Porous microparticles as a tool for minimizing 5-Fluorouracil induced intestinal mucositis.

Abstract

5 Fluorouracil (5-FU) is used primarily to treat solid malignant tumors and is administered via the intravenous route; however, this administration is accompanied by intestinal mucositis, represented by diarrhea. In this work, 5-FU microsponges (porous microparticles) were prepared to be taken orally to minimize the intestinal mucositis associated with the intravenous IV administration of 5-FU. 15 male albino rabbits were utilized to compare the degree of intestinal mucositis related to the intravenous administration to that of 5-FU microsponges capsule oral administration (at the same dose). The experiment was conducted for five consecutive days. Results showed that the mean villus height of the IV group measured about 260.0± 6.9 µm, which was considerably lower (p<0.05) than that of the Capsule group, which measured about 285.0± 9.3 µm; in addition, the mean depth of crypts of IV group measured about 110.0± 6.8 µm which is significant (p<0.05) lower than that of Capsule group which measured about 141.0± 7.8 µm which means that the degree of intestinal mucositis induced by the intravenous injection of 5-FU was significantly higher than that caused by that of oral administration of 5- FU microsponges formulation. By the way, on the fourth day, one rabbit of the IV group died, indicating the severity of the intestinal mucositis after the IV administration of 5-FU. The results showed that the oral administration of 5-FU microsponges is more safe than IV drug administration at the same dose.