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Preparation and Evaluation of 5-Fluorouracil Loaded Microsponges for Treatment of Colon Cancer

Abstract

Mahmoud H Othman, Gamal M Zayed, Gamal H El-Sokkary, Usama F Ali and Ahmed AH Abdellatif

5-Fluorouracil (5-FU) has a wide anticancer activity versus several types of solid tumors. The activity of 5-FU can be improved and its toxicity can be diminished by enhancing the relative specific accumulation in the tumor regions. The aim of this work was to develop Eudragit RS100 based 5-FU microsponges (MS) for treatment of colon cancer. Oil in oil emulsion solvent diffusion method was used for the preparation of 5-FU sustained release Eudragit RS100 MS. MS were characterized for their encapsulation efficiency, production yield, drug polymer interaction and drug release profiles. Shape, surface morphology visualized by scanning electron microscope (SEM) and particle size of MS was investigated using laser light scattering technique and. Eventually, HCT 116 and CACO2 cell lines were used for determination of cell viability by MTT assay. The results showed that all prepared MS were spherical in shape with several pores on their surfaces. The production yield was in (62.76% ±1.06% and 93.80% ± 1.75%), encapsulation efficiency was in (71.80% ± 1.62% and 101.3% ± 2.60%) and particle size was in ( 53.11 μm ± 41.03 nm and 118.12 μm ± 48.21 nm). Fourier transform infrared revealed that there is no chemical interaction between 5-FU and Eudragit RS100. MS loaded 5-FU was more effective than 5-FU itself as shown by cell viability assay. The results demonstrated that 5-FU with Eudragit RS100 was successfully formulated as sustained release manner and could be a substitution delivery method of 5-FU for oral anticancer treatment.

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