Concanavalin A conjugated biodegradable nanoparticles for oral insulin delivery

Major research issues in oral protein delivery include the stabilization of protein in delivery devices which could increase its oral bioavailability. The study deals with development of oral insulin delivery system utilizing biodegradable poly(lactic-co-glycolic acid) (PLGA) nanoparticles and modif...

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Bibliographic Details
Published in:Journal of nanoparticle research : an interdisciplinary forum for nanoscale science and technology 2012-11, Vol.14 (11), p.1-14, Article 1219
Main Authors: Hurkat, Pooja, Jain, Aviral, Jain, Ashish, Shilpi, Satish, Gulbake, Arvind, Jain, Sanjay K.
Format: Article
Language:English
Subjects:
Bioavailability
Biodegradability
Biodegradation
Characterization and Evaluation of Materials
Chemistry and Materials Science
Computing time
Inorganic Chemistry
Insulin
Lasers
Materials Science
Nanoparticles
Nanotechnology
Optical Devices
Optics
Photonics
Physical Chemistry
Proteins
Rats
Research Paper
Stability
Uptakes
Zeta potential
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Summary:Major research issues in oral protein delivery include the stabilization of protein in delivery devices which could increase its oral bioavailability. The study deals with development of oral insulin delivery system utilizing biodegradable poly(lactic-co-glycolic acid) (PLGA) nanoparticles and modifying its surface with Concanavalin A to increase lymphatic uptake. Surface-modified PLGA nanoparticles were characterized for conjugation efficiency of ligand, shape and surface morphology, particle size, zeta potential, polydispersity index, entrapment efficiency, and in vitro drug release. Stability of insulin in the developed formulation was confirmed by SDS-PAGE, and integrity of entrapped insulin was assessed using circular dichroism spectrum. Ex vivo study was performed on Wistar rats, which exhibited the higher intestinal uptake of Con A conjugated nanoparticles. In vivo study performed on streptozotocin-induced diabetic rats which indicate that a surface-modified nanoparticle reduces blood glucose level effectively within 4 h of its oral administration. In conclusion, the present work resulted in successful production of Con A NPs bearing insulin with sustained release profile, and better absorption and stability. The Con A NPs showed high insulin uptake, due to its relative high affinity for non-reducing carbohydrate residues i.e., fucose present on M cells and have the potential for oral insulin delivery in effective management of Type 1 diabetes condition.
ISSN:1388-0764
1572-896X
DOI:10.1007/s11051-012-1219-4