In vitro stability and permeability studies of liposomal delivery systems for a novel lipophilic endomorphin 1 analogue

Koda, Y., Liang, M., Blanchfield, J. T. and Toth, I. (2008) In vitro stability and permeability studies of liposomal delivery systems for a novel lipophilic endomorphin 1 analogue. International Journal of Pharmaceutics, 356 1-2: 37-43. doi:10.1016/j.ijpharm.2007.12.036


Author Koda, Y.
Liang, M.
Blanchfield, J. T.
Toth, I.
Title In vitro stability and permeability studies of liposomal delivery systems for a novel lipophilic endomorphin 1 analogue
Journal name International Journal of Pharmaceutics   Check publisher's open access policy
ISSN 0378-5173
Publication date 2008-01-01
Year available 2008
Sub-type Article (original research)
DOI 10.1016/j.ijpharm.2007.12.036
Open Access Status
Volume 356
Issue 1-2
Start page 37
End page 43
Total pages 7
Editor Florence, A. T,
Place of publication Netherlands
Publisher Elsevier BV
Language eng
Subject C1
0304 Medicinal and Biomolecular Chemistry
9204 Public Health (excl. Specific Population Health)
Abstract We have previously shown that the stability and permeability of peptides can be greatly improved by conjugation with lipoamino acids such as 2-aminododecanoic acid (C12Laa). However, the increase in lipophilicity which this conjugation provides can also cause a significant decrease in the compound's water solubility. In this study, we coupled C12Laa to the N-terminus of endomorphin1 (Endo-1, Tyr-Pro-Trp-Phe-NH2), and addressed its solubility issue by formulating C12Laa-Endo-1 into phosphatidylcholine liposomes. The aqueous solubility of the lipidic analogue was greatly improved, facilitating the accurate analysis of the compound in in vitro assays. The metabolic stability and in vitro endothelial permeability of the C12Laa-Endo-1 liposomal formulation was assessed using Caco-2 cells, and compared with the formulation of the parent peptide Endo-1. The liposome-encapsulated C12Laa-Endo exhibited significant increases in both stability and permeability. These results suggest that the combination of chemical modification and liposome formulation has great potentials in improving the bioavailability of neuroactive peptides.
Keyword Liposomes
Lipopeptide
Drug delivery
Endomorphin
Opioid peptide delivery
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: 2009 Higher Education Research Data Collection
School of Pharmacy Publications
 
Versions
Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 15 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 20 times in Scopus Article | Citations
Google Scholar Search Google Scholar
Created: Sat, 04 Apr 2009, 01:14:28 EST by Elizabeth Pyke on behalf of School of Pharmacy