Author(s): Aravind Shyamprasad Rekharani, Bala Sai Soujith Nidamanuri, Praharsh Kumar Mandadhi Rajendra, Senthil Venkatachalam, Jubie Selvaraj and Jawahar Natarajan*
Page: [217 - 232] Pages: 16
* (Excluding Mailing and Handling)
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 bioavailability 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. Histopathological studies were conducted using goat nasal mucosa, and results indicated the NLC formulation as non-toxic for intranasal administration.
Conclusion: Thus, through the intra-nasal route, an increased concentration of drug can be delivered to the brain via the olfactory pathway, thereby improving the therapeutic effect and exhibiting better patient compliance in smoking cessation.
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