Abstract
Mucoadhesion implicates the possibility to achieve a very close contact between drug delivery system and biological membrane. This may increase the concentration gradient and also reduce the enzymatic degradation of peptide drugs during the absorption process.
A multiple-unit BDDS has been developed based on microspheres of poly-(2-hydroxyethylmethacrylate). The beads were loaded with the model peptide 9-desglycinamide, 8-arginine vasopressin (DGAVP) and coated with mucoadhesive polymers. Mucoadhesive properties were evaluated by measuring the force of detachment from porcine intestinal mucosa and studying the transit of microspheres in an in-situ perfused ileal loop in conscious rats. The mean residence time of microspheres coated with Polycarbophil appeared to be significantly increased in comparison with non-coated spheres and those coated with Carbopol.
An in-vitro model was developed to study the influence of mucoadhesion on peptide transport across the intestinal wall under controlled conditions. Significantly more DGAVP was found in the transmucosal compartments when delivered from mucoadhesive carriers in comparison to the non-adhesive control. These preliminary results indicate a beneficial influence of muco-adhesive polymers on the intestinal absorption of peptides.
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References
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Lehr, CM., Bouwstra, J.A., Tukker, J.J., Verhoef, J., de Boer, A.G., Junginger, H.E. (1990). Improved Oral Peptide Delivery by Means of Mucoadhesion. In: Crommelin, D.J.A., Schellekens, H. (eds) From Clone to Clinic. Developments in Biotherapy, vol 1. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-3780-5_41
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DOI: https://doi.org/10.1007/978-94-011-3780-5_41
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