BiopestPeptidV1, Main, Exploration, bibRecord, 000846

Impact of different hydrophobic ion pairs of octreotide on its oral bioavailability in pigs.

Identifieur interne : 000846 ( Main/Exploration ); précédent : 000845; suivant : 000847

Impact of different hydrophobic ion pairs of octreotide on its oral bioavailability in pigs.

Auteurs : Sonja Bonengel [Autriche] ; Max Jelkmann [Autriche] ; Muthanna Abdulkarim [Royaume-Uni] ; Mark Gumbleton [Royaume-Uni] ; Vera Reinstadler [Autriche] ; Herbert Oberacher [Autriche] ; Felix Prüfert [Autriche] ; Andreas Bernkop-Schnürch [Autriche]

Source :

Journal of controlled release : official journal of the Controlled Release Society [ 1873-4995 ] ; 2018.

RBID : pubmed:29355620

Descripteurs français

English descriptors

KwdEn :
- Animals (MeSH), Antineoplastic Agents, Hormonal (administration & dosage), Antineoplastic Agents, Hormonal (chemistry), Antineoplastic Agents, Hormonal (pharmacokinetics), Biological Availability (MeSH), Decanoates (chemistry), Decanoates (pharmacokinetics), Deoxycholic Acid (administration & dosage), Deoxycholic Acid (chemistry), Deoxycholic Acid (pharmacokinetics), Dioctyl Sulfosuccinic Acid (administration & dosage), Dioctyl Sulfosuccinic Acid (chemistry), Dioctyl Sulfosuccinic Acid (pharmacokinetics), Drug Delivery Systems (MeSH), Drug Liberation (MeSH), Hydrophobic and Hydrophilic Interactions (MeSH), Lipase (chemistry), Male (MeSH), Octreotide (administration & dosage), Octreotide (chemistry), Octreotide (pharmacokinetics), Swine (MeSH).
MESH :
- chemical , administration & dosage : Antineoplastic Agents, Hormonal, Deoxycholic Acid, Dioctyl Sulfosuccinic Acid, Octreotide.
- chemical , chemistry : Antineoplastic Agents, Hormonal, Decanoates, Deoxycholic Acid, Dioctyl Sulfosuccinic Acid, Lipase, Octreotide.
- chemical , pharmacokinetics : Antineoplastic Agents, Hormonal, Decanoates, Deoxycholic Acid, Dioctyl Sulfosuccinic Acid, Octreotide.
- Animals, Biological Availability, Drug Delivery Systems, Drug Liberation, Hydrophobic and Hydrophilic Interactions, Male, Swine.

Abstract

The objective of this study was to investigate the impact of different hydrophobic ion pairs (HIP) on the oral bioavailability of the model drug octreotide in pigs. Octreotide was ion paired with the anionic surfactants deoxycholate, decanoate and docusate differing in lipophilicity. These hydrophobic ion pairs were incorporated in self-emulsifying drug delivery systems (SEDDS) based on BrijO10, octyldodecanol, propylene glycol and ethanol in a concentration of 5mg/ml. SEDDS were characterized regarding size distribution, zeta potential, stability towards lipase, log D_{SEDDS/release medium} and mucus diffusion behavior. The oral bioavailability of octreotide was evaluated in pigs via LC-MS/MS analyses. Most efficient ion pairing was achieved at a molar ratio of 1:3 (peptide: surfactant). SEDDS containing the octreotide-deoxycholate, -decanoate and -docusate ion pair exhibited a mean droplet size of 152nm, 112nm and 191nm and a zeta potential of -3.7, -4.6 and -5.7mV, respectively. They were completely stable towards degradation by lipase and showed a log D_{SEDDS/release medium} of 1.7, 1.8 and 2.7, respectively. The diffusion coefficient of these SEDDS was in the range of 0.03, 0.11 and 0.17×10^-9cm²/s, respectively. In vivo studies with these HIPs showed no improvement in the oral bioavailability in case of octreotide-decanoate. In contrast, octreotide-deoxycholate and octreotide-docusate SEDDS resulted in a 17.9-fold and 4.2-fold higher bioavailability vs.

CONTROL

According to these results, hydrophobic ion pairing could be identified as a key parameter for SEDDS to achieve high oral bioavailability.

