FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLES OF A POORLY WATER SOLUBLE MODEL DRUG, IBUPROFEN

Abstract

Approximately 40% of lipophilic drug candidates fail to comply the commercial requirements of solubility and formulation stability, prompting significant research activity in advanced lipophile delivery technologies. Solid lipid nanoparticle (SLN) technology represents a promising new approach to lipophile drug delivery. Solid lipid nanoparticles typically are spherical with average diameters between 1 to 1000 nanometers. SLNs possess a solid lipid core matrix that can solubilize lipophilic molecules. The lipid core is stabilized by surfactants. Primary objective of this study is to enhance the solubility and dissolution rate of Ibuprofen by formulation into SLN using hot homogenization method. Further, this study also investigates the effect of various formulation parameters like stabilizer concentration, surfactant ratio, Lipid ratio and drug loading. SLNs were characterized for size distribution, entrapment efficiency, drug release and stability. SLN of Ibuprofen was prepared using stearic acid (lipid) Phospholipon 80 H (surfactant) and Tween-80 as stabilizer. The FTIR study shows no major interaction of Ibuprofen with other formulation ingredients, and the Differential Scanning Calorimetry (DSC) study revealed that the drug is molecularly dispersed into the lipid. The particle size determinations confirm the particle size distribution in the nanoparticular range (27% Volume to 56% volume). In- vitro drug release through the dialysis membrane from the prepared SLNs is much higher than the pure drug. The stability study indicates the stability of the formulations without changing its performance on storage. Hence formulation of Ibuprofen in SLN enhances the dissolution rate as well as it will enhance the bioavailability of the drug which could be stabilized during storage.

KEY WORDS: Solid Lipid Nanoparticle, Lipophilic drug, Phospholipon 80H, Ibuprofen

Approximately 40% of lipophilic drug candidates fail to comply the commercial requirements of solubility and formulation stability, prompting significant research activity in advanced lipophile delivery technologies. Solid lipid nanoparticle (SLN) technology represents a promising new approach to lipophile drug delivery. Solid lipid nanoparticles typically are spherical with average diameters between 1 to 1000 nanometers. SLNs possess a solid lipid core matrix that can solubilize lipophilic molecules. The lipid core is stabilized by surfactants. Primary objective of this study is to enhance the solubility and dissolution rate of Ibuprofen by formulation into SLN using hot homogenization method. Further, this study also investigates the effect of various formulation parameters like stabilizer concentration, surfactant ratio, Lipid ratio and drug loading. SLNs were characterized for size distribution, entrapment efficiency, drug release and stability. SLN of Ibuprofen was prepared using stearic acid (lipid) Phospholipon 80 H (surfactant) and Tween-80 as stabilizer. The FTIR study shows no major interaction of Ibuprofen with other formulation ingredients, and the Differential Scanning Calorimetry (DSC) study revealed that the drug is molecularly dispersed into the lipid. The particle size determinations confirm the particle size distribution in the nanoparticular range (27% Volume to 56% volume). In- vitro drug release through the dialysis membrane from the prepared SLNs is much higher than the pure drug. The stability study indicates the stability of the formulations without changing its performance on storage. Hence formulation of Ibuprofen in SLN enhances the dissolution rate as well as it will enhance the bioavailability of the drug which could be stabilized during storage.