Formulation of 5-Fluorouracil Microsponges as Colon Targeted Delivery System Using 32 Factorial Design

Abstract

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 and 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 µm 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). Thus 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.

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

“…PVA as a stabilising agent in the external aqueous phase had been reported in most of earlier cases. Ahmed U. Ali et al [28] used PEG 4000 solution (0.02% W/V) in water (outer phase). Besides polymers, plasticiser (triethyl citrate) is used to reduce fragility, and pore inducers/ porogens (hydrogen peroxide or sodium bicarbonate, gelatinised starch) are used for increasing number of pores to accommodate higher amount of drug.…”

“…Optimisation by QBD for preparing microparticulate systems is nowadays practised by formulation scientists, and optimised operating variables aid in scale-up design. To enhance reliability and reproducibility of the method, several investigators started attempting simple factorial design [29], Central Composite Design -RSM method by design expert software [1,11,13,16,[28][29][30][31]. They presented linear as well as quadratic models.…”

Formulation and Assessment of Celecoxib Floating Beads in Capsule using 2^3 Full Factorial Design

“…The operation conditions of DSC were carried out under purging of nitrogen at a rate of 40-50 ml/min, and heating at a rate of 10 ̊ C/min. Aluminum pans were used, the weight of the sample was(4-5mg) and the temperature range was from room temperature to 300 C [44].…”