Juliano R L
Prog Clin Biol Res. 1976;9:21-32.
One approach to effective cancer chemotherapy is to maximize the exposure of tumor cells to cytotoxic drugs while minimizing the exposure of sensitive normal cells to such agents. This implies the need for control of the pharmacodynamics of anti-tumor drugs in terms of blood clearance kinetics, disposition in tissues, passage across membrane barriers, and interaction with metabolic pathways. A promising approach to pharmacodynamic control is the microencapsulation of drugs within liposomes. The clearance kinetics and tissue disposition of the drug is then dictated by the pharmacokinetic behavior of the liposomal carrier. The blood clearance rates and tissue uptake of liposomes themselves depend upon physical characteristics such as particle size and surface charge. It is also possible to promote specific interaction between cells and liposomes in vitro by preparing liposomes containing biological macromolecules such as lectin receptors. The potentialities of microencapsulation as an adjunct to chemotherapy are discussed.
有效进行癌症化疗的一种方法是,在尽量减少敏感正常细胞接触细胞毒性药物的同时,使肿瘤细胞最大程度地接触此类药物。这意味着需要从血液清除动力学、在组织中的分布、穿过膜屏障以及与代谢途径的相互作用等方面控制抗肿瘤药物的药效学。药效学控制的一种有前景的方法是将药物微囊化于脂质体中。然后,药物的清除动力学和组织分布由脂质体载体的药代动力学行为决定。脂质体本身的血液清除率和组织摄取取决于诸如粒径和表面电荷等物理特性。通过制备含有诸如凝集素受体等生物大分子的脂质体,也有可能在体外促进细胞与脂质体之间的特异性相互作用。本文讨论了微囊化作为化疗辅助手段的潜力。