DOI: 10.1016/j.jconrel.2018.01.012
PubMed: 29355620

Affiliations:

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Le document en format XML

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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals (MeSH)</term>
<term>Antineoplastic Agents, Hormonal (administration & dosage)</term>
<term>Antineoplastic Agents, Hormonal (chemistry)</term>
<term>Antineoplastic Agents, Hormonal (pharmacokinetics)</term>
<term>Biological Availability (MeSH)</term>
<term>Decanoates (chemistry)</term>
<term>Decanoates (pharmacokinetics)</term>
<term>Deoxycholic Acid (administration & dosage)</term>
<term>Deoxycholic Acid (chemistry)</term>
<term>Deoxycholic Acid (pharmacokinetics)</term>
<term>Dioctyl Sulfosuccinic Acid (administration & dosage)</term>
<term>Dioctyl Sulfosuccinic Acid (chemistry)</term>
<term>Dioctyl Sulfosuccinic Acid (pharmacokinetics)</term>
<term>Drug Delivery Systems (MeSH)</term>
<term>Drug Liberation (MeSH)</term>
<term>Hydrophobic and Hydrophilic Interactions (MeSH)</term>
<term>Lipase (chemistry)</term>
<term>Male (MeSH)</term>
<term>Octreotide (administration & dosage)</term>
<term>Octreotide (chemistry)</term>
<term>Octreotide (pharmacokinetics)</term>
<term>Swine (MeSH)</term>
</keywords>
<keywords scheme="KwdFr" xml:lang="fr"><term>Acide désoxycholique (administration et posologie)</term>
<term>Acide désoxycholique (composition chimique)</term>
<term>Acide désoxycholique (pharmacocinétique)</term>
<term>Animaux (MeSH)</term>
<term>Antinéoplasiques hormonaux (administration et posologie)</term>
<term>Antinéoplasiques hormonaux (composition chimique)</term>
<term>Antinéoplasiques hormonaux (pharmacocinétique)</term>
<term>Biodisponibilité (MeSH)</term>
<term>Décanoate (composition chimique)</term>
<term>Décanoate (pharmacocinétique)</term>
<term>Interactions hydrophobes et hydrophiles (MeSH)</term>
<term>Libération de médicament (MeSH)</term>
<term>Mâle (MeSH)</term>
<term>Octréotide (administration et posologie)</term>
<term>Octréotide (composition chimique)</term>
<term>Octréotide (pharmacocinétique)</term>
<term>Suidae (MeSH)</term>
<term>Sulfo-succinate de dioctyle (administration et posologie)</term>
<term>Sulfo-succinate de dioctyle (composition chimique)</term>
<term>Sulfo-succinate de dioctyle (pharmacocinétique)</term>
<term>Systèmes de délivrance de médicaments (MeSH)</term>
<term>Triacylglycerol lipase (composition chimique)</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="administration & dosage" xml:lang="en"><term>Antineoplastic Agents, Hormonal</term>
<term>Deoxycholic Acid</term>
<term>Dioctyl Sulfosuccinic Acid</term>
<term>Octreotide</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antineoplastic Agents, Hormonal</term>
<term>Decanoates</term>
<term>Deoxycholic Acid</term>
<term>Dioctyl Sulfosuccinic Acid</term>
<term>Lipase</term>
<term>Octreotide</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Antineoplastic Agents, Hormonal</term>
<term>Decanoates</term>
<term>Deoxycholic Acid</term>
<term>Dioctyl Sulfosuccinic Acid</term>
<term>Octreotide</term>
</keywords>
<keywords scheme="MESH" qualifier="administration et posologie" xml:lang="fr"><term>Acide désoxycholique</term>
<term>Antinéoplasiques hormonaux</term>
<term>Octréotide</term>
<term>Sulfo-succinate de dioctyle</term>
</keywords>
<keywords scheme="MESH" qualifier="composition chimique" xml:lang="fr"><term>Acide désoxycholique</term>
<term>Antinéoplasiques hormonaux</term>
<term>Décanoate</term>
<term>Octréotide</term>
<term>Sulfo-succinate de dioctyle</term>
<term>Triacylglycerol lipase</term>
</keywords>
<keywords scheme="MESH" qualifier="pharmacocinétique" xml:lang="fr"><term>Acide désoxycholique</term>
<term>Antinéoplasiques hormonaux</term>
<term>Décanoate</term>
<term>Octréotide</term>
<term>Sulfo-succinate de dioctyle</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>Animals</term>
<term>Biological Availability</term>
<term>Drug Delivery Systems</term>
<term>Drug Liberation</term>
<term>Hydrophobic and Hydrophilic Interactions</term>
<term>Male</term>
<term>Swine</term>
</keywords>
<keywords scheme="MESH" xml:lang="fr"><term>Animaux</term>
<term>Biodisponibilité</term>
<term>Interactions hydrophobes et hydrophiles</term>
<term>Libération de médicament</term>
<term>Mâle</term>
<term>Suidae</term>
<term>Systèmes de délivrance de médicaments</term>
</keywords>
</textClass>
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<front><div type="abstract" xml:lang="en">The objective of this study was to investigate the impact of different hydrophobic ion pairs (HIP) on the oral bioavailability of the model drug octreotide in pigs. Octreotide was ion paired with the anionic surfactants deoxycholate, decanoate and docusate differing in lipophilicity. These hydrophobic ion pairs were incorporated in self-emulsifying drug delivery systems (SEDDS) based on BrijO10, octyldodecanol, propylene glycol and ethanol in a concentration of 5mg/ml. SEDDS were characterized regarding size distribution, zeta potential, stability towards lipase, log D<sub>SEDDS/release medium</sub>
