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Intranasal drug delivery: an efficient and non-invasive route for systemic administration: focus on opioids.

Abstract
Intranasal administration is a non-invasive route for drug delivery, which is widely used for the local treatment of rhinitis or nasal polyposis. Since drugs can be absorbed into the systemic circulation through the nasal mucosa, this route may also be used in a range of acute or chronic conditions requiring considerable systemic exposure. Indeed, it offers advantages such as ease of administration, rapid onset of action, and avoidance of first-pass metabolism, which consequently offers for example an interesting alternative to intravenous, subcutaneous, oral transmucosal, oral or rectal administration in the management of pain with opioids. Given these indisputable interests, fentanyl-containing formulations have been recently approved and marketed for the treatment of breakthrough cancer pain. This review will outline the relevant aspects of the therapeutic interest and limits of intranasal delivery of drugs, with a special focus on opioids, together with an in-depth discussion of the physiological characteristics of the nasal cavity as well as physicochemical properties (lipophilicity, molecular weight, ionisation) and pharmaceutical factors (absorption enhancers, devices for application) that should be considered for the development of nasal drugs.
AuthorsStanislas Grassin-Delyle, Amparo Buenestado, Emmanuel Naline, Christophe Faisy, Sabine Blouquit-Laye, Louis-Jean Couderc, Morgan Le Guen, Marc Fischler, Philippe Devillier
JournalPharmacology & therapeutics (Pharmacol Ther) Vol. 134 Issue 3 Pg. 366-79 (Jun 2012) ISSN: 1879-016X [Electronic] England
PMID22465159 (Publication Type: Journal Article, Review)
CopyrightCopyright © 2012 Elsevier Inc. All rights reserved.
Chemical References
  • Analgesics, Opioid
Topics
  • Absorption (physiology)
  • Administration, Intranasal (methods)
  • Analgesics, Opioid (administration & dosage, pharmacokinetics)
  • Humans
  • Models, Biological
  • Nasal Cavity (drug effects, physiology)
  • Nasal Mucosa (blood supply, drug effects)
  • Pain (drug therapy)

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