Vaginal distribution and retention of a multiparticulate drug delivery system, assessed by gamma scintigraphy and magnetic resonance imaging.
Identifieur interne : 000945 ( Main/Exploration ); précédent : 000944; suivant : 000946Vaginal distribution and retention of a multiparticulate drug delivery system, assessed by gamma scintigraphy and magnetic resonance imaging.
Auteurs : RBID : pubmed:22265911English descriptors
- KwdEn :
- Administration, Intravaginal, Adult, Animals, Capsules, Cetomacrogol (chemistry), Chemistry, Pharmaceutical, Contrast Media (administration & dosage), Contrast Media (chemistry), Contrast Media (pharmacokinetics), Cross-Over Studies, Drug Carriers, Drug Compounding, Female, Humans, Magnetic Resonance Imaging, Meglumine (administration & dosage), Meglumine (chemistry), Meglumine (pharmacokinetics), Models, Animal, Mucous Membrane (metabolism), Mucous Membrane (radionuclide imaging), Ointments, Organometallic Compounds (administration & dosage), Organometallic Compounds (chemistry), Organometallic Compounds (pharmacokinetics), Pentetic Acid (administration & dosage), Pentetic Acid (chemistry), Pentetic Acid (pharmacokinetics), Radiopharmaceuticals (administration & dosage), Radiopharmaceuticals (chemistry), Radiopharmaceuticals (pharmacokinetics), Sheep, Starch (chemistry), Surface-Active Agents (chemistry), Technology, Pharmaceutical (methods), Tissue Distribution, Vagina (metabolism), Vagina (radionuclide imaging), Young Adult.
- MESH :
- chemical , administration & dosage : Contrast Media, Meglumine, Organometallic Compounds, Pentetic Acid, Radiopharmaceuticals.
- chemical , chemistry : Cetomacrogol, Contrast Media, Meglumine, Organometallic Compounds, Pentetic Acid, Radiopharmaceuticals, Starch, Surface-Active Agents.
- chemical , pharmacokinetics : Contrast Media, Meglumine, Organometallic Compounds, Pentetic Acid, Radiopharmaceuticals.
- chemical : Capsules, Drug Carriers, Ointments.
- metabolism : Mucous Membrane, Vagina.
- methods : Technology, Pharmaceutical.
- radionuclide imaging : Mucous Membrane, Vagina.
- Administration, Intravaginal, Adult, Animals, Chemistry, Pharmaceutical, Cross-Over Studies, Drug Compounding, Female, Humans, Magnetic Resonance Imaging, Models, Animal, Sheep, Tissue Distribution, Young Adult.
Abstract
For any new vaginal dosage form, the distribution and retention in the vagina has to be assessed by in vivo evaluation. We evaluated the vaginal distribution and retention of starch-based pellets in sheep as live animal model by gamma scintigraphy (using Indium-111 DTPA as radiolabel) and in women via magnetic resonance imaging (MRI, using a gadolinium chelate as contrast agent). A conventional cream formulation was used as reference in both studies.
