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Multifunctional Polyelectrolyte Microparticles for Oral Insulin Delivery
Author(s) -
Balabushevich Nadezhda G.,
Pechenkin Mikhail A.,
Shibanova Elena D.,
Volodkin Dmitry V.,
Mikhalchik Elena V.
Publication year - 2013
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201300207
Subject(s) - bioavailability , polyelectrolyte , chitosan , insulin , chemistry , protease , microparticle , proteolysis , pharmacology , dextran , oral administration , biochemistry , chemical engineering , polymer , endocrinology , medicine , enzyme , organic chemistry , engineering
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 Ca 2+ 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.