Novel insulin thiomer nanoparticles: in vivo evaluation of an oral drug delivery system.

Abstract:

:It was aim of the study to investigate the in vivo potential of a novel insulin-thiomer complex nanoparticulate delivery system. Insulin loaded nanoparticles were obtained by the formation of hydrogen bonds between poly(vinyl pyrrolidone) (PVP) and poly(acrylic acid)-cysteine (PAA-Cys) or poly(acrylic acid) (PAA), respectively, in the presence of insulin. Dissolution behavior of insulin from tablets as well as nanoparticulate suspensions was evaluated in vitro. Serum insulin concentrations and reduction of blood sugar values were determined after oral administration of nanoparticles formulated as enteric coated tablets and suspensions. Results displayed a low serum insulin concentration and pharmacological efficacy in terms of blood sugar reduction after oral administration of enteric coated tablets. On the contrary, nanoparticulate suspensions led to significant serum insulin concentrations. Furthermore a 2.3-fold improvement of the AUC of insulin could be achieved due to the use of thiolated PAA instead of unmodified PAA. In addition, a blood sugar reduction of 22% was observed. Results demonstrate that this novel complex nanoparticulate formulation is an encouraging new attempt toward the noninvasive delivery of peptide drugs.

journal_name

Biomacromolecules

journal_title

Biomacromolecules

authors

Deutel B,Greindl M,Thaurer M,Bernkop-Schnürch A

doi

10.1021/bm700916h

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

278-85

issue

1

eissn

1525-7797

issn

1526-4602

journal_volume

9

pub_type

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