Nose as a Route for Drug Delivery

Intranasal administration of topical drugs has always been used for symptomatic relief or treatment of local nasal dysfunctions. However, over the last years, the use of the nasal route for drug delivery as a viable and promising alternative to convention

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Ana Serralheiro, Gilberto Alves, Joana Sousa, Ana Fortuna, and Amílcar Falcão

Keywords

Nasal route • Nasal drug delivery • Intranasal administration • Nasal therapeutic agents • Intranasal delivery • Small-molecule drugs • Topical drugs • Systemic drugs • Central nervous system-acting drugs • Biomolecular drugs

Core Messages

A. Serralheiro, PharmD, MSc J. Sousa, PharmD, MSc A. Fortuna, PharmD, PhD A. Falcão, PharmD, PhD(*) Laboratory of Pharmacology, Pharmacology Department, Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal CNC – Centre for Neuroscience and Cell Biology, University of Coimbra, 3004-517 Coimbra, Portugal e-mail: [email protected]; [email protected]; [email protected]; [email protected] G. Alves, PharmD, PhD Department of Medical Sciences, Faculty of Health Sciences, CICS-UBI – Health Sciences Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506, Covilhã, Portugal e-mail: [email protected]

IN administration of topical drugs (decongestants, antihistamines, corticosteroids or antimicrobials) has been widely used for symptomatic relief and prevention/treatment of nasal dysfunctions, such as nasal congestion and acute or chronic rhinosinusitis. IN administration is now recognised as a therapeutically viable way for delivery of systemic drugs as alternative to the parenteral and oral routes. Over the last years, new pharmaceutical formulations and novel delivery strategies have been developed offering promising opportunities to expand the delivery of small-molecule drugs and biomacromolecular drugs by the nasal route. Nasal drug delivery is particularly interesting for compounds such as polar small drugs, and therapeutic peptides and proteins. IN drug delivery is a patient-friendly administration route avoiding the pain associated with parenteral administration

T.M. Önerci (ed.), Nasal Physiology and Pathophysiology of Nasal Disorders, DOI 10.1007/978-3-642-37250-6_15, © Springer-Verlag Berlin Heidelberg 2013

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and that enables to circumvent poor stability in gastrointestinal fluids, poor intestinal absorption and/or hepatic firstpass metabolism related with oral route. A wide variety of IN drugs exhibit plasma concentrations and systemic bioavailability frequently higher than those obtained for oral administration. Sometimes they are even comparable to those obtained after IV administration. The potential of the nasal route for administration of drugs into systemic circulation has been remarkably evidenced for a wide variety of drugs and it is particularly interesting when a rapid onset of action is a key requirement. IN administration is currently emerging as a promising way for direct delivery of drugs to the brain, which may be extremely useful for treatment of neurological conditions such as epilepsy, Alzheimer’s disease and Parkinson’s disease. IN delivery of some CNS-acting drugs has afforded higher concentrations in the brai

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