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Amorphous solid dispersions of enzalutamide and novel polysaccharide derivatives: Investigation of relationships between polymer structure and performance

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dc.contributor.authorWilson, Venecia R.en
dc.contributor.authorLou, Xiaochunen
dc.contributor.authorOsterling, Donald J.en
dc.contributor.authorStolarik, DeAnne F.en
dc.contributor.authorJenkins, Gary J.en
dc.contributor.authorNichols, Brittany L. B.en
dc.contributor.authorDong, Yifanen
dc.contributor.authorEdgar, Kevin J.en
dc.contributor.authorZhang, Geoff G. Z.en
dc.contributor.authorTaylor, Lynne S.en
dc.date.accessioned2022-02-22T23:58:57Zen
dc.date.available2022-02-22T23:58:57Zen
dc.date.issued2020-10-28en
dc.date.updated2022-02-22T23:58:55Zen
dc.description.abstractAmorphous solid dispersion (ASD) is a widely employed formulation technique for drugs with poor aqueous solubility. Polymers are integral components of ASDs, but mechanisms by which polymers lead to the generation and maintenance of supersaturated solutions, which enhance oral absorption in vivo, are poorly understood. Herein, a diverse group of newly synthesized cellulose derivatives was evaluated for their ability to inhibit crystallization of enzalutamide, a poorly soluble compound used to treat prostate cancer. ASDs were prepared from selected polymers, specifically a somewhat hydrophobic polymer that was extremely effective at inhibiting drug crystallization, and a less effective, but more hydrophilic, crystallization inhibitor, that might afford better release. Drug membrane transport rate was evaluated in vitro and compared to in vivo performance, following oral dosing in rats. Good correlation was noted between the in vitro diffusion cell studies and the in vivo data. The ASD formulated with the less effective crystallization inhibitor outperformed the ASD prepared with the highly effective crystallization inhibitor in terms of the amount and rate of drug absorbed in vivo. This study provides valuable insight into key factors impacting oral absorption from enabling ASD formulations, and how best to evaluate such formulations using in vitro approaches.en
dc.description.versionPublished versionen
dc.format.mimetypeapplication/pdfen
dc.identifier.citationWilson, V.R., Lou, X., Osterling, D.J. et al. Amorphous solid dispersions of enzalutamide and novel polysaccharide derivatives: investigation of relationships between polymer structure and performance. Sci Rep 10, 18535 (2020). https://doi.org/10.1038/s41598-020-75077-7en
dc.identifier.doihttps://doi.org/10.1038/s41598-020-75077-7en
dc.identifier.orcidEdgar, Kevin [0000-0002-9459-9477]en
dc.identifier.urihttp://hdl.handle.net/10919/108831en
dc.language.isoenen
dc.publisherSpringer Natureen
dc.rightsCreative Commons Attribution 4.0 Internationalen
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.subjectcrystallization kineticsen
dc.subjectdrug-rich nanodropleten
dc.subjectpolymer-drug interactionen
dc.subjectamorphous solid dispersionen
dc.subjectPharmacology & Pharmacyen
dc.titleAmorphous solid dispersions of enzalutamide and novel polysaccharide derivatives: Investigation of relationships between polymer structure and performanceen
dc.title.serialScientific Reportsen
dc.typeArticle - Refereeden
dc.type.dcmitypeTexten
dc.type.otherArticleen
dc.type.otherJournalen
pubs.organisational-group/Virginia Techen
pubs.organisational-group/Virginia Tech/Natural Resources & Environmenten
pubs.organisational-group/Virginia Tech/Natural Resources & Environment/Sustainable Biomaterialsen
pubs.organisational-group/Virginia Tech/University Research Institutesen
pubs.organisational-group/Virginia Tech/University Research Institutes/Fralin Life Sciencesen
pubs.organisational-group/Virginia Tech/All T&R Facultyen
pubs.organisational-group/Virginia Tech/Natural Resources & Environment/CNRE T&R Facultyen
pubs.organisational-group/Virginia Tech/University Research Institutes/Fralin Life Sciences/Durelle Scotten

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