Delivery of a lactose derivative of endomorphin 1 to the brain via the olfactory epithelial pathway

Cros, Cécile D., Toth, Istvan and Blanchfield, Joanne T. (2014) Delivery of a lactose derivative of endomorphin 1 to the brain via the olfactory epithelial pathway. Bioorganic and Medicinal Chemistry Letters, 24 5: 1373-1375. doi:10.1016/j.bmcl.2014.01.041


Author Cros, Cécile D.
Toth, Istvan
Blanchfield, Joanne T.
Title Delivery of a lactose derivative of endomorphin 1 to the brain via the olfactory epithelial pathway
Journal name Bioorganic and Medicinal Chemistry Letters   Check publisher's open access policy
ISSN 0960-894X
1464-3405
Publication date 2014-03-01
Sub-type Article (original research)
DOI 10.1016/j.bmcl.2014.01.041
Open Access Status
Volume 24
Issue 5
Start page 1373
End page 1375
Total pages 3
Place of publication Kidlington, Oxford, United Kingdom
Publisher Pergamon
Collection year 2015
Language eng
Formatted abstract
The rapid and direct delivery of a neuroactive endomorphin 1 derivative to the brain via nasal delivery is reported. A synthetic derivative of the native opioid peptide, endomorphin 1 bearing a lactose unit on the N-terminus of the peptide has been previously reported to exhibit antinoceceptive activity similar to morphine after both intravenous and oral administration. This compound has been administered nasally to rats and appeared in the olfactory bulb within 10 min of administration with negligible levels appearing in the circulating blood or in the rest of the brain. These results indicate that the peptide is absorbed into the brain via the olfactory epithelial pathway suggesting nasal delivery may be a viable alternative route of delivery in clinical applications.
Keyword Endomorphin-1
Lactose
Peptide drug delivery
Nasal drug delivery
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2015 Collection
Official Audit
School of Chemistry and Molecular Biosciences
School of Pharmacy Publications
 
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Citation counts: TR Web of Science Citation Count  Cited 2 times in Thomson Reuters Web of Science Article | Citations
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Created: Fri, 14 Feb 2014, 10:35:08 EST by Mrs Louise Nimwegen on behalf of School of Chemistry & Molecular Biosciences