Hagiwara A, Takahashi T, Sawai K, Sakakura C, Tsujimoto H, Imanishi T, Ohgaki M, Yamazaki J, Muranishi S, Yamamoto A, Fujita T
First Department of Surgery, Kyoto Prefectural University of Medicine, Japan.
Br J Cancer. 1996 Nov;74(9):1392-6. doi: 10.1038/bjc.1996.554.
A new delivery formulation (5FU-MS) of 5-fluorouracil (5FU), 5FU incorporated in microspheres composed of poly(glycolide-co-lactide) matrix, has been developed for the treatment of peritoneal carcinomatosis, and is designed to slowly release the incorporated 5FU for 3 weeks. Intraperitoneal 5FU-MS distributed higher concentrations of 5FU to the intraperitoneal tissues, such as the omentum and the mesentery, for a longer period with lower blood plasma concentrations than did the aqueous 5FU solution in rats. In experiments using mice, the lethal toxicity, determined by the probit method, in 5FU-MS was reduced to less than half that in aqueous 5FU solution. We evaluated the therapeutic effects on peritoneal carcinomatosis induced by the intraperitoneal inoculation of B-16 PC melanoma cells. The therapeutic effects of 5FU-MS were enhanced when compared with both the equivalent doses and same toxicity doses of the aqueous 5FU solution.
一种新的5-氟尿嘧啶（5FU）递送制剂（5FU-MS）已被开发出来，它是将5FU包裹在由聚（乙交酯-丙交酯）基质组成的微球中，用于治疗腹膜癌，其设计目的是使包裹的5FU在3周内缓慢释放。与大鼠腹腔内注射5FU水溶液相比，腹腔内注射5FU-MS能在更长时间内将更高浓度的5FU分布到腹腔组织，如大网膜和肠系膜，同时血浆浓度更低。在小鼠实验中，通过概率单位法测定，5FU-MS的致死毒性降低到5FU水溶液的一半以下。我们评估了腹腔接种B-16 PC黑色素瘤细胞诱导的腹膜癌的治疗效果。与等量剂量和相同毒性剂量的5FU水溶液相比，5FU-MS的治疗效果得到了增强。
