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Sökning: WFRF:(Bergström Christel A. S.) > Experiences and Tra...

LIBRIS Formathandbok  (Information om MARC21)
FältnamnIndikatorerMetadata
00004804naa a2200505 4500
001oai:DiVA.org:uu-522682
003SwePub
008240208s2024 | |||||||||||000 ||eng|
0247 a https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-5226822 URI
0247 a https://doi.org/10.1021/acs.molpharmaceut.3c008722 DOI
040 a (SwePub)uu
041 a engb eng
042 9 SwePub
072 7a ref2 swepub-contenttype
072 7a art2 swepub-publicationtype
1001 a Emeh, Prosperu Uppsala universitet,Institutionen för farmaci4 aut0 (Swepub:uu)proem558
2451 0a Experiences and Translatability of In Vitro and In Vivo Models to Evaluate Caprate as a Permeation Enhancer
264 1b American Chemical Society (ACS),c 2024
338 a print2 rdacarrier
520 a Transient permeation enhancers (PEs) have been widely used to improve the oral absorption of macromolecules. During pharmaceutical development, the correct selection of the macromolecule, PE, and the combination needs to be made to maximize oral bioavailability and ensure successful clinical development. Various in vitro and in vivo methods have been investigated to optimize this selection. In vitro methods are generally preferred by the pharmaceutical industry to reduce the use of animals according to the "replacement, reduction, and refinement" principle commonly termed "3Rs," and in vitro methods typically have a higher throughput. This paper compares two in vitro methods that are commonly used within the pharmaceutical industry, being Caco-2 and an Ussing chamber, to two in vivo models, being in situ intestinal instillation to rats and in vivo administration via an endoscope to pigs. All studies use solution formulation of sodium caprate, which has been widely used as a PE, and two macromolecules, being FITC-dextran 4000 Da and MEDI7219, a GLP-1 receptor agonist peptide. The paper shares our experiences of using these models and the challenges with the in vitro models in mimicking the processes occurring in vivo. The paper highlights the need to consider these differences when translating data generated using these in vitro models for evaluating macromolecules, PE, and combinations thereof for enabling oral delivery.
650 7a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Farmaceutiska vetenskaper0 (SwePub)301012 hsv//swe
650 7a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Pharmaceutical Sciences0 (SwePub)301012 hsv//eng
650 7a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Farmakologi och toxikologi0 (SwePub)301022 hsv//swe
650 7a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Pharmacology and Toxicology0 (SwePub)301022 hsv//eng
653 a transient permeation enhancer
653 a sodium caprate
653 a oral peptide delivery
653 a Ussing chamber
653 a Caco-2
653 a intestinal bolus instillation
653 a in vitro-in vivotranslatability
7001 a Breitholtz, Katarinau AstraZeneca, Drug Metab & Pharmacokinet, Res & Early Dev, Cardiovasc Renal & Metab,BioPharmaceut R&D, SE-43183 Gothenburg, Sweden.4 aut
7001 a Berg, Staffanu AstraZeneca, Adv Drug Delivery, Pharmaceut Sci, R&D, SE-43183 Gothenburg, Sweden.4 aut
7001 a Vedin, Charlottau AstraZeneca, Drug Metab & Pharmacokinet, Res & Early Dev, Cardiovasc Renal & Metab,BioPharmaceut R&D, SE-43183 Gothenburg, Sweden.4 aut
7001 a Englund, Mariau AstraZeneca, Drug Metab & Pharmacokinet, Res & Early Dev, Cardiovasc Renal & Metab,BioPharmaceut R&D, SE-43183 Gothenburg, Sweden.4 aut
7001 a Uggla, Teresiau AstraZeneca, BioPharmaceut R&D, Clin Pharmacol & Safety Sci, Lab Anim Sci, SE-43183 Gothenburg, Sweden.4 aut
7001 a Antonsson, Malinu AstraZeneca, BioPharmaceut R&D, Clin Pharmacol & Safety Sci, Lab Anim Sci, SE-43183 Gothenburg, Sweden.4 aut
7001 a Nunes, Filipeu AstraZeneca, BioPharmaceut R&D, Clin Pharmacol & Safety Sci, Lab Anim Sci, SE-43183 Gothenburg, Sweden.4 aut
7001 a Hilgendorf, Constanzeu AstraZeneca, Drug Metab & Pharmacokinet, Res & Early Dev, Cardiovasc Renal & Metab,BioPharmaceut R&D, SE-43183 Gothenburg, Sweden.4 aut
7001 a Bergström, Christel A. S.u Uppsala Univ, Swedish Drug Delivery Ctr, Dept Pharm, SE-75123 Uppsala, Sweden.4 aut
7001 a Davies, Nigelu AstraZeneca, Adv Drug Delivery, Pharmaceut Sci, R&D, SE-43183 Gothenburg, Sweden.4 aut
7102 a Uppsala universitetb Institutionen för farmaci4 org
7730 t Molecular Pharmaceuticsd : American Chemical Society (ACS)g 21:1, s. 313-324q 21:1<313-324x 1543-8384x 1543-8392
8564 8u https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-522682
8564 8u https://doi.org/10.1021/acs.molpharmaceut.3c00872

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