NATEGLINIDE SILICA LIPID HYBRID PARTICLES FOR IMPROVED SOLUBILITY

Porous silica-based drug delivery systems have shown substantial potential for improving the oral delivery of poorly water-soluble drugs. The major problem with nateglinide, a BCS Class II drug, is pH-dependent solubility, limited aqueous solubility, poor dissolution and variable bioavailability. The aim of the present investigation was to develop a lipid-based solid formulation of nateglinide, as a strategy to improve both the solubility and the dissolution rate of the drug in a tablet dosage form. The Silica lipid hybrid particles (SLH) were formulated using Miglyol 812 and Acrysol EL 135 as liquid lipid vehicles AND Labrasol and Transcutol HP as surfactants. Nateglinide was dissolved in different lipids and later adsorbed on highly porous silica Sylloid PF244 to obtain a free-flowing powder. The prepared nateglinide SLH was characterized by FT-IR, DSC, and XRD. Nateglinide SLH was evaluated for solubility and dissolution. SLH of NTG prepared with Miglyol 812 and Transcutol HP enhanced solubility of NTG by 57.21 fold. From the study, it may be concluded that the oral solid lipid-based formulation, SLH has an improved potential for enhancing solubility and dissolution of BCS class II drugs like nateglinide.