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PLoS One. 2012;7(1):e29585. doi: 10.1371/journal.pone.0029585. Epub 2012 Jan 17.

Non inflammatory boronate based glucose-responsive insulin delivery systems.

Author information

1
School of Biomedical Informatics, The University of Texas Health Sciences Center at Houston, Houston, Texas, United States of America.

Abstract

Boronic acids, known to bind diols, were screened to identify non-inflammatory cross-linkers for the preparation of glucose sensitive and insulin releasing agglomerates of liposomes (Agglomerated Vesicle Technology-AVT). This was done in order to select a suitable replacement for the previously used cross-linker, ConcanavalinA (ConA), a lectin known to have both toxic and inflammatory effects in vivo. Lead-compounds were selected from screens that involved testing for inflammatory potential, cytotoxicity and glucose-binding. These were then conjugated to insulin-encapsulating nanoparticles and agglomerated via sugar-boronate ester linkages to form AVTs. In vitro, the particles demonstrated triggered release of insulin upon exposure to physiologically relevant concentrations of glucose (10 mmoles/L-40 mmoles/L). The agglomerates were also shown to be responsive to multiple spikes in glucose levels over several hours, releasing insulin at a rate defined by the concentration of the glucose trigger.

PMID:
22272238
PMCID:
PMC3260138
DOI:
10.1371/journal.pone.0029585
[Indexed for MEDLINE]
Free PMC Article

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