Formulation, Evaluation and Optimization of Nebivolol Hydrochloride Mouth Dissolving Film

The present study is an effort to enhance solubility and to formulate and optimized BCS class II antihypertensive drug Nebivolol HCl a selective β1 blocker. Solid dispersions with binary and ternary ratios of drug: carrier: surfactant was developed by solvent evaporation method. Results confirmed solid dispersion comprising Nebivolol HCl: Poloxamer: Gelucire in ratio enhanced solubility. FTIR, DSC, PXRD and SEM studies confirms compatibility and polymorphic form of drug converted from crystalline to amorphous due to solid dispersion. Ternary solid dispersion 1:7:9 was best selected ratio for development of mouth dissolving film (MDF) by solvent casting method. Preliminary trial batches of MDF were developed and approved batch showed desirable % drug release and folding endurance was further selected for optimization by 32 full factorial design. Two independent variables selected were HPMC E 15 (X1) and TEC (X2) and two responses as % drug release and folding endurance as Y1 and Y2 respectively. The MDF were evaluated for their physio mechanical parameters like visual inspection, mouth feel, Thickness, weight variation, Dispersion and Disintegration test. The optimized MDF coded as OB using HPMC E 15 225 mg and TEC 0.7 ml was selected as suggested by software with high desirability of 0.787 with drug release of 94.92% within 120 sec. and folding endurance 319. From the above results it can be concluded that solid dispersion technique was effective strategy to enhance solubility of Nebivolol and all evaluation results suggested that MDF with excipients used improved drug release rapidly and it may improve bioavailability.