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Pharm Res. 2011 Jan;28(1):58-65. doi: 10.1007/s11095-010-0133-7. Epub 2010 Apr 6.

Microneedles with intrinsic immunoadjuvant properties: microfabrication, protein stability, and modulated release.

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  • 1Research & Development, Apogee Technology, Inc., 129 Morgan Drive, Norwood, Massachusetts 02062, USA. aandrianov@apogeebio.com

Abstract

PURPOSE:

Intradermal immunization using microneedles requires compatible immunoadjuvant system. To address this challenge, we investigated microneedles coated with polyphosphazene polyelectrolyte, which served both as microfabrication material and an immunoadjuvant compound.

METHODS:

Coated microneedles were fabricated by depositing formulations containing Poly[di(carboxylatophenoxy)phosphazene], PCPP, on metal shafts, and their physico-chemical characterization was conducted.

RESULTS:

Microfabrication of PCPP-coated microneedles exhibited strong dependence on protein-PCPP interactions in solutions and allowed for high efficiency of protein encapsulation. 70°C thermal inactivation studies demonstrated a remarkable increase in functional stability of protein in coated microneedles compared to solution formulation. A potential for modulation of protein release from coated microneedles has been demonstrated through ionic complexation of PCPP with small ions.

CONCLUSIONS:

Microneedles containing PCPP coatings provide improved protein stability, modulated release, and protein-friendly microfabrication process.

[PubMed - indexed for MEDLINE]
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