DOI: 10.1016/j.ijpharm.2012.01.006
PubMed: 22265911
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Vaginal distribution and retention of a multiparticulate drug delivery system, assessed by gamma scintigraphy and magnetic resonance imaging.</title><author><name sortKey="Mehta, Samata" uniqKey="Mehta S">Samata Mehta</name><affiliation wicri:level="1"><nlm:affiliation>Laboratory of Pharmaceutical Technology, Ghent University, Harelbekestraat 72, B-9000 Ghent, Belgium.</nlm:affiliation><country xml:lang="fr">Belgique</country><wicri:regionArea>Laboratory of Pharmaceutical Technology, Ghent University, Harelbekestraat 72, B-9000 Ghent</wicri:regionArea></affiliation></author><author><name sortKey="Verstraelen, Hans" uniqKey="Verstraelen H">Hans Verstraelen</name></author><author><name sortKey="Peremans, Kathelijne" uniqKey="Peremans K">Kathelijne Peremans</name></author><author><name sortKey="Villeirs, Geert" uniqKey="Villeirs G">Geert Villeirs</name></author><author><name sortKey="Vermeire, Simon" uniqKey="Vermeire S">Simon Vermeire</name></author><author><name sortKey="De Vos, Filip" uniqKey="De Vos F">Filip De Vos</name></author><author><name sortKey="Mehuys, Els" uniqKey="Mehuys E">Els Mehuys</name></author><author><name sortKey="Remon, Jean Paul" uniqKey="Remon J">Jean Paul Remon</name></author><author><name sortKey="Vervaet, Chris" uniqKey="Vervaet C">Chris Vervaet</name></author></titleStmt><publicationStmt><date when="2012">2012</date><idno type="doi">10.1016/j.ijpharm.2012.01.006</idno><idno type="RBID">pubmed:22265911</idno><idno type="pmid">22265911</idno><idno type="wicri:Area/Main/Corpus">000F46</idno><idno type="wicri:Area/Main/Curation">000F46</idno><idno type="wicri:Area/Main/Exploration">000945</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Administration, Intravaginal</term><term>Adult</term><term>Animals</term><term>Capsules</term><term>Cetomacrogol (chemistry)</term><term>Chemistry, Pharmaceutical</term><term>Contrast Media (administration & dosage)</term><term>Contrast Media (chemistry)</term><term>Contrast Media (pharmacokinetics)</term><term>Cross-Over Studies</term><term>Drug Carriers</term><term>Drug Compounding</term><term>Female</term><term>Humans</term><term>Magnetic Resonance Imaging</term><term>Meglumine (administration & dosage)</term><term>Meglumine (chemistry)</term><term>Meglumine (pharmacokinetics)</term><term>Models, Animal</term><term>Mucous Membrane (metabolism)</term><term>Mucous Membrane (radionuclide imaging)</term><term>Ointments</term><term>Organometallic Compounds (administration & dosage)</term><term>Organometallic Compounds (chemistry)</term><term>Organometallic Compounds (pharmacokinetics)</term><term>Pentetic Acid (administration & dosage)</term><term>Pentetic Acid (chemistry)</term><term>Pentetic Acid (pharmacokinetics)</term><term>Radiopharmaceuticals (administration & dosage)</term><term>Radiopharmaceuticals (chemistry)</term><term>Radiopharmaceuticals (pharmacokinetics)</term><term>Sheep</term><term>Starch (chemistry)</term><term>Surface-Active Agents (chemistry)</term><term>Technology, Pharmaceutical (methods)</term><term>Tissue Distribution</term><term>Vagina (metabolism)</term><term>Vagina (radionuclide imaging)</term><term>Young Adult</term></keywords><keywords scheme="MESH" type="chemical" qualifier="administration & dosage" xml:lang="en"><term>Contrast Media</term><term>Meglumine</term><term>Organometallic Compounds</term><term>Pentetic Acid</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Cetomacrogol</term><term>Contrast Media</term><term>Meglumine</term><term>Organometallic Compounds</term><term>Pentetic Acid</term><term>Radiopharmaceuticals</term><term>Starch</term><term>Surface-Active Agents</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Contrast Media</term><term>Meglumine</term><term>Organometallic Compounds</term><term>Pentetic Acid</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" type="chemical" xml:lang="en"><term>Capsules</term><term>Drug Carriers</term><term>Ointments</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Mucous Membrane</term><term>Vagina</term></keywords><keywords scheme="MESH" qualifier="methods" xml:lang="en"><term>Technology, Pharmaceutical</term></keywords><keywords scheme="MESH" qualifier="radionuclide imaging" xml:lang="en"><term>Mucous Membrane</term><term>Vagina</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Administration, Intravaginal</term><term>Adult</term><term>Animals</term><term>Chemistry, Pharmaceutical</term><term>Cross-Over Studies</term><term>Drug Compounding</term><term>Female</term><term>Humans</term><term>Magnetic Resonance Imaging</term><term>Models, Animal</term><term>Sheep</term><term>Tissue Distribution</term><term>Young Adult</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">For any new vaginal dosage form, the distribution and retention in the vagina has to be assessed by in vivo evaluation. We evaluated the vaginal distribution and retention of starch-based pellets in sheep as live animal model by gamma scintigraphy (using Indium-111 DTPA as radiolabel) and in women via magnetic resonance imaging (MRI, using a gadolinium chelate as contrast agent). A conventional cream formulation was used as reference in both studies.