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Smoking-related health problems are one of the leading causes of deaths worldwide, causing a serious threat and tremendous economic burden to public health. Currently, varenicline and nicotine replacement therapies (NRTs) in the forms of nicotine gums, patches, nasal sprays, and vapor inhalation formulations are the first-line medications for the management of nicotine cessation; however, they could not deliver high levels of nicotine to the brain as fast as cigarette smoking. E-cigarettes, an alternative to tobacco smoking, although available on the market, has been banned by the US Food and Drug Administration (FDA) due to some uncertainties of the dose, safety, and efficacy of this product. Deep lung delivery of drugs enables lower doses with an equivalent therapeutic action compared to oral or parenteral routes as the lungs have a huge surface area for drug absorption. Additionally, pulmonary drug delivery has superior efficacy, low toxicity, and rapid onset of drug action. This chapter demonstrates the health problems associated with cigarette smoking, available drugs, their dosage forms and limitations. Finally, the development of inhaled nicotine formulations as a potential anti-smoking therapeutic has been discussed.
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