In Vivo Performance of Innovative Polyelectrolyte Matrices for Hot Melt Extrusion of Amorphous Drug Systems

dc.accessRightsAnonymous*
dc.audienceScienceen_US
dc.contributor.authorDitzinger, Felix
dc.contributor.authorWieland, Rebecca
dc.contributor.authorStatelova, Marina
dc.contributor.authorVertzoni, Maria
dc.contributor.authorHolm, Rene
dc.contributor.authorKuentz, Martin
dc.date.accessioned2020-11-12T15:47:49Z
dc.date.available2020-11-12T15:47:49Z
dc.date.issued2020
dc.description.abstractHot melt extrusion of amorphous systems has become a pivotal technology to cope with challenges of poorly water-soluble drugs. Previous research showed that small molecular additives with targeted molecular interactions enabled introduction of a polyelectrolyte matrix into hot melt extrusion that would otherwise not be possible to process due to the unfavorable properties upon heating of the pure polymer. Carboxymethyl cellulose sodium (NaCMC) with lysine or alternatively meglumine led to modified polymeric matrices that showed adequate processability by hot melt extrusion and yielded stable amorphous formulations. The investigated formulations, including fenofibrate as a model drug, were characterized by attenuated total reflectance Fourier transform infrared spectroscopy, differential scanning calorimetry, and viscosity measurements after aqueous dispersion. Further biopharmaceutical assessment started with biorelevant nonsink dissolution testing followed by a pharmacokinetic in vivo study in rats. The in vitro assessment showed superiority of the lysine-containing formulation in the extent of in vitro supersaturation and overall drug release. In accordance with this, the in vivo study also demonstrated increased exposure of the amorphous formulations and in particular for the system containing lysine. In summary, the combination of polyelectrolytes with interacting additives presents a promising opportunity for the formulation of poorly water-soluble drugs.en_US
dc.identifier.doi10.1021/acs.molpharmaceut.0c00485
dc.identifier.issn1543-8384
dc.identifier.issn1543-8392
dc.identifier.urihttps://irf.fhnw.ch/handle/11654/31788
dc.identifier.urihttps://doi.org/10.26041/fhnw-3604
dc.issue8en_US
dc.language.isoenen_US
dc.publisherAmerican Chemical Societyen_US
dc.relation.ispartofMolecular Pharmaceuticsen_US
dc.subjectpoorly water-soluble drugen_US
dc.subjectin vivo studyen_US
dc.subjecthot melt extrusionen_US
dc.subjectpolyelectrolyte matricesen_US
dc.subjectNaCMCen_US
dc.subjectamorphous solid dispersionsen_US
dc.titleIn Vivo Performance of Innovative Polyelectrolyte Matrices for Hot Melt Extrusion of Amorphous Drug Systemsen_US
dc.type01A - Beitrag in wissenschaftlicher Zeitschrift
dc.volume17en_US
dspace.entity.typePublication
fhnw.InventedHereYesen_US
fhnw.IsStudentsWorknoen_US
fhnw.PublishedSwitzerlandYesen_US
fhnw.ReviewTypeAnonymous ex ante peer review of a complete publicationen_US
fhnw.affiliation.hochschuleHochschule für Life Sciencesde_CH
fhnw.affiliation.institutInstitut für Pharma Technologyde_CH
fhnw.pagination3053-3061en_US
fhnw.publicationOnlineJaen_US
fhnw.publicationStatePublisheden_US
relation.isAuthorOfPublicationc98cfb03-0873-44b0-9b19-e4193630a183
relation.isAuthorOfPublication68819448-8611-488b-87bc-1b1cf9a6a1b4
relation.isAuthorOfPublication.latestForDiscovery68819448-8611-488b-87bc-1b1cf9a6a1b4
Dateien
Originalbündel
Gerade angezeigt 1 - 1 von 1
Lade...
Vorschaubild
Name:
Ditzinger Mol Pharm In vivo performance of matrices IRF version.pdf
Größe:
430.48 KB
Format:
Adobe Portable Document Format
Beschreibung: