Takahashi T, Kono K, Yamaguchi T
Tohoku J Exp Med. 1977 Nov;123(3):235-46. doi: 10.1620/tjem.123.235.
Utilizing the lipid-adsorbing ability of lymphatic capillaries, anticancer agents were given in the form of fat emulsion in order to deliver them to regional lymph nodes. The emulsion, in which the drug solution is contained as the innermost phase, yielded high drug concentration in the lymphatic system. Intratumoral injection of emulsified anticancer agent resulted in significantly prolonged retension of the drug within the tumor tissue. Therapeutic experiments of the emulsion also disclosed remarkable tumor reduction and cure rate as compared with aqueous solution of drugs. Oral administration of emulsified 5-Fluorouracil (5-FU) was also attempted for stomach cancer. With 5-FU, the maximum concentration of drug in thoracic lymph and stomach was greater when administered as an emulsion than as an aqueous solution, and a high concentration persisted longer. As a clinical trial of the emulsion method, eight patients with inoperable malignant growth were injected locally with emulsified anticancer agents and 121 patients were given 5-FU emulsion orally. From the clinical and histological findings, it was thought that the emulsion enhanced the chemotherapeutic effect of the anticancer agent on lymph node metastasis.
利用毛细淋巴管的脂质吸附能力，将抗癌剂制成脂肪乳剂的形式，以便将其输送到区域淋巴结。这种乳剂以药物溶液作为最内相，在淋巴系统中产生了高药物浓度。瘤内注射乳化抗癌剂导致药物在肿瘤组织内的滞留时间显著延长。与药物水溶液相比，该乳剂的治疗实验还显示出显著的肿瘤缩小和治愈率。还尝试了口服乳化5-氟尿嘧啶（5-FU）治疗胃癌。对于5-FU，以乳剂形式给药时，胸淋巴和胃中的药物最大浓度高于水溶液，且高浓度持续时间更长。作为乳剂方法的临床试验，对8例无法手术的恶性肿瘤患者局部注射乳化抗癌剂，对121例患者口服5-FU乳剂。从临床和组织学结果来看，认为该乳剂增强了抗癌剂对淋巴结转移的化疗效果。
