Formulation Development and Evaluation of Furosemide Loaded Solid Lipid Microparticles

Abstract

Furosemide is a loop diuretic because of having very low half-life, low oral bioavailability, degraded in gastric juice; it was chosen to formulate as the solid lipid microparticle (SLMs) to overcome above. In this study, an attempt was made to improve the oral bioavailability of furosemide by preparing SLMs using stearic acid (SA) and cetostearyl alcohol (CsA) as lipid polymers by hot homogenization method at different drug: polymer ratios (1:5, 1:10, 1:15 and 1:20) and Span-80 used as a emulsifier. The particle size of SLMs was found in the range of 20 to 200 μm. DSC and XRD study confirmed that drug was completely dispersed in the lipid matrix due to reduced the crystallinity of drug. The SEM of SLMs indicated that SA SLMs were found to be porous and perfectly spherical compared to CsA SLMs. IN vitro dissolution studies showed that, the release was prolonged up to 24 h from SLMs prepared with both lipids. As the speed of homogenizer and concentration of emulsifier increases, it leads to decrease in the particle size and % Encapsulation Efficiency ( % EE) of SLMs. Furosemide-CsA SLMs imparted the strongest drug release retardation compared to furosemide-SA SLMs. Final formulation (capsule) showed sustained drug release throughout 24 h, compared to the marketed formulation (LASIX®-40 mg). The release pattern of formulation was found to follow first order with exhibited non-fickian diffusion-controlled release. Keywords: Furosemide, cetostearyl alcohol, stearic acid, solid lipid microparticles (SLMs), oral controlled drug delivery systems Cite this Article Velenti Chauhan, Bhavesh Akbari, Sandip Tarpara, Rohan Barse. Formulation Development and Evaluation of Furosemide Loaded Solid Lipid Microparticles. Research & Reviews: A Journal of Drug Formulation, Development and Production . 2019; 6(2): 6–18p.