J.Jpn. Surg. Soc.. 87(2): 133-140, 1986

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Original article

THE NEW ANTICANCER PREPATATION, 5-FLUOROURACIL－POLY L-LACTIC ACID-MICROCAPSULE AND ITS THERAPEUTIC EVALUATION

An attempt was made to develop the new anticancer drug inducing enhanced tumor response to arterial chemoembolization therapy. 5-Fluorouracil (5-FU) was microencapsulated with poly L-lactic acid by the organic phase separation technique. This granular preparation containing 5-FU (FU-PLA-mc) was about 200μm in diameter and was about 40％in 5-FU content. The release of 5-FU in vitro from FU-PLA-mc gradually increased, extending over 50 hours to reach maximum level.
When 75mg of FU-PLA-mc (5-FU content, 30mg) was infused into nomal rabbits through femoral arteries, maximum level of 5-FU in blood was 1.03±0.16μg/g after 15 minutes. Meanwhile, arterial infusion of the same dosage of FU-PLA-mc into VX2 tumor bearing rabbits resulted in the production of high level of 5-FU (2.1±0.5μg/g) in tumors even after 72 hours. In vivo anticancer effect of FU-PLA-mc was significantly demonstrated ; when 75mg of FU-PLA-mc was administrated to VX2 tumor bearing rabbits through arterial infusion, T/C ratio of mean tumor weight was 0.01％ on the 14th day after infusion. After hepatic arteril embolization with FU-PLA-mc in normal rabbits, elevation of serum transanimases was observed, but it was transient.
Hepatic arterial chemoembolization with FU-PLA-mc was carried out for 8 patients with hepatic malignancies. Of these 8 patients, partial response was obtained in 3 patients and no severe complication was observed.

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