Formulation and Invitro Evaluation of Transdermal Patches of Nebivolol Hydrochloride

Nebivolol is a highly cardio selective β1 -receptor blocker with nitric oxide -potentiating vasodilator effect and used in 50 mg dose for the treatment of the hypertension. Moreover, it is a long-acting antihypertensive agent preferred for treating chronic heart failure in high-risk patients. Transdermal drug delivery systems (TDDS) are adhesive drug-containing devices of defined surface area that deliver a predetermined amount of drug to the intact skin at a preprogrammed rate. The biopharmaceutical classification system (BCS) has categorized nebivolol under class II (low solubility and high permeability), suggesting that the non-oral route can be a feasible alternative. Therefore, the present research work was aimed to develop sustain release transdermal patch of Nebivolol utilizing different polymers such as HPMC E50, PVP, Eudragit RS100, and ethyl cellulose and plasticizers such as PEG-400 and Dibutyl phthalate and DMSO as a penetration enhancer via solvent casting method for a low dose of the drug. According to in-vitro drug study, Nebivolol loaded with polymers HPMC E50-EC with PEG-400 as a plasticizer was shown to be the optimum formulation, with drug release of 4.66 mg/cm² /12 h. The patches of Nebivolol concentration remained steady for three months, and their physicochemical and drug release properties did not alter significantly. The formulation was help to avoid first pass metabolism and provide sustained release of the drug and avoid non-compliance with the tablet dosage form. The results indicated that the strategy adopted, viz, preparation of Nebivolol transdermal patch, was successful in enhancing the permeation of drug.