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

Abstract

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.represent an important factor to oral as compared to administration intravenously as reported previously [9].Conversely, intravenous administration of 5-FU yields severe systemic toxic effects of gastrointestinal (GIT), blood complaints, and skin diseases, due to the 5-FU cytotoxicity on healthful human cells. Hence, the need to formulate targeted delivery of 5-FU through oral route would not only diminish the exposure of healthy cells to the drug but also provide an efficient and harmless curative effect for colon cancer with a lower dose and reduced duration of therapy [5]. It was reported that the therapeutic effect of 5-FU can be augmented and its harmful effects can be suppressed by the precise accumulation of the anticancer agent in the tumor regions with continued exposure of the cells to this drug [10]. To extend the exposure time of cancer cells to 5-FU, the drug delivery was formulated by incorporation into microsponge formulation.Microsponges (MS) are micro-sized particles with high porosity and unique ability for encapsulation of a wide multiplicity of pharmaceutical active ingredients. MS delivery system is used to target and modify the release of active ingredients from pharmaceutical formulations, enhance the stability and decrease the side effects [11]. MS have high load activity reach up to 90% entrapment efficiency [12], self-sterilizing Citation: Othman MH, Zayed GM, El-Sokkary GH, Ali UF, Abdellatif AAH (2017) Preparation and Evaluation of 5-Fluorouracil Loaded Microsp...

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