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Efficacy of Mucoadhesive Hydrogel Microparticles of Whey Protein and Alginate for Oral Insulin Delivery

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ABSTRACT

Purpose

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.

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Abbreviations

ALG:

alginate

EE:

encapsulation efficiency

ins-MP:

insulin-loaded microparticles

MP:

microparticle

WP:

whey protein

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Authors and Affiliations

  1. Univ Clermont 1, UFR Pharmacie, ERT 18 Laboratoire de Biopharmacie, Clermont-Ferrand, 63001, France

    Emmanuelle Déat-Lainé, Valérie Hoffart, Ghislain Garrait, Jean-François Jarrige, Jean-Michel Cardot & Eric Beyssac

  2. Institute of Nutraceuticals & Functional Foods (INAF), Milk and Dairy Products (STELA Center), Université Laval, Pavillon Paul Comtois, Sainte-Foy, Québec, Canada, G1K 7P4

    Muriel Subirade

Authors
  1. Emmanuelle Déat-Lainé
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  2. Valérie Hoffart
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  3. Ghislain Garrait
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  4. Jean-François Jarrige
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  5. Jean-Michel Cardot
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  6. Muriel Subirade
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  7. Eric Beyssac
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Corresponding author

Correspondence to Eric Beyssac.

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Déat-Lainé, E., Hoffart, V., Garrait, G. et al. Efficacy of Mucoadhesive Hydrogel Microparticles of Whey Protein and Alginate for Oral Insulin Delivery. Pharm Res 30, 721–734 (2013). https://doi.org/10.1007/s11095-012-0913-3

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  • DOI: https://doi.org/10.1007/s11095-012-0913-3

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