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">22265911</PMID><DateCreated><Year>2012</Year><Month>03</Month><Day>05</Day></DateCreated><DateCompleted><Year>2012</Year><Month>06</Month><Day>22</Day></DateCompleted><DateRevised><Year>2013</Year><Month>11</Month><Day>21</Day></DateRevised><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1873-3476</ISSN><JournalIssue CitedMedium="Internet"><Volume>426</Volume><Issue>1-2</Issue><PubDate><Year>2012</Year><Month>Apr</Month><Day>15</Day></PubDate></JournalIssue><Title>International journal of pharmaceutics</Title><ISOAbbreviation>Int J Pharm</ISOAbbreviation></Journal><ArticleTitle>Vaginal distribution and retention of a multiparticulate drug delivery system, assessed by gamma scintigraphy and magnetic resonance imaging.</ArticleTitle><Pagination><MedlinePgn>44-53</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1016/j.ijpharm.2012.01.006</ELocationID><Abstract><AbstractText Label="BACKGROUND" NlmCategory="BACKGROUND">For any new vaginal dosage form, the distribution and retention in the vagina has to be assessed by in vivo evaluation. We evaluated the vaginal distribution and retention of starch-based pellets in sheep as live animal model by gamma scintigraphy (using Indium-111 DTPA as radiolabel) and in women via magnetic resonance imaging (MRI, using a gadolinium chelate as contrast agent). A conventional cream formulation was used as reference in both studies.</AbstractText><AbstractText Label="METHOD" NlmCategory="METHODS">Cream and pellets were administered to sheep (n=6) in a two period-two treatment study and to healthy female volunteers (n=6) via a randomized crossover trial. Pellets (filled into hard gelatin capsule) and cetomacrogol cream, both labeled with Indium-111 DTPA (for gamma scintigraphy) or with gadolinium chelate (for MRI) were evaluated for their intravaginal distribution and retention over a 24h period. Spreading in the vagina was assessed based on the part of the vagina covered with formulation (expressed in relation to the total vaginal length). Vaginal retention of the formulation was quantified based on the radioactivity remaining in the vaginal area (sheep study), or qualitatively evaluated (women study).</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">Both trials indicated a rapid distribution of the cream within the vagina as complete coverage of the vaginal mucosa was seen 1h after dose administration. Clearance of the cream was rapid: about 10% activity remained in the vaginal area of the sheep 12h post-administration, while after 8h only a thin layer of cream was detected on the vaginal mucosa of women. After disintegration of the hard gelatin capsule, the pellet formulation gradually distributed over the entire vaginal mucosa. Residence time of the pellets in the vagina was longer compared to the semi-solid formulation: after 24h 23 ± 7% radioactivity was detected in the vaginal area of the sheep, while in women the pellet formulation was still detected throughout the vagina.</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">A multi-particulate system containing starch-based pellets was identified as a promising novel vaginal drug delivery system, resulting in complete coverage of the vaginal mucosa and long retention time.</AbstractText><CopyrightInformation>Copyright © 2012 Elsevier B.V. All rights reserved.</CopyrightInformation></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Mehta</LastName><ForeName>Samata</ForeName><Initials>S</Initials><Affiliation>Laboratory of Pharmaceutical Technology, Ghent University, Harelbekestraat 72, B-9000 Ghent, Belgium.</Affiliation></Author><Author ValidYN="Y"><LastName>Verstraelen</LastName><ForeName>Hans</ForeName><Initials>H</Initials></Author><Author ValidYN="Y"><LastName>Peremans</LastName><ForeName>Kathelijne</ForeName><Initials>K</Initials></Author><Author ValidYN="Y"><LastName>Villeirs</LastName><ForeName>Geert</ForeName><Initials>G</Initials></Author><Author ValidYN="Y"><LastName>Vermeire</LastName><ForeName>Simon</ForeName><Initials>S</Initials></Author><Author ValidYN="Y"><LastName>De Vos</LastName><ForeName>Filip</ForeName><Initials>F</Initials></Author><Author ValidYN="Y"><LastName>Mehuys</LastName><ForeName>Els</ForeName><Initials>E</Initials></Author><Author ValidYN="Y"><LastName>Remon</LastName><ForeName>Jean Paul</ForeName><Initials>JP</Initials></Author><Author