Development and Characterization of Oil Entrapped Stomach Site Specific 5-Fluorouracil Loaded Microcapsules

Abstract

Purpose: 5-Fluorouracil (5-FU), a pyrimidine antimetabolite attains permeability but is low in solubility. Conventional intravenous administration of 5-FU is known to cause severe systemic toxic effects and thus restricts its versatile use in neoplastic diseases. Therefore, the present study was undertaken to develop stomach site specific 5-Fluorouracil (5-FU) loaded microcapsules in order to evaluate the effect of incorporated mineral oil on physiochemical properties of alginate and pectin microcapsules. Design/methodology: Mineral oil entrapped buoyant beads of 5-FU was prepared by the ionotropic gelation technique. During the preparation of various batches of beads, the ratio of mineral oil to water (v/v), the ratio of drug to polymer (w/w), were kept as variables at two levels; either high or low. Findings: Smooth, spherical beads with nominal weight variation were obtained. All batches of beads floated for 24 hours with a lag time of 41-84 sec. The release of drug followed for 9 h. Higuchi and other order kinetic modeling indicated a diffusion-controlled release of drug from the beads. The study also demonstrated the influence of mineral oil on drug entrapment (64.3 to 80.15%) and in vitro release. Higher level of oil increased drug entrapment efficiency but retarded drug release rate as compared to lower level of oil containing beads. Formulation D was found to be the optimized formulation. Practical implications: It is perceived that a saturation supply can provide a constant pool locally and up to the desired tissue sites such that the therapeutic effects can be attained in cancerous conditions. Social Implications: Oral bioavailability of 5-FU is only 28% and that limits its compliance and oral usage. This strategy for 5-FU delivery is a retentive formulation for a saturation supply of the drug. Value of paper: The optimized formulation showed 99.987% release of 5-FU in 9 h with 82.51% drug entrapment. The results were found statistically significant hence the developed formulation has enhanced therapeutic value and commercial potential.