LIPID BASED SOLID DISPERSIONS OF NEBIVOLOL HYDROCHLORIDE TO IMPROVE SOLUBILITY AND DISSOLUTION RATE

Abstract

Oral drug delivery remains the most preferred route due to its low cost, convenience, and good patient compliance. However, about 40–70% of new chemical entities show poor oral absorption mainly because of low solubility and slow dissolution, leading to poor bioavailability and formulation challenges. To overcome this limitation, the present study focused on developing lipid-based solid dispersions (LBSDs) of Nebivolol Hydrochloride, a β1-adrenergic blocker used for hypertension management, to enhance its solubility, dissolution, and permeability. LBSDs were prepared using different ratios of lipid carriers by the solvent evaporation method, with Fujicalin used as a hydrophilic inert carrier in all formulations. Phase solubility and saturation solubility studies demonstrated a linear increase in drug solubility with increasing carrier concentration. The prepared formulations were evaluated for micromeritic properties, drug content, in vitro dissolution, in vitro diffusion, and ex vivo permeation. Dissolution studies showed that LBSDs significantly improved drug release compared to pure drug and marketed formulation, with Gelucire 50/13 performing better than Gelucire 44/14. The formulation containing Gelucire 50/13 in a 1:5:5 ratio exhibited the highest drug release of 96.9 ± 1.41% within 1 hour. Ex vivo studies using goat intestinal membrane confirmed enhanced permeability of LBSDs. FTIR analysis indicated no drug–excipient interaction, while DSC studies showed peak broadening, suggesting conversion to an amorphous form. XRD results further confirmed partial loss of crystallinity, indicating transformation of the drug into an amorphous state, which contributed to improved solubility and dissolution. Overall, the study concludes that lipid-based solid dispersions of nebivolol hydrochloride effectively enhance dissolution and may improve oral bioavailability.