Enhanced intestinal absorption and bioavailability of raloxifene hydrochloride via lyophilized solid lipid nanoparticles

The current oral therapy with raloxifene hydrochloride (RXH) is less effective due to its poor bioavailability (only 2%). Henceforth, an attempt was made to investigate the utility of triglyceride (trimyristin, tripalmitin and tristearin) based solid lipid nanoparticles (SLNs) for improved oral delivery of RXH. The SLN formulations prepared were evaluated for particle size, zeta potential and % entrapment and the optimized formulation was lyophilized. Solid state characterization studies unravel the transformation of RXH to amorphous or molecular state from the native crystalline form. Further the in situ perfusion studies carried out in rat intestine reveal the potential of SLN for enhanced permeation of raloxifene HCl across gastrointestinal barrier. To derive the conclusions, in vivo pharmacokinetic study was conducted in rats to assess the bioavailability of RXH from SLN formulation compared to drug suspension. Overall a twofold increase in bioavailability with SLN formulations confer their potential for improved oral delivery of RXH.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Solid lipid nanoparticles of raloxifene hydrochloride (RXH) were prepared and characterized. ► In situ rat permeation studies were performed to assess potential of SLN for improved absorption. ► To draw out the conclusions in vivo bioavailability studies were conducted in rats. ► A twofold increase in bioavailability with SLN formulations confer their potential for improved oral delivery of RXH.