Takahashi T, Ueda S, Kono K, Majima S
Cancer. 1976 Oct;38(4):1507-14. doi: 10.1002/1097-0142(197610)38:4<1507::aid-cncr2820380411>3.0.co;2-v.
A fat emulsion when injected into tissue is scarcely taken up by the blood vascular system but is retained within the tissue over a relatively extended period, and is distributed slowly into the surrounding tissues and to the regional lymph nodes. Attempts were made to use this property of the emulsion in the local administration of anticancer agents in emulsion, both in experimental animals and in man. The concentrations of bleomycin in the tumor tissue of rats were significantly higher after the intratumoral injection of the emulsion form than when the drug was administered in the aqueous solution, either systemically or intratumorally. Experimental antitumor activity against this tumor was superior after the bleomycin emulsion, as well. In the clinical trials six of eight patients with either squamous cell carcinoma of skin or local recurrence of adenocarcinoma of the breast responded favorably to this treatment.
脂肪乳剂注入组织后几乎不被血管系统摄取，而是在组织内保留较长时间，并缓慢分布到周围组织和局部淋巴结。在实验动物和人体中，人们尝试利用乳剂的这一特性进行抗癌药物的局部给药。大鼠肿瘤组织中博来霉素的浓度，在瘤内注射乳剂形式后显著高于药物以水溶液形式全身或瘤内给药时。博来霉素乳剂对该肿瘤的实验性抗肿瘤活性也更优。在临床试验中，8例皮肤鳞状细胞癌或乳腺癌局部复发患者中有6例对该治疗反应良好。
