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

Abstract

Background: Tobacco smoking is a major factor leading to cardiovascular diseases. About 48% of cardiovascular diseases occur due to cigarette smoking. Bupropion hydrochloride is a non-nicotine treatment for smoking cessation. The existing marketed formulation of bupropion has limitations, like low bioavailability and extensive first-pass metabolism. In order to boost the bioa-vailability and increase the brain biodistribution of the drug, a colloidal drug delivery system, like nanostructured lipid carriers, is employed. Methods: NLC formulation was prepared using the microemulsion technique and an optimized formula was developed using a three-level factorial design. Results: The particle size of the optimized formulation was 162 nm, the polydispersity index was 12.2%, and the 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 the drug was released, indicating the sustained release of the drug. Histo-pathological studies were conducted using goat nasal mucosa, and results indicated the NLC formu-lation as non-toxic for intranasal administration. Conclusion: Thus, through the intra-nasal route, an increased concentration of drug can be deliv-ered to the brain via the olfactory pathway, thereby improving the therapeutic effect and exhibiting better patient compliance in smoking cessation.