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

Pharmacol Ther. 2012 Jun;134(3):366-79. doi: 10.1016/j.pharmthera.2012.03.003. Epub 2012 Mar 23.


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.

Publication types

  • Review

MeSH terms

  • Absorption / physiology
  • Administration, Intranasal / methods*
  • Analgesics, Opioid / administration & dosage*
  • Analgesics, Opioid / pharmacokinetics*
  • Humans
  • Models, Biological
  • Nasal Cavity / drug effects
  • Nasal Cavity / physiology
  • Nasal Mucosa / blood supply
  • Nasal Mucosa / drug effects
  • Pain / drug therapy


  • Analgesics, Opioid