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Drug delivery studies in Caco-2 monolayers. III. Intestinal transport of various vasopressin analogues in the presence of lysophosphatidylcholine

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The transport of a series of vasopressin and oxytocin analogues with varying lipophilicities was studied in Caco-2 monolayers. Transport was studied across the bare monolayer and after treatment with a phospholipid absorption enhancer, palmitoyl lysophosphatidylcholine. The range in lipophilicity of the analogues, estimated as the capacity factor, was found to be from 0.19 to 3.43. The intrinsic transport of the peptides across Caco-2 monolayers was found to be low. The apparent permeability coefficients, Papp, were in the range of 2 × 10-8-6 × 107 cm/s. However, peptide transport was significantly greater (Papp in the range of 5 × 10-6-2 × 10-5 cm/s) when facilitated by addition of palmitoyllysophosphatidylcholine. The results suggest that polypeptide transport across Caco-2 monolayers does not depend on lipophilicity, but that the facilitated transport does depend on the lipophilicity.

OriginalsprogEngelsk
TidsskriftInternational Journal of Pharmaceutics
Vol/bind114
Udgave nummer2
Sider (fra-til)151-157
Antal sider7
ISSN0378-5173
DOI
StatusUdgivet - 14 feb. 1995

ID: 239817259