Balabushevich, N.G.N.G.BalabushevichPechenkin, M.A.M.A.PechenkinShibanova, E.D.E.D.ShibanovaVolodkin, D.V.D.V.VolodkinMikhalchik, E.V.E.V.Mikhalchik2022-03-042022-03-042013https://publica.fraunhofer.de/handle/publica/23297410.1002/mabi.201300207Multicomponent 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.en610572journal article