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This study investigated the use of a self-microemulsifying drug delivery system to enhance the solubility and intestinal permeability of furosemide, a poorly soluble and poorly permeable drug with limited oral bioavailability.
Formulations were developed using selected surfactants and oils, guided by pseudo-ternary phase diagrams. Dispersions were characterised for droplet size, electrokinetic potential, and drug release. Permeability was assessed ex vivo using ovine intestinal tissue in diffusion chambers.
The optimised formulation (sesame oil 10%, Tween 80 45%, polyethylene glycol 400 45%) formed droplets with a mean size of 0.78 µm, a size distribution span of 0.320, and an electrokinetic potential of -23.5 ± 3.84 mV, indicating good physical stability. At pH 1.2, the formulation exhibited significantly faster drug release, with a mean drug release time of 8.16 ± 0.36 minutes, compared to 28.76 ± 1.33 minutes for the commercial tablet. Ex vivo, the cumulative transport of furosemide across duodenal tissue was 0.981 ± 0.42% for the formulation, compared to 0.434 ± 0.17% for the tablet. The apparent permeability of furosemide in the formulation was more than twofold higher (7.09 x 10-7 cm/s vs. 3.06 x 10-7 cm/s) than the commercial tablet.
Smaller and uniformly distributed droplets enhanced drug release and intestinal transport. The improved solubility and permeability of the formulation indicate enhanced potential for oral absorption.
The self-microemulsifying system significantly improved furosemide’s solubility and intestinal permeability. Further in vivo studies are required to confirm improved oral bioavailability.
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