Arndt D, Zeisig R, Bechtel D, Fichtner I
Max Delbrück Center for Medicine for Molecular Medicine, Berlin, Germany.
Drug Deliv. 2001 Jan-Mar;8(1):1-7. doi: 10.1080/107175401300002685.
Conventional and sterically stabilized liposomes derived from phosphatidylcholine or the antitumor agents, hexadecylphosphocholine and octadecyl-(1,1-dimethyl-4-piperidino-4-yl)-phosphate, as bilayer forming constituents, containing bleomycin, were developed and tested. Liposomal encapsulation of bleomycin enhanced strongly the antitumor activity against P388 leukemia and the Lewis lung carcinoma. This effect was clearly dependent on the size and lipid composition of the bleomycin-containing liposomes. The therapeutic effects were nearly equal for liposomal and free bleomycin in the B16 melanoma. The partial replacement of phosphatidylcholine by alkylphospholipids and the inclusion of polyethylene glycol modified lipids for sterical stabilization did not further improve the therapeutic efficacy but increased, in some cases, the toxicity of liposomes. Bleomycin-induced lung injury was not observed if liposomal bleomycin was administered.
开发并测试了由磷脂酰胆碱或抗肿瘤药物十六烷基磷胆碱和十八烷基 -（1,1 - 二甲基 - 4 - 哌啶基 - 4 - 基） - 磷酸酯作为双层形成成分衍生而来的传统脂质体和空间稳定脂质体，这些脂质体含有博来霉素。博来霉素的脂质体包封显著增强了对P388白血病和Lewis肺癌的抗肿瘤活性。这种效果明显取决于含博来霉素脂质体的大小和脂质组成。在B16黑色素瘤中，脂质体博来霉素和游离博来霉素的治疗效果几乎相同。用烷基磷脂部分替代磷脂酰胆碱以及加入聚乙二醇修饰脂质以实现空间稳定，并没有进一步提高治疗效果，但在某些情况下增加了脂质体的毒性。如果给予脂质体博来霉素，则未观察到博来霉素诱导的肺损伤。
