Development and characterization of α-Lipoic acid amorphous solid dispersion for improved oral bioavailability and...

α-Lipoic acid (LA), a naturally occurring antioxidant and anti-inflammatory agent, has limited aqueous solubility and bioavailability which hinder its clinical application. To overcome these limitations, in this study, we have developed LA solid dispersion (LASD) using soluplus (SOL) to improve its oral bioavailability and therapeutic efficacy for modulating ovalbumin-lipopolysaccharide (OVA-LPS)-induced allergic airway inflammation. LASD was prepared using lyophilization technique and optimized based on solid-state characterizations. The developed solid dispersion has been comprehensively characterized using Fourier-transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and powder X-ray diffraction (P-XRD) which confirmed the molecular dispersion of LA within the SOL matrix and its amorphous transformation. The in vitro dissolution and pharmacokinetic studies revealed enhanced dissolution and oral bioavailability (5.3-fold) of LASD compared to native LA. The developed LASD significantly attenuated airway inflammation by reducing cytokine levels, major inflammatory markers and histopathological changes in lung tissues. Our study demonstrats that LASD formulation can be a promising strategy to overcome bioavailability and therapeutic efficacy challenges associated with LA.