ArticleInternational journal of molecular sciences2016
Investigation of Enantioselective Membrane Permeability of α-Lipoic Acid in Caco-2 and MDCKII Cell.
Article in International journal of molecular sciences, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- Enhancing the Pharmaceutical Profile of Alpha Lipoic Acid: Cyclodextrin Inclusion Complexation for Improved Stability and Bioavailability.Pharmaceutics · 2026Article
- Nanotechnological Approaches to Enhance the Potential of α-Lipoic Acid for Application in the Clinic.Antioxidants (Basel, Switzerland) · 2024Review
- Alpha-Lipoic Acid Promotes Intestinal Epithelial Injury Repair by Regulating MAPK Signaling Pathways.Mediators of inflammation · 2022Article
- Development of a Hierarchical Support Vector Regression-Based In Silico Model for Caco-2 Permeability.Pharmaceutics · 2021Article
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Authors and funding
5 authors.
Funding
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Abstract
α-Lipoic acid (LA) contains a chiral carbon and exists as two enantiomers (R-α-lipoic acid (RLA) and S-α-lipoic acid (SLA)). We previously demonstrated that oral bioavailability of RLA is better than that of SLA. This difference arose from the fraction absorbed multiplied by gastrointestinal availability (F(a) × F(g)) and hepatic availability (F(h)) in the absorption phase. However, it remains unclear whether F(a) and/or F(g) are involved in enantioselectivity. In this study, Caco-2 cells and Madin-Darby canine kidney strain II cells were used to assess the enantioselectivity of membrane permeability. LA was actively transported from the apical side to basal side, regardless of the differences in its steric structure. Permeability rates were proportionally increased in the range of 10-250 µg LA/mL, and the permeability coefficient did not differ significantly between enantiomers. Hence, we conclude that enantioselective pharmacokinetics arose from the metabolism (F(h) or F(g) × F(h)), and definitely not from the membrane permeation (F(a)) in the absorption phase.
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