title: Surface engineered and ligand anchored nanobioconjugate: an effective therapeutic approach for oral insulin delivery in experimental diabetic rats.
abstract: The present study was designed to enhance intestinal absorption of insulin by nanobioconjugate formulated with PEGylation and Concanavalin A based targeted synergistic approach. The attempts were aimed at maximizing bioavailability and therapeutic efficacy of insulin by incorporating it in Concanavalin A anchored PEGylated nanoconstructs. The Con A anchored PEGylated PLGA diblock copolymer was synthesized by modified surface functionalization method, and was then characterized by FTIR and 1H NMR spectrum analysis. The nanoparticles from synthesized polymers were prepared and characterized for mean size and distribution by laser diffraction spectroscopy. The physicochemically characterized (by SEM and TEM) formulations were evaluated for optimum particle size, polydispersity index, zeta potential and entrapment efficiency 196.3±4.5 nm, 0.15±0.04, -25.6±1.68 and 44.6±3.5% respectively. The insulin encapsulation efficiency and in vitro release were assessed by bicinchoninic protein assay (BCA). The in vitro results corroborated in vivo studies carried out in experimentally created diabetic albino rats. The nano-encapsulated insulin was discovered to meet the requirements by achieving better stability, improved absorption and enhanced oral bioavailability elucidated by in vivo and in vitro bioassays.
authors: Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour Central University, Sagar, MP 470003, India.
authors: Rajeev
authors: R
authors: Sharma
authors: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer Rajasthan 305817, India.
authors: Umesh
authors: U
authors: Gupta
authors: Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour Central University, Sagar, MP 470003, India.
authors: Neeraj K
authors: NK
authors: Garg
authors: Department of Periodontics, College of Dental Medicine Georgia Regents University, 1120, 15th Street, Augusta, GA 30912, USA; Biosafety Support Unit, Regional Center for Biotechnology, Department of Biotechnology, Room No. 810, 8th Floor, Block No-9 C.G.O. Complex, Lodhi Road, New Delhi - 110003, India.
authors: Rajeev K
authors: RK
authors: Tyagi
authors: Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour Central University, Sagar, MP 470003, India. Electronic address: jnarendr@yahoo.co.in.
authors: N K
authors: NK
authors: Jain
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D001786:Blood Glucose / Q000378:metabolism; D018938:Caco-2 Cells; D003208:Concanavalin A / Q000737:chemistry; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy*; D016503:Drug Delivery Systems / Q000379:methods*; D065546:Drug Liberation; D004591:Electrophoresis, Polyacrylamide Gel; D004705:Endocytosis / Q000187:drug effects; D005455:Fluorescent Antibody Technique; D006801:Humans; D007328:Insulin / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use*; D008024:Ligands; D058726:Nanoconjugates / Q000737:chemistry* / Q000648:ultrastructure; D053758:Nanoparticles / Q000648:ultrastructure; D011092:Polyethylene Glycols / Q000737:chemistry; D011100:Polyglycolic Acid / Q000138:chemical synthesis / Q000737:chemistry; D066244:Proton Magnetic Resonance Spectroscopy; D017207:Rats, Sprague-Dawley; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D001786:Blood Glucose; D007328:Insulin; D008024:Ligands; D058726:Nanoconjugates; D003208:Concanavalin A; D011100:Polyglycolic Acid; D011092:Polyethylene Glycols
keywords: Concanavalin A; Insulin oral delivery; Nanoparticles; PEGylation; PLGA