Formulation, Optimization and Characterization of Bupropion Hydrochloride Loaded Nanostructured Lipid Carriers for Intra-Nasal Administration: An Approach for Management of Smoking Cessation

Abstract

Tobacco smoking is a major factor leading to cardiovascular diseases. About 48% of cardiovascular diseases occur due to cigarette smoking. Bupropion Hydrochloride is non-nicotine treatment for smoking cessation. The existing marketed formulation of bupropion have limitations like low bioavailability and extensive first-pass metabolism. In order to boost the bioavailability and increase the brain biodistribution of the drug, a colloidal drug delivery system like nanostructured lipid carriers is employed. NLC formulation was prepared using microemulsion technique and optimized formula was developed using three-level factorial design. The particle size of the optimized formulation was 162 nm, Polydispersity index was 12.2% and zeta potential was -29.0mV. Entrapment efficiency was found to be 41.2%. SEM images show that these NLCs are spherical. In-vitro drug release study was conducted and at the end of 72 hours, 50 % of drug was released, indicates the sustained release of drug. Histopathological studies were conducted using goat nasal mucosa and results indicates that NLC formulation is non-toxic for intranasal administration. Thus, through intra-nasal route an increased concentration of drug can be delivered to the brain via olfactory pathway and improve the therapeutic effect and better patient compliance in smoking cessation.