ArticlePharmaceutical research2004
Stimulation of triglyceride-rich lipoprotein secretion by polysorbate 80: in vitro and in vivo correlation using Caco-2 cells and a cannulated rat intestinal lymphatic model.
Article in Pharmaceutical research, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 75 citations in OpenAlex.
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- Bioactive-Chylomicrons for Oral Lymphatic Targeting of Berberine Chloride: Novel Flow-Blockage Assay in Tissue-Based and Caco-2 Cell Line Models.Pharmaceutical research · 2018Article
- Exploring the impact of drug properties on the extent of intestinal lymphatic transport - in vitro and in vivo studies.Pharmaceutical research · 2015Article
- In vitro lipolysis and intestinal transport of β-arteether-loaded lipid-based drug delivery systems.Pharmaceutical research · 2013Article
- Advanced drug delivery to the lymphatic system: lipid-based nanoformulations.International journal of nanomedicine · 2013Review
- Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation.International journal of nanomedicine · 2012Article
- Intestinal lymphatic transport for drug delivery.Advanced drug delivery reviews · 2011Review
- C-terminal domain deletion enhances the protective activity of cpa/cpb loaded solid lipid nanoparticles against Leishmania major in BALB/c mice.PLoS neglected tropical diseases · 2011Article
- Lipid-based formulations for danazol containing a digestible surfactant, Labrafil M2125CS: in vivo bioavailability and dynamic in vitro lipolysis.Pharmaceutical research · 2008Article
- Lipid-based delivery systems and intestinal lymphatic drug transport: a mechanistic update.Advanced drug delivery reviews · 2008Review
- Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo assess the effects of polysorbates 80 and 60 on intestinal lipoprotein processing in vitro, using Caco-2 cells, and to compare the results with those obtained using an in vivo intestinal lymphatic cannulated rat model.
methodsCaco-2 monolayers were used to monitor changes in lipoprotein secretion following exposure to excipients. In vivo data was obtained by monitoring intestinal lymphatic triglyceride levels following intraduodenal administration of the excipient to an anesthetised mesenteric lymph cannulated rat.
resultsCaco-2 cells digested the polysorbate 80 to liberate oleic acid, which was used by the cells to enhance basolateral secretion of triglyceride-rich lipoproteins including chylomicrons. This response was not seen with polysorbate 60. Polysorbate 80 elicited a similar response in vivo in the rat model, stimulating enhanced triglyceride secretion in mesenteric lymph. Inhibition of lipoprotein secretion by Cremophor EL in Caco-2 cells was reversed by co-administration with polysorbate 80.
conclusionsPolysorbate 80 promoted chylomicron secretion in Caco-2 cells and counteracted the inhibitory effects of other surfactants. These properties, in tandem with its P-gp inhibitory activity, make polysorbate 80 an ideal excipient for lymphotrophic vehicles. The ability to predict the in vivo response to Polysorbate 80 implies that the Caco-2 model is useful for studying absorption mechanisms from oral lipid-based formulations.
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