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Fluorescence resonance energy transfer measurements as a tool to detect fusion and drug exchange in liposomal suspensions

机译:荧光共振能量转移测量作为检测脂质体悬浮液中融合和药物交换的工具

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Zinc-(II)-phthalocyanine (ZnPc) is a drug that can potentially be used in photodynamic therapy. A promising formulation approach for the strongly hydrophobic ZnPc is to embed the molecule in liposomes. CGP 55847 is such a liposomal ZnPc formulation. From our data, we could conclude that approximately one quarter of the drug molecules were only loosely bound to the liposomes and exchanged between them with a relaxation time of about 15 min. Energy transfer measurements before and after the lyophilization process revealed that the liposomes were stable when suspended in a 10% lactose solution, i.e. no fusion of liposomes took place. In aqueous solution, however, lyophilization induced fusion of liposomes to a small extent with a concomitant increase in size.
机译:锌-(ii) - 苯二氰酸酯(ZnPC)是可能用于光动力疗法的药物。强疏水性ZnPC的有希望的配方方法是将分子嵌入脂质体中。 CGP 55847是这种脂质体ZnPC制剂。从我们的数据来源于,我们可以得出结论,药物分子的大约四分之一仅被松散地与脂质体结合并在它们之间交换,弛豫时间约15分钟。在冻干过程之前和之后的能量转移测量表明,当悬浮在10%乳糖溶液中时,脂质体稳定,即未发生脂质体的融合。然而,在水溶液中,冻干诱导脂质体的融合在很小程度上,伴随的尺寸增加。

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