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LIPOSOME COMPOSITION HAVING BUFFER SOLUTION OF HIGH BUFFER CAPACITY

机译:具有高缓冲剂容量的缓冲剂的脂质体组合物

摘要

A method for encapsulation of antineoplastic agents in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes may be made by a process that loads the drug by an active mechanism using a transmembrane ion gradient, preferably a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%, and liposomes may be loaded with drug immediately prior to use, eliminating stability problems related to drug retention in the liposomes. Drug:lipid ratios employed are about 3-80 fold higher than for traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. An assay method to determine free antineoplastic agents in a liposome preparation is also disclosed.
机译:提供了一种将抗肿瘤剂包封在脂质体内的方法,该方法优选具有高的药物:脂质比例。脂质体可以通过使用跨膜离子梯度,优选跨膜pH梯度通过主动机制加载药物的方法制备。使用这种技术,捕集效率接近100%,并且可以在使用前立即在脂质体中装载药物,从而消除了与药物在脂质体中滞留有关的稳定性问题。使用的药物:脂质比率比传统脂质体制剂高约3-80倍,并且药物从脂质体的释放速率降低。还公开了测定脂质体制剂中游离抗肿瘤剂的测定方法。

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