title: Efficacy of mucoadhesive hydrogel microparticles of whey protein and alginate for oral insulin delivery.
abstract: OBJECTIVE
  To evaluate the efficacy of mucoadhesive insulin-loaded whey protein (WP) /alginate (ALG) microparticles (MP) for oral insulin administration.
  
  
  METHODS
  Insulin-loaded microparticles (ins-MP) made of whey protein and alginate were prepared by a cold gelation technique and an adsorption method, without adjunction of organic solvent in order to develop a biocompatible vehicle for oral administration of insulin. In vitro characterization, evaluations of ins-MP in excised intestinal tissues and hypoglycaemic effects after intestinal administration in healthy rats were performed
  
  
  RESULTS
  The release properties and swelling behaviors, investigated in different pH buffers, demonstrated a release based on diffusion mechanism following matrix swelling. Mucoadhesion studies in rabbits and insulin transport experiments with excised intestinal rat tissues revealed that encapsulation in microparticles with mucoadhesive properties promotes insulin absorption across duodenal membranes and bioactivity protection. In vivo experiments reinforced the interest of encapsulation in whey protein/alginate combination. Confocal microscopic observations associated with blood glucose levels bring to light duodenal absorption of insulin biologically active following in vivo administration.
  
  
  CONCLUSIONS
  Insulin-loaded WP/ALG MP with high quantities of drug entrapped, in vitro matrix swelling and protective effect as well as excellent mucohadesive properties was developped. Improvement of intestinal delivery of insulin and increased in bioavailability were recorded.
authors.affiliation: Univ Clermont 1, UFR Pharmacie, ERT 18 Laboratoire de Biopharmacie, Clermont-Ferrand, 63001, France.
authors.forename: Emmanuelle
authors.initials: E
authors.lastname: Déat-Lainé
authors.forename: Valérie
authors.initials: V
authors.lastname: Hoffart
authors.forename: Ghislain
authors.initials: G
authors.lastname: Garrait
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Jarrige
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Cardot
authors.forename: Muriel
authors.initials: M
authors.lastname: Subirade
authors.forename: Eric
authors.initials: E
authors.lastname: Beyssac
mesh_terms: D000284:Administration, Oral; D000464:Alginates / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism; D004386:Duodenum / Q000378:metabolism / Q000648:ultrastructure; D020723:Glucuronic Acid / Q000737:chemistry / Q000378:metabolism; D006603:Hexuronic Acids / Q000737:chemistry / Q000378:metabolism; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate / Q000737:chemistry / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology; D007328:Insulin / Q000008:administration & dosage* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D008863:Microspheres; D008894:Milk Proteins / Q000737:chemistry* / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D014014:Tissue Adhesives / Q000737:chemistry* / Q000378:metabolism; D000067816:Whey Proteins
chemical_list: D000464:Alginates; D004337:Drug Carriers; D006603:Hexuronic Acids; D007004:Hypoglycemic Agents; D007328:Insulin; D008894:Milk Proteins; D014014:Tissue Adhesives; D000067816:Whey Proteins; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate; D020723:Glucuronic Acid