FORMULATION OF 5-FLUOROURACIL MICROSPONGES AS COLON TARGETED DELIVERY SYSTEM USING 32 FACTORIAL DESIGN

摘要

5-Fluorouracil is widely used for treatment of colorectal cancer and is provided as intravenous bolus or infusion because it has erratic oral bioavailability. Diarrhea and myelosuppression are potential and the major side effects of the intravenous administration route. This work was aimed to develop colon-targeted delivery of 5-Fluorouracil microsponges so that, the oral bioavailability enhanced and the side effects could be potentially reduced. Quassi-emulsion solvent diffusion method was used to prepare 5-Fluorouracil microsponges using polyethylene glycol as an emulsifier. Different formulae were prepared with different composition am! processing factors. The entrapment efficiency 5-Fluorouracil in these formulae ranged from 17.81 to 78.61%, the particle size of the prepared microsponges ranged from 87 to 229 urn and the % cumulative drug released after 24 hours ranged from 47.7 to 98.58%. The prepared microsponges were subjected to compatibility studies as Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Tlius 5-fluorouracil microsponges considered as a promising system for the colon-specific delivery that has potential for future use as an anticancer therapy for colorectal cancer.