title: Folate-decorated PLGA nanoparticles as a rationally designed vehicle for the oral delivery of insulin.
abstract: OBJECTIVE
  The present study reports a novel approach for enhancing the oral absorption and hypoglycemic activity of insulin via encapsulation in folate-(FA) coupled polyethylene glycol (PEG)ylated polylactide-co-glycolide (PLGA) nanoparticles (NPs; FA-PEG-PLGA NPs).
  
  
  METHODS
  Insulin-loaded FA-PEG-PLGA NPs (size ∼260 nm; insulin loading ∼6.5% [w/w]; encapsulation efficiency: 87.0 ± 1.92%) were prepared by double-emulsion solvent evaporation method. The bioavailability and hypoglycemic activity of orally administered FA-insulin NPs were studied in diabetic rats.
  
  
  CONCLUSIONS
  FA-PEG-PLGA NPs (50 U/kg) exhibited a twofold increase in the oral bioavailability (double hypoglycemia) without any hypoglycemic shock as compared to subcutaneously administered standard insulin solution. Insulin NPs maintained a continual blood glucose level for 24 h, which, however, was transient (<8 h) in the case of subcutaneous insulin and associated with severe hypoglycemic shock. Overall, we have developed a patient-compliant, oral nanoformulation of insulin, once-daily administration of which would be sufficient to control diabetes for at least 24 h.
authors.affiliation: Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, Sector 67, SAS Nagar, (Mohali), Punjab 160062, India. sanyogjain@niper.ac.in
authors.forename: Sanyog
authors.initials: S
authors.lastname: Jain
authors.forename: Vishal V
authors.initials: VV
authors.lastname: Rathi
authors.forename: Amit K
authors.initials: AK
authors.lastname: Jain
authors.forename: Manasmita
authors.initials: M
authors.lastname: Das
authors.forename: Chandraiah
authors.initials: C
authors.lastname: Godugu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001786:Blood Glucose / Q000032:analysis; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D004337:Drug Carriers / Q000737:chemistry; D005492:Folic Acid / Q000737:chemistry*; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D007328:Insulin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D001786:Blood Glucose; D004337:Drug Carriers; D007004:Hypoglycemic Agents; D007328:Insulin; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D005492:Folic Acid