Abstract
The main objective of the current research work was to formulate and evaluate furosemide loaded silica lipid hybrid microparticles for improved oral delivery. A novel silica-lipid hybrid microparticulate system is used for enhancing the oral absorption of low solubility and low permeability of (BCS Class IV) drugs. Silica-lipid hybrid microparticles include the drug solubilising effect of dispersed lipids and stabilizing effect of hydrophilic silica particles to increase drug solubilisation, which leads to enhanced oral bioavailability. The slica lipid hybrid (SLH) microparticles were composed of poorly soluble drug (furosemide), dispersion of oil phase (Soya bean oil and miglyol) in lecithin (Phospholipoid 90H), non-ionic surfactant (Polysorbate 80) and adsorbent (Aerosol 380). Saturation solubility studies were performed in different oils and surfactants with increased concentration of drug revealed increased solubility of furosemide. In vitro dissolution studies conducted under simulated gastric medium revealed 2-4 fold increase in dissolution efficiencies for SLH microparticles compared to that of pure drug (furosemide) and marketed formulation Lasix®. Ex vivo studies showed enhanced lipid digestibility, which improved drug permeability. Solid-state characterization of SLH microparticles by X-ray powder diffraction and Fourier transform infrared spectroscopic analysis confirmed non-crystalline nature and more compatibility of furosemide in silica-lipid hybrid microparticles. It can be concluded that the role of lipids and hydrophilic silica based carrier highlighted in enhancing solubility and permeability, and hence the oral bioavailability of poorly soluble drugs.
Highlights
Oral route of drug delivery is the most convenient and noninvasive method of drug administration which is having the highest degree of patient compliance
The slica lipid hybrid (SLH) microparticles were composed of poorly soluble drug, dispersion of oil phase (Soya bean oil and miglyol) in lecithin (Phospholipoid 90H), non-ionic surfactant (Polysorbate 80) and adsorbent (Aerosol 380)
Materials and Methods Materials Furosemide is a sulfonamide, potent loop diuretic obtained as gift sample from Aventis Pharmaceuticals Ltd, Ankaleshwar, Phospolipoid 90H and Soyabean oil were obtained from Lipoid, Germany, Miglyol 812 was obtained from Hamilton laboratories, Australia, Aerosil® 380 was obtained from Evonik degussa, Germany and the remaining excipients used were of analytical grade
Summary
Oral route of drug delivery is the most convenient and noninvasive method of drug administration which is having the highest degree of patient compliance. In order to improve the solubility and permeability limited bioavailability, lipid-based formulations have emerged as an effective and versatile technology.[5,6,7] Some potential mechanisms by which silica-based materials enhance the oral absorption of drugs are mainly via the preservation of the drug amorphous or molecularly dispersed form, as well as increased wettability in the aqueous medium, which lead to enhanced dissolution or release kinetics.[1,8] the current research was aimed to develop a novel formulation (i.e. silica-lipid hybrid microparticles) for improving the absorption of poorly water-soluble and poorly permeable drug furosemide (BCS Class IV drug) based on appropriately selected lipid excipients and the utilization of nanoparticle technology.[9]
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