165(84)90377-5
PMID:6692008
Abstract

Hydration of an ethoxylate derivative of cholesterol, triethoxycholesterol, results in the formation of stable, rigid, bilayer-like structures capable of encapsulating polar compounds. Studies on the stability and tissue distribution of these liposomes in mice indicate that they are suitable as a drug delivery system. Intraperitoneal injection of triethoxycholesterol encapsulated methotrexate into mice bearing hepatoma ascites tumor results in a doubling of the survival time, relative to untreated mice and those receiving unencaptulated drug. These studies show that fluid, acyl chains are not required for the formation of pharmacologically useful vesicles and that such formulations need not be limited to phospholipid-containing systems.

摘要

胆固醇的一种乙氧基化衍生物三乙氧基胆固醇水合后,会形成能够包裹极性化合物的稳定、刚性的双层样结构。对这些脂质体在小鼠体内的稳定性和组织分布的研究表明,它们适合用作药物递送系统。对患有肝癌腹水瘤的小鼠腹腔注射三乙氧基胆固醇包裹的甲氨蝶呤,相对于未治疗的小鼠和接受未包裹药物的小鼠,其存活时间延长了一倍。这些研究表明,形成具有药理作用的囊泡并不需要流动性的酰基链,并且此类制剂不必局限于含磷脂的系统。

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The pharmacological efficacy of a rigid non-phospholipid liposome drug delivery system.一种刚性非磷脂脂质体药物递送系统的药理功效。
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In vitro uptake and therapeutic application of liposome-encapsulated methotrexate in mouse hepatoma 129.脂质体包裹的甲氨蝶呤在小鼠肝癌129中的体外摄取及治疗应用
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Sterol-modified phospholipids: cholesterol and phospholipid chimeras with improved biomembrane properties.甾醇修饰的磷脂:具有改善生物膜特性的胆固醇与磷脂嵌合体。
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