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Multifunctional polyelectrolyte microparticles for oral insulin delivery

: Balabushevich, N.G.; Pechenkin, M.A.; Shibanova, E.D.; Volodkin, D.V.; Mikhalchik, E.V.


Macromolecular bioscience 13 (2013), Nr.10, S.1379-1388
ISSN: 1616-5187
Fraunhofer IBMT ()

Multicomponent insulin-containing microparticles are prepared by layer-by-layer assembly of dextran sulfate and chitosan on the core of protein-polyanion complex with or without protease inhibitors. Oral bioavailability of the encapsulated insulin is improved due to the cumulative effect of each component. A physico-chemical study shows that the particle design allows adjustment of the pH-dependent profile of the insulin release, as well as mucoadhesive properties and Ca2+ binding ability of the microparticles. Supplementing the microparticles with 2-3% protease inhibitors fully prevents proteolysis of human insulin. The pharmacological effect of microencapsulated insulin in doses 50-100 IU kg-1 is demonstrated in chronic experiments after oral administration to diabetic rats fed ad libitum.