World Library  
Flag as Inappropriate
Email this Article

Nasal administration

Article Id: WHEBN0022034247
Reproduction Date:

Title: Nasal administration  
Author: World Heritage Encyclopedia
Language: English
Subject: Drug delivery, Amphetamine, Intracavernous injection, Sublabial administration, Transdermal
Collection: Dosage Forms, Medical Treatments, Routes of Administration
Publisher: World Heritage Encyclopedia
Publication
Date:
 

Nasal administration

Spiral of Ketamine for Snorting

Nasal administration can be used to deliver drugs for either local or systemic effect. Locally acting drugs are for example decongestants and allergy treatments. Examples of systemically active drugs available as nasal sprays are migraine drugs, nicotine replacement and hormone treatments.

Contents

  • Advantages with nasal systemic drug delivery 1
  • Limitations with nasal systemic drug delivery 2
  • Drugs for nasal administration 3
  • Olfactory transfer 4
  • References 5

Advantages with nasal systemic drug delivery

The nasal cavity is covered by a thin mucosa which is well vascularised.[1] Therefore, a drug molecule can be transferred quickly across the single epithelial cell layer directly to the systemic blood circulation without first-pass hepatic and intestinal metabolism. The effect is often reached within 5 min for smaller drug molecules.[2] Nasal administration can therefore be used as an alternative to oral administration of for example tablets and capsules if a fast effect is desired or if the drug is extensively degraded in the gut or liver.[3]drug which shows poor absorbtivity can be given by this route

Limitations with nasal systemic drug delivery

Nasal administration is primarily suitable for potent drugs since only a limited volume can be sprayed into the nasal cavity. Drugs for continuous and frequent administration may be less suitable because of the risk of harmful long term effects on the nasal epithelium.[4] Nasal administration has also been associated with a high variability in the amount of drug absorbed. Upper airway infections may increase the variability as may the extent of sensory irritation of the nasal mucosa, differences in the amount of liquid spray that is swallowed and not kept in the nasal cavity and differences in the spray actuation process.[5] However, the variability in the amount absorbed after nasal administration should be comparable to that after oral administration.[6][7]

Drugs for nasal administration

Nasal sprays for local effect are quite common. Several antimigraine drugs are also currently administered by nasal administration because a fast effect is desired and oral administration can be prohibited by nausea.[8] Peptide drugs (hormone treatments) are also available as nasal sprays, in this case to avoid drug degradation after oral administration. The peptide analogue desmopressin is, for example, available for both nasal and oral administration. The bioavailability of the commercial tablet is 0.1% while that of the nasal spray is 3-5% according to the SPC (Summary of Product Characteristics).[9] Other potential drug candidates for nasal administration include anaesthetics, antiemetics and sedatives that all benefit from a fast onset of effect.[10]

The live attenuated influenza vaccine sold under the brand names FluMist (USA) or Fluenz (Europe) is delivered intranasally.

Olfactory transfer

The major part of the approximately 150 cm2 surface in the human nasal cavity is covered by respiratory epithelium, across which systemic drug absorption can be achieved. The olfactory epithelium is situated in the upper posterior part and covers approximately 10 cm2 of the human nasal cavity. The nerve cells of the olfactory epithelium project into the olfactory bulb of the brain, which provides a direct connection between the brain and the external environment. The transfer of drugs to the brain from the blood circulation is normally hindered by the blood–brain barrier (BBB), which is virtually impermeable to passive diffusion of all but small, lipophilic substances. However, if drug substances can be transferred along the olfactory nerve cells, they can bypass the BBB and enter the brain directly.,[11][12]

The olfactory transfer of drugs into the brain is thought to occur by either slow transport inside the olfactory nerve cells to the olfactory bulb or by faster transfer along the perineural space surrounding the olfactory nerve cells into the cerebrospinal fluid surrounding the olfactory bulbs and the brain (8, 9) [13][14]

Olfactory transfer could theoretically be used to deliver drugs that have a required effect in the central nervous system such as those for Parkinson’s or Alzheimer’s diseases. Studies have been presented that show that direct transfer of drugs is achievable [15][16] but the possibility of olfactory delivery of therapeutically relevant doses to humans remains to be demonstrated.

