uu.seUppsala University Publications
Change search
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • ieee
  • modern-language-association
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf
Caco-2 Cell Conditions Enabling Studies of Drug Absorption from Digestible Lipid-Based Formulations
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. (Bergström research group)
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. (Bergström research group)ORCID iD: 0000-0002-8917-2612
2018 (English)In: Pharmaceutical Research, ISSN 0724-8741, Vol. 35, no 74, p. 1-11Article in journal (Refereed) Published
Abstract [en]

Purpose

To identify conditions allowing the use of cell-based models for studies of drug absorption during in vitro lipolysis of lipid-based formulations (LBFs).

Methods

Caco-2 was selected as the cell-based model system. Monolayer integrity was evaluated by measuring mannitol permeability after incubating Caco-2 cells in the presence of components available during lipolysis. Pure excipients and formulations representing the lipid formulation classification system (LFCS) were evaluated before and after digestion. Porcine mucin was evaluated for its capacity to protect the cell monolayer.

Results

Most undigested formulations were compatible with the cells (II-LC, IIIB-LC, and IV) although some needed mucin to protect against damaging effects (II-MC, IIIB-MC, I-LC, and IIIA-LC). The pancreatic extract commonly used in digestion studies was incompatible with the cells but the Caco-2 monolayers could withstand immobilized recombinant lipase. Upon digestion, long chain formulations caused more damage to Caco-2 cells than their undigested counterparts whereas medium chain formulations showed better tolerability after digestion.

Conclusions

Most LBFs and components thereof (undigested and digested) are compatible with Caco-2 cells. Pancreatic enzyme is not tolerated by the cells but immobilized lipase can be used in combination with the cell monolayer. Mucin is beneficial for critical formulations and digestion products.

Place, publisher, year, edition, pages
2018. Vol. 35, no 74, p. 1-11
Keywords [en]
Caco-2 cells, digestion, intestinal absorption, lipid-based formulation
National Category
Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy) Pharmacology and Toxicology
Research subject
Pharmaceutical Science
Identifiers
URN: urn:nbn:se:uu:diva-395485DOI: 10.1007/s11095-017-2327-8OAI: oai:DiVA.org:uu-395485DiVA, id: diva2:1362414
Available from: 2019-10-19 Created: 2019-10-19 Last updated: 2020-01-15Bibliographically approved

Open Access in DiVA

fulltext(1374 kB)3 downloads
File information
File name FULLTEXT01.pdfFile size 1374 kBChecksum SHA-512
fede4c08b623401f3ad79917cee3e88969880742ce5045c4c2ed8868d54421f7e93a11032afd80ea4609f280307f00892794c48e7ef2824ce1ff2e6ad8776c5f
Type fulltextMimetype application/pdf

Other links

Publisher's full texthttps://link.springer.com/article/10.1007/s11095-017-2327-8#citeas

Authority records BETA

Keemink, JannekeBergström, Christel

Search in DiVA

By author/editor
Keemink, JannekeBergström, Christel
By organisation
Department of Pharmacy
Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)Pharmacology and Toxicology

Search outside of DiVA

GoogleGoogle Scholar
Total: 3 downloads
The number of downloads is the sum of all downloads of full texts. It may include eg previous versions that are now no longer available

doi
urn-nbn

Altmetric score

doi
urn-nbn
Total: 11 hits
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • ieee
  • modern-language-association
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf