title: Mucoadhesive polyelectrolyte microparticles containing recombinant human insulin and its analogs aspart and lispro.
abstract: Microparticles containing recombinant human insulin and its analogs aspart and lispro were prepared using an alternate adsorption of chitosan and dextran sulfate from solutions onto microaggregates of protein-dextran sulfate insoluble complex. The following properties of polyelectrolyte hormone-containing microparticles were studied: pH stability, surface charge, mucoadhesive properties, Ca(2+) binding, degradation under the influence of proteases (trypsin, chymotrypsin). The influence of the self-association ability of encapsulated insulins on the form of protein releasing from microparticles was studied. Insulins aspart and lispro released from the microparticles as monomers were more liable to proteolysis than human insulin released as a hexamer. The combined effect of properties of polyelectrolyte microparticles and of encapsulated recombinant proteins on the bioavailability of insulin under peroral administration is discussed.
authors.affiliation: Chemical Faculty, Lomonosov Moscow State University, Russia. nbalab@enzyme.chem.msu.ru
authors.forename: N G
authors.initials: NG
authors.lastname: Balabushevich
authors.forename: M A
authors.initials: MA
authors.lastname: Pechenkin
authors.forename: I N
authors.initials: IN
authors.lastname: Zorov
authors.forename: E D
authors.initials: ED
authors.lastname: Shibanova
authors.forename: N I
authors.initials: NI
authors.lastname: Larionova
mesh_terms: D000327:Adsorption; D001682:Biological Availability; D055598:Chemical Phenomena; D048271:Chitosan / Q000737:chemistry; D016264:Dextran Sulfate / Q000737:chemistry; D004573:Electrolytes / Q000737:chemistry; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007328:Insulin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D061267:Insulin Aspart; D061268:Insulin Lispro; D007700:Kinetics; D009092:Mucous Membrane / Q000378:metabolism; D049329:Nanostructures / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D055503:Protein Multimerization; D020836:Protein Structure, Quaternary; D011994:Recombinant Proteins / Q000737:chemistry* / Q000378:metabolism*
chemical_list: D004573:Electrolytes; D007328:Insulin; D061268:Insulin Lispro; D011108:Polymers; D011994:Recombinant Proteins; D048271:Chitosan; D016264:Dextran Sulfate; D061267:Insulin Aspart