 and mucus diffusion behavior. The oral bioavailability of octreotide was evaluated in pigs via LC-MS/MS analyses. Most efficient ion pairing was achieved at a molar ratio of 1:3 (peptide: surfactant). SEDDS containing the octreotide-deoxycholate, -decanoate and -docusate ion pair exhibited a mean droplet size of 152nm, 112nm and 191nm and a zeta potential of -3.7, -4.6 and -5.7mV, respectively. They were completely stable towards degradation by lipase and showed a log D<sub>SEDDS/release medium</sub>
 of 1.7, 1.8 and 2.7, respectively. The diffusion coefficient of these SEDDS was in the range of 0.03, 0.11 and 0.17×10<sup>-9</sup>
cm<sup>2</sup>
/s, respectively. In vivo studies with these HIPs showed no improvement in the oral bioavailability in case of octreotide-decanoate. In contrast, octreotide-deoxycholate and octreotide-docusate SEDDS resulted in a 17.9-fold and 4.2-fold higher bioavailability vs.</div>
<div type="abstract" xml:lang="en"><p><b>CONTROL</b>
</p>
<p>According to these results, hydrophobic ion pairing could be identified as a key parameter for SEDDS to achieve high oral bioavailability.</p>
</div>
</front>
</TEI>
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<DateCompleted><Year>2019</Year>
<Month>03</Month>
<Day>18</Day>
</DateCompleted>
<DateRevised><Year>2019</Year>
<Month>03</Month>
<Day>18</Day>
</DateRevised>
<Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1873-4995</ISSN>
<JournalIssue CitedMedium="Internet"><Volume>273</Volume>
<PubDate><Year>2018</Year>
<Month>03</Month>
<Day>10</Day>
</PubDate>
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<Title>Journal of controlled release : official journal of the Controlled Release Society</Title>
<ISOAbbreviation>J Control Release</ISOAbbreviation>
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<ArticleTitle>Impact of different hydrophobic ion pairs of octreotide on its oral bioavailability in pigs.</ArticleTitle>
<Pagination><MedlinePgn>21-29</MedlinePgn>
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<Abstract><AbstractText>The objective of this study was to investigate the impact of different hydrophobic ion pairs (HIP) on the oral bioavailability of the model drug octreotide in pigs. Octreotide was ion paired with the anionic surfactants deoxycholate, decanoate and docusate differing in lipophilicity. These hydrophobic ion pairs were incorporated in self-emulsifying drug delivery systems (SEDDS) based on BrijO10, octyldodecanol, propylene glycol and ethanol in a concentration of 5mg/ml. SEDDS were characterized regarding size distribution, zeta potential, stability towards lipase, log D<sub>SEDDS/release medium</sub>
 and mucus diffusion behavior. The oral bioavailability of octreotide was evaluated in pigs via LC-MS/MS analyses. Most efficient ion pairing was achieved at a molar ratio of 1:3 (peptide: surfactant). SEDDS containing the octreotide-deoxycholate, -decanoate and -docusate ion pair exhibited a mean droplet size of 152nm, 112nm and 191nm and a zeta potential of -3.7, -4.6 and -5.7mV, respectively. They were completely stable towards degradation by lipase and showed a log D<sub>SEDDS/release medium</sub>
 of 1.7, 1.8 and 2.7, respectively. The diffusion coefficient of these SEDDS was in the range of 0.03, 0.11 and 0.17×10<sup>-9</sup>
cm<sup>2</sup>
/s, respectively. In vivo studies with these HIPs showed no improvement in the oral bioavailability in case of octreotide-decanoate. In contrast, octreotide-deoxycholate and octreotide-docusate SEDDS resulted in a 17.9-fold and 4.2-fold higher bioavailability vs.</AbstractText>
<AbstractText Label="CONTROL">According to these results, hydrophobic ion pairing could be identified as a key parameter for SEDDS to achieve high oral bioavailability.</AbstractText>
<CopyrightInformation>Copyright © 2018 Elsevier B.V. All rights reserved.</CopyrightInformation>
</Abstract>
<AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Bonengel</LastName>
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<AffiliationInfo><Affiliation>Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Chemistry and Biomedicine, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.</Affiliation>
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<AffiliationInfo><Affiliation>Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Chemistry and Biomedicine, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.</Affiliation>
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<Initials>M</Initials>
<AffiliationInfo><Affiliation>School of Pharmacy and Pharmaceutical Sciences, Cardiff University, Cardiff CF 10 3 NB, United Kingdom.</Affiliation>
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<Initials>M</Initials>
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<ForeName>Vera</ForeName>
