Yuan F, Dellian M, Fukumura D, Leunig M, Berk D A, Torchilin V P, Jain R K
Edwin L. Steele Laboratory, Department of Radiation Oncology, Massachusetts General Hospital, Boston, Massachusetts, USA.
Cancer Res. 1995 Sep 1;55(17):3752-6.
Molecular size is one of the key determinants of transvascular transport of therapeutic agents in tumors. However, there are no data in the literature on the molecular size dependence of microvascular permeability in tumors. Therefore, we measured microvascular permeability to various macromolecules in the human colon adenocarcinoma LS174T transplanted in dorsal skin chambers in severe combined immunodeficient mice. These molecules were fluorescently labeled and injected i.v. into mice. The microvascular permeability was calculated from the fluorescence intensity measured by the intravital fluorescence microscopy technique. The value of permeability varied approximately 2-fold in the range of molecular weight from 25,000 to 160,000. These data indicate that tumor vessels are less permselective than normal vessels, presumably due to large pores in the vessel wall. The transport of macromolecules appears to be limited by diffusion through these pores. The cutoff size of the pores was estimated by observations of transvascular transport of sterically stabilized liposomes of 100-600 nm in diameter. We found that tumor vessels in our model were permeable to liposomes of up to 400 nm in diameter, suggesting that the cutoff size of the pores is between 400 and 600 nm in diameter.
分子大小是治疗药物在肿瘤中跨血管转运的关键决定因素之一。然而,文献中尚无关于肿瘤微血管通透性对分子大小依赖性的数据。因此,我们测量了严重联合免疫缺陷小鼠背部皮肤腔室中移植的人结肠腺癌LS174T对各种大分子的微血管通透性。这些分子用荧光标记并静脉注射到小鼠体内。微血管通透性通过活体荧光显微镜技术测量的荧光强度计算得出。在分子量从25,000到160,000的范围内,通透性值大约变化2倍。这些数据表明,肿瘤血管的通透选择性低于正常血管,推测是由于血管壁上存在大孔隙。大分子的转运似乎受到通过这些孔隙扩散的限制。通过观察直径为100 - 600 nm的空间稳定脂质体的跨血管转运来估计孔隙的截止大小。我们发现,在我们的模型中,肿瘤血管对直径达400 nm的脂质体具有通透性,这表明孔隙的截止大小在直径400至600 nm之间。