ValidYN="Y"><LastName>Vervaet</LastName><ForeName>Chris</ForeName><Initials>C</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Comparative Study</PublicationType><PublicationType>Journal Article</PublicationType><PublicationType>Randomized Controlled Trial</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2012</Year><Month>01</Month><Day>13</Day></ArticleDate></Article><MedlineJournalInfo><Country>Netherlands</Country><MedlineTA>Int J Pharm</MedlineTA><NlmUniqueID>7804127</NlmUniqueID><ISSNLinking>0378-5173</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Capsules</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Contrast Media</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Drug Carriers</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Ointments</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Organometallic Compounds</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Surface-Active Agents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>gadoterate meglumine</NameOfSubstance></Chemical><Chemical><RegistryNumber>6HG8UB2MUY</RegistryNumber><NameOfSubstance>Meglumine</NameOfSubstance></Chemical><Chemical><RegistryNumber>7A314HQM0I</RegistryNumber><NameOfSubstance>Pentetic Acid</NameOfSubstance></Chemical><Chemical><RegistryNumber>9004-95-9</RegistryNumber><NameOfSubstance>Cetomacrogol</NameOfSubstance></Chemical><Chemical><RegistryNumber>9005-25-8</RegistryNumber><NameOfSubstance>Starch</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Administration, Intravaginal</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Adult</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Capsules</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Cetomacrogol</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Chemistry, Pharmaceutical</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Contrast Media</DescriptorName><QualifierName MajorTopicYN="Y">administration & dosage</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Cross-Over Studies</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="Y">Drug Carriers</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Drug Compounding</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Female</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="Y">Magnetic Resonance Imaging</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Meglumine</DescriptorName><QualifierName MajorTopicYN="Y">administration & dosage</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Models, Animal</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mucous Membrane</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="N">radionuclide imaging</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Ointments</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Organometallic Compounds</DescriptorName><QualifierName MajorTopicYN="Y">administration & dosage</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Pentetic Acid</DescriptorName><QualifierName MajorTopicYN="Y">administration & dosage</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radiopharmaceuticals</DescriptorName><QualifierName MajorTopicYN="Y">administration & dosage</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Sheep</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Starch</DescriptorName><QualifierName MajorTopicYN="Y">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Surface-Active Agents</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Technology, Pharmaceutical</DescriptorName><QualifierName MajorTopicYN="N">methods</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tissue Distribution</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Vagina</DescriptorName><QualifierName MajorTopicYN="Y">metabolism</QualifierName><QualifierName MajorTopicYN="Y">radionuclide imaging</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Young Adult</DescriptorName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="received"><Year>2011</Year><Month>11</Month><Day>7</Day></PubMedPubDate><PubMedPubDate PubStatus="revised"><Year>2012</Year><Month>1</Month><Day>4</Day></PubMedPubDate><PubMedPubDate PubStatus="accepted"><Year>2012</Year><Month>1</Month><Day>6</Day></PubMedPubDate><PubMedPubDate PubStatus="aheadofprint"><Year>2012</Year><Month>1</Month><Day>13</Day></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2012</Year><Month>1</Month><Day>24</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2012</Year><Month>1</Month><Day>24</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2012</Year><Month>6</Month><Day>23</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pii">S0378-5173(12)00010-5</ArticleId><ArticleId IdType="doi">10.1016/j.ijpharm.2012.01.006</ArticleId><ArticleId IdType="pubmed">22265911</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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