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

Research output: Contribution to journalArticle

Standard

A combined in vitro and in vivo study on the interactions between somatostatin and lipid-based liquid crystalline drug carriers and bilayers. / Cervin, Camilla; Vandoolaeghe, Pauline; Nistor, Catalin; Tiberg, Fredrik; Johnsson, Markus.

In: European Journal of Pharmaceutical Sciences, Vol. 36, No. 4-5, 2009, p. 377-385.

Research output: Contribution to journalArticle

Harvard

APA

CBE

MLA

Vancouver

Author

Cervin, Camilla ; Vandoolaeghe, Pauline ; Nistor, Catalin ; Tiberg, Fredrik ; Johnsson, Markus. / A combined in vitro and in vivo study on the interactions between somatostatin and lipid-based liquid crystalline drug carriers and bilayers. In: European Journal of Pharmaceutical Sciences. 2009 ; Vol. 36, No. 4-5. pp. 377-385.

RIS

TY - JOUR

T1 - A combined in vitro and in vivo study on the interactions between somatostatin and lipid-based liquid crystalline drug carriers and bilayers

AU - Cervin, Camilla

AU - Vandoolaeghe, Pauline

AU - Nistor, Catalin

AU - Tiberg, Fredrik

AU - Johnsson, Markus

PY - 2009

Y1 - 2009

N2 - 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.

AB - 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.

KW - Lipid

KW - Peptide half-life

KW - Drug delivery

KW - In vivo stability

KW - Liquid

KW - crystalline

U2 - 10.1016/j.ejps.2008.11.001

DO - 10.1016/j.ejps.2008.11.001

M3 - Article

VL - 36

SP - 377

EP - 385

JO - European Journal of Pharmaceutical Sciences

JF - European Journal of Pharmaceutical Sciences

SN - 1879-0720

IS - 4-5

ER -