References

  1. ^ D.F. Proctor and I. Andersen. The nose. Upper airway physiology and the atmospheric environment, Elsevier Biomedical Press, Amsterdam, 1982.
  2. ^ Y.W. Chien, K.S.E. Su, and S.-F. Chang. Nasal systemic drug delivery, Marcel Dekker, Inc., New York, 1989.
  3. ^ http://www.diva-portal.org/diva/getDocument?urn_nbn_se_uu_diva-9292__fulltext.pdf
  4. ^ http://publications.uu.se/theses/abstract.xsql?lang=en&dbid=9292
  5. ^ H. Kublik and M.T. Vidgren. Nasal delivery systems and their effect on deposition and absorption. Adv Drug Deliv Rev. 29:157-177 (1998).
  6. ^ B.A. Coda, A.C. Rudy, S.M. Archer, and D.P. Wermeling. Pharmacokinetics and bioavailability of single-dose intranasal hydromorphone hydrochloride in healthy volunteers. Anesth Analg. 97:117-123 (2003).
  7. ^ J. Studd, B. Pornel, I. Marton, J. Bringer, C. Varin, Y. Tsouderos, and C. Christiansen. Efficacy and acceptability of intranasal 17 beta-oestradiol for menopausal symptoms: randomised dose-response study. Aerodiol Study Group. Lancet. 353:1574-1578 (1999).
  8. ^ http://www.diva-portal.org/diva/getDocument?urn_nbn_se_uu_diva-9292__fulltext.pdf
  9. ^ FerringPharmaceuticals. SPC: Minirin nasal spray, Minirin Freeze-dried tablet and Minirin tablet, 2005.
  10. ^ H.R. Costantino, L. Illum, G. Brandt, P.H. Johnson, and S.C. Quay. Intranasal delivery: physicochemical and therapeutic aspects. Int J Pharm. 337:1-24 (2007).
  11. ^ http://publications.uu.se/abstract.xsql?dbid=3905
  12. ^ http://publications.uu.se/abstract.xsql?dbid=7829
  13. ^ S. Mathison, R. Nagilla, and U.B. Kompella. Nasal route for direct delivery of solutes to the central nervous system: Fact or fiction? J Drug Target. 5:415-441 (1998)
  14. ^ L. Illum. Is nose-to-brain transport of drugs in man a reality? J Pharm Pharmacol. 56:3-17 (2004).
  15. ^ L. Illum. Is nose-to-brain transport of drugs in man a reality? J Pharm Pharmacol. 56:3-17 (2004).
  16. ^ U.E. Westin, E. Bostrom, J. Grasjo, M. Hammarlund-Udenaes, and E. Bjork. Direct nose-to-brain transfer of morphine after nasal administration to rats. Pharm Res. 23:565-572 (2006).
This article was sourced from Creative Commons Attribution-ShareAlike License; additional terms may apply. World Heritage Encyclopedia content is assembled from numerous content providers, Open Access Publishing, and in compliance with The Fair Access to Science and Technology Research Act (FASTR), Wikimedia Foundation, Inc., Public Library of Science, The Encyclopedia of Life, Open Book Publishers (OBP), PubMed, U.S. National Library of Medicine, National Center for Biotechnology Information, U.S. National Library of Medicine, National Institutes of Health (NIH), U.S. Department of Health & Human Services, and USA.gov, which sources content from all federal, state, local, tribal, and territorial government publication portals (.gov, .mil, .edu). Funding for USA.gov and content contributors is made possible from the U.S. Congress, E-Government Act of 2002.
 
Crowd sourced content that is contributed to World Heritage Encyclopedia is peer reviewed and edited by our editorial staff to ensure quality scholarly research articles.
 
By using this site, you agree to the Terms of Use and Privacy Policy. World Heritage Encyclopedia™ is a registered trademark of the World Public Library Association, a non-profit organization.
 


Copyright © World Library Foundation. All rights reserved. eBooks from Project Gutenberg are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.