Forssen E A, Tökes Z A
Cancer Treat Rep. 1983 May;67(5):481-4.
The severe tissue damage which occurs when doxorubicin (Dxn) is extravasated during infusion has been attenuated by encapsulating the drug in anionic liposomes. Mice were injected intradermally with either 0.05 or 0.10 mg of Dxn in the free or liposome-entrapped form. At both dose levels, the animals receiving free drug developed dermal lesions at a higher frequency and of a greater severity than did those animals receiving Dxn-liposomes. Determination of tissue-associated fluorescence indicated that free Dxn was removed from the area of the dermal injection more rapidly than was the liposome-entrapped drug. The data suggest that the dermal toxicity of Dxn may be determined more by its mode of disposition than by the absolute amount of drug in tissue. Similar observation was made earlier for the Dxn-induced chronic cardiotoxicity.
当阿霉素（Dxn）在输注过程中发生外渗时会出现严重的组织损伤，而将该药物包裹于阴离子脂质体中可减轻这种损伤。给小鼠皮内注射0.05或0.10毫克游离形式或脂质体包裹形式的Dxn。在这两个剂量水平下，接受游离药物的动物出现皮肤损伤的频率更高、严重程度更大，高于接受Dxn脂质体的动物。组织相关荧光的测定表明，游离Dxn从皮肤注射部位清除的速度比脂质体包裹的药物更快。数据表明，Dxn的皮肤毒性可能更多地取决于其处置方式，而非组织中药物的绝对量。早些时候对Dxn诱导的慢性心脏毒性也有类似观察。