<Initials>V</Initials>
<AffiliationInfo><Affiliation>Institute of Legal Medicine and Core Facility Metabolomics, Medical University of Innsbruck, Muellerstraße 44, 6020 Innsbruck, Austria.</Affiliation>
</AffiliationInfo>
</Author>
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<ForeName>Herbert</ForeName>
<Initials>H</Initials>
<AffiliationInfo><Affiliation>Institute of Legal Medicine and Core Facility Metabolomics, Medical University of Innsbruck, Muellerstraße 44, 6020 Innsbruck, Austria.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Prüfert</LastName>
<ForeName>Felix</ForeName>
<Initials>F</Initials>
<AffiliationInfo><Affiliation>Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Chemistry and Biomedicine, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.</Affiliation>
</AffiliationInfo>
</Author>
<Author ValidYN="Y"><LastName>Bernkop-Schnürch</LastName>
<ForeName>Andreas</ForeName>
<Initials>A</Initials>
<AffiliationInfo><Affiliation>Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Chemistry and Biomedicine, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria. Electronic address: andreas.bernkop@uibk.ac.at.</Affiliation>
</AffiliationInfo>
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<Language>eng</Language>
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<PublicationType UI="D013485">Research Support, Non-U.S. Gov't</PublicationType>
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<ArticleDate DateType="Electronic"><Year>2018</Year>
<Month>02</Month>
<Day>06</Day>
</ArticleDate>
</Article>
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<MedlineTA>J Control Release</MedlineTA>
<NlmUniqueID>8607908</NlmUniqueID>
<ISSNLinking>0168-3659</ISSNLinking>
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<NameOfSubstance UI="D018931">Antineoplastic Agents, Hormonal</NameOfSubstance>
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<Chemical><RegistryNumber>10041-19-7</RegistryNumber>
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<Chemical><RegistryNumber>EC 3.1.1.3</RegistryNumber>
<NameOfSubstance UI="D008049">Lipase</NameOfSubstance>
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<Chemical><RegistryNumber>RWM8CCW8GP</RegistryNumber>
<NameOfSubstance UI="D015282">Octreotide</NameOfSubstance>
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</MeshHeading>
<MeshHeading><DescriptorName UI="D018931" MajorTopicYN="N">Antineoplastic Agents, Hormonal</DescriptorName>
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<MeshHeading><DescriptorName UI="D016503" MajorTopicYN="Y">Drug Delivery Systems</DescriptorName>
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<MeshHeading><DescriptorName UI="D065546" MajorTopicYN="N">Drug Liberation</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D057927" MajorTopicYN="N">Hydrophobic and Hydrophilic Interactions</DescriptorName>
</MeshHeading>
<MeshHeading><DescriptorName UI="D008049" MajorTopicYN="N">Lipase</DescriptorName>
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<MeshHeading><DescriptorName UI="D008297" MajorTopicYN="N">Male</DescriptorName>
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<MeshHeading><DescriptorName UI="D015282" MajorTopicYN="Y">Octreotide</DescriptorName>
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<MeshHeading><DescriptorName UI="D013552" MajorTopicYN="N">Swine</DescriptorName>
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<KeywordList Owner="NOTNLM"><Keyword MajorTopicYN="Y">Drug release</Keyword>
<Keyword MajorTopicYN="Y">In-vivo study</Keyword>
<Keyword MajorTopicYN="Y">Lipase stability</Keyword>
<Keyword MajorTopicYN="Y">Octreotide</Keyword>
<Keyword MajorTopicYN="Y">Self-emulsifying drug delivery systems</Keyword>
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<PubmedData><History><PubMedPubDate PubStatus="received"><Year>2017</Year>
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<PubMedPubDate PubStatus="accepted"><Year>2018</Year>
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<ArticleIdList><ArticleId IdType="pubmed">29355620</ArticleId>
<ArticleId IdType="pii">S0168-3659(18)30022-1</ArticleId>
<ArticleId IdType="doi">10.1016/j.jconrel.2018.01.012</ArticleId>
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<affiliations><list><country><li>Autriche</li>
<li>Royaume-Uni</li>
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<region><li>Tyrol (Land)</li>
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<settlement><li>Innsbruck</li>
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<orgName><li>Université de médecine d'Innsbruck</li>
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Impact of different hydrophobic ion pairs of octreotide on its oral bioavailability in pigs.

Impact of different hydrophobic ion pairs of octreotide on its oral bioavailability in pigs.

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