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Structural Elements Which Govern the Resistance of Intestinal Tissues to Compound Transport

Published online by Cambridge University Press:  15 February 2011

Werner Rubas ,
Mary Cromwell ,
Tom Gadek ,
Daljit Narindray  and
Randy Mrsny
Werner Rubas
Affiliation:
Pharmaceutical Research and Development, Drug Delivery Biology Group, Genentech, Inc., 460 Point San Bruno Boulevard, South San Francisco, CA 94080-4990.
Mary Cromwell
Affiliation:
Pharmaceutical Research and Development, Drug Delivery Biology Group, Genentech, Inc., 460 Point San Bruno Boulevard, South San Francisco, CA 94080-4990.
Tom Gadek
Affiliation:
Department of Bioorganic Chemistry Genentech, Inc., 460 Point San Bruno Boulevard, South San Francisco, CA 94080-4990.
Daljit Narindray
Affiliation:
Department of Bioorganic Chemistry Genentech, Inc., 460 Point San Bruno Boulevard, South San Francisco, CA 94080-4990.
Randy Mrsny
Affiliation:
Pharmaceutical Research and Development, Drug Delivery Biology Group, Genentech, Inc., 460 Point San Bruno Boulevard, South San Francisco, CA 94080-4990.
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Extract

The series of cyclized RGD peptides in this study demonstrated a very low partition into octanol as judged by HPLC. Thus, these molecules are likely to move predominantly through the paracellular pathway. Permeability across Caco-2 monolayers was determined using reversed phase HPLC and found to be restricted by molecular weight and possibly charge-charge interactions between the solute and charged moieties within the paracellular shunt. When normalized for molecular weight, molecules with a net charge between -1 and -2 demonstrated the highest permeabilities, which suggests an optimal net charge with respect to permeability.

Type
Research Article
Information
MRS Online Proceedings Library (OPL) , Volume 331: Symposium T – Biomaterials for Drug and Cell Delivery , 1993 , 179
Copyright
Copyright © Materials Research Society 1994

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References

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