Heath T D, Montgomery J A, Piper J R, Papahadjopoulos D
Proc Natl Acad Sci U S A. 1983 Mar;80(5):1377-81. doi: 10.1073/pnas.80.5.1377.
Liposomes conjugated with anti-H2Kk antibody associate with L929 murine fibroblasts in 6- to 20-fold greater amount than do nonspecific liposomes. The ability of methotrexate-gamma-aspartate to inhibit L929 growth is increased 10-fold when encapsulated in targeted liposomes but is decreased to 50% when encapsulated in liposomes with no specificity for the target cells. Ammonium chloride inhibits the effects of the encapsulated but not the free drug. Soluble antibody does not inhibit the efficacy of targeted vesicles, but empty targeted vesicles do inhibit the efficacy. The compound in both targeted and nontargeted vesicles has a minimal effect on BALB/c3T6 fibroblasts. These results demonstrate the potential of antibody-targeted liposomes and the importance of selecting liposome-dependent cytotoxic agents.
与抗H2Kk抗体偶联的脂质体与L929小鼠成纤维细胞的结合量比非特异性脂质体高6至20倍。甲氨蝶呤-γ-天冬氨酸封装于靶向脂质体时抑制L929生长的能力提高了10倍，但封装于对靶细胞无特异性的脂质体时，该能力降至50%。氯化铵抑制封装药物的作用，但不抑制游离药物的作用。可溶性抗体不抑制靶向囊泡的功效，但空的靶向囊泡会抑制其功效。靶向和非靶向囊泡中的化合物对BALB/c3T6成纤维细胞的影响极小。这些结果证明了抗体靶向脂质体的潜力以及选择脂质体依赖性细胞毒性药物的重要性。
