| Antacid co-encapsulated polyester nanoparticles for peroral delivery of insulin: Development, pharmacokinetics, biodistribution and pharmacodynamics. | |
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MedLine Citation:
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PMID: 22227604 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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The in vitro/in vivo characterization of antacid-insulin co-encapsulated poly(lactide-co-glycolide) (PLGA) nanoparticles is presented here. The optimized nanoparticle composition has 1% surfactant (didodecyl dimethylammonium bromide) and 2% antacid (magnesium hydroxide or zinc carbonate) in the size range ∼136-143nm with ∼81-85% entrapment of insulin at a 4% (w/w) initial load to that of polymer. Molecular characterization using circular dichroism, fluorescence and Fourier transform infrared spectroscopy showed that the structural integrity of insulin was maintained during formulation. Furthermore, the encapsulated insulin was well protected under in vitro simulated gastric and intestinal fluids. Nanoparticle insulin results in six fold increase in oral bioavailability to that of plain insulin in healthy rats. In diabetic rats, a 120IU/kg oral dose of insulin nanoparticles achieved an equivalent blood glucose lowering effect to a 20IU/kg subcutaneous (sc) dose of insulin solution, the nadir in blood glucose concentration occurring 24h and 1h post-administration, respectively. Both sc insulin and oral nanoparticle insulin partially attenuated hyperglycemia-induced inflammation caused by tumor necrosis factor α, but not by interleukin-6 or C-reactive protein; on the other hand, subcutaneous insulin was found to be more effective on lipid profile measured in the form of high density lipoprotein, cholesterol and triglyceride. Successful oral insulin could be beneficial in type II complications. |
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Authors:
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G Sharma; C F van der Walle; M N V Ravi Kumar |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-12-30 |
Journal Detail:
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Title: International journal of pharmaceutics Volume: - ISSN: 1873-3476 ISO Abbreviation: - Publication Date: 2011 Dec |
Date Detail:
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Created Date: 2012-1-9 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 7804127 Medline TA: Int J Pharm Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2012. Published by Elsevier B.V. |
Affiliation:
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Strathclyde Institute of Pharmacy and Biomedical Sciences (SIPBS), University of Strathclyde, 27 Taylor Street, Glasgow G4 0NR, UK. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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