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A combined in vitro and in vivo study on the interactions between somatostatin and lipid-based liquid crystalline drug carriers and bilayers

Cervin, Camilla LU ; Vandoolaeghe, Pauline LU ; Nistor, Catalin LU ; Tiberg, Fredrik LU and Johnsson, Markus LU (2009) In European Journal of Pharmaceutical Sciences 36(4-5). p.377-385
Abstract
Somatostatin (SST) is a peptide hormone active in the regulation of the endocrine system via different somatostatin receptors subtypes. It inhibits the release of multiple secondary peptide hormones, affecting neurotransmission and cell proliferation. SST has a high therapeutic potential in the treatment of disease, such as acromegali, acute pancreatitis and gastroenteropathic endocrine tumors. However, its practical use is hampered by a short in vivo half-life of only a few minutes in man. For this reason more long-lived SST analogues, including octreotide and lanreotide, have been developed. Here we have used native SST as a model compound for a different approach of extending plasma half-lives of in vivo labile biomolecules. Through... (More)
Somatostatin (SST) is a peptide hormone active in the regulation of the endocrine system via different somatostatin receptors subtypes. It inhibits the release of multiple secondary peptide hormones, affecting neurotransmission and cell proliferation. SST has a high therapeutic potential in the treatment of disease, such as acromegali, acute pancreatitis and gastroenteropathic endocrine tumors. However, its practical use is hampered by a short in vivo half-life of only a few minutes in man. For this reason more long-lived SST analogues, including octreotide and lanreotide, have been developed. Here we have used native SST as a model compound for a different approach of extending plasma half-lives of in vivo labile biomolecules. Through association of the peptide hormone with lipid-based liquid crystalline nanoparticle (LCNP) carriers, the terminal half-life of SST injected intravenously in rats is shown to be significantly extended from less than 10 min to more than 1 h. The effect on the in vivo circulation behavior depends on the mode of peptide association to the lipid particles and related physicochemical properties are discussed on the basis of in vitro light scattering, z-potential and adsorption measurements. It is concluded that application of the LCNP delivery system represents an interesting alternative to chemical modifications of in vivo sensitive therapeutically interesting peptides. (c) 2008 Elsevier B.V All rights reserved. (Less)
Please use this url to cite or link to this publication:
author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Lipid, Peptide half-life, Drug delivery, In vivo stability, Liquid, crystalline
in
European Journal of Pharmaceutical Sciences
volume
36
issue
4-5
pages
377 - 385
publisher
Elsevier
external identifiers
  • wos:000264008600001
  • scopus:59349116463
ISSN
1879-0720
DOI
10.1016/j.ejps.2008.11.001
language
English
LU publication?
yes
id
38fefb2c-8cdc-4532-9940-26d69a616528 (old id 1404927)
date added to LUP
2009-06-15 09:57:35
date last changed
2017-10-01 03:42:06
@article{38fefb2c-8cdc-4532-9940-26d69a616528,
  abstract     = {Somatostatin (SST) is a peptide hormone active in the regulation of the endocrine system via different somatostatin receptors subtypes. It inhibits the release of multiple secondary peptide hormones, affecting neurotransmission and cell proliferation. SST has a high therapeutic potential in the treatment of disease, such as acromegali, acute pancreatitis and gastroenteropathic endocrine tumors. However, its practical use is hampered by a short in vivo half-life of only a few minutes in man. For this reason more long-lived SST analogues, including octreotide and lanreotide, have been developed. Here we have used native SST as a model compound for a different approach of extending plasma half-lives of in vivo labile biomolecules. Through association of the peptide hormone with lipid-based liquid crystalline nanoparticle (LCNP) carriers, the terminal half-life of SST injected intravenously in rats is shown to be significantly extended from less than 10 min to more than 1 h. The effect on the in vivo circulation behavior depends on the mode of peptide association to the lipid particles and related physicochemical properties are discussed on the basis of in vitro light scattering, z-potential and adsorption measurements. It is concluded that application of the LCNP delivery system represents an interesting alternative to chemical modifications of in vivo sensitive therapeutically interesting peptides. (c) 2008 Elsevier B.V All rights reserved.},
  author       = {Cervin, Camilla and Vandoolaeghe, Pauline and Nistor, Catalin and Tiberg, Fredrik and Johnsson, Markus},
  issn         = {1879-0720},
  keyword      = {Lipid,Peptide half-life,Drug delivery,In vivo stability,Liquid,crystalline},
  language     = {eng},
  number       = {4-5},
  pages        = {377--385},
  publisher    = {Elsevier},
  series       = {European Journal of Pharmaceutical Sciences},
  title        = {A combined in vitro and in vivo study on the interactions between somatostatin and lipid-based liquid crystalline drug carriers and bilayers},
  url          = {http://dx.doi.org/10.1016/j.ejps.2008.11.001},
  volume       = {36},
  year         = {2009},
}