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

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

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.

MeSH terms

  • Adjuvants, Immunologic / chemistry*
  • Chemistry, Pharmaceutical
  • Immunization* / instrumentation
  • Immunization* / methods
  • Injections, Intradermal
  • Microinjections* / instrumentation
  • Microinjections* / methods
  • Needles*
  • Organophosphorus Compounds / chemistry*
  • Polymers / chemistry*
  • Protein Stability
  • Serum Albumin, Bovine / administration & dosage
  • Solubility
  • Technology, Pharmaceutical / methods*
  • Time Factors
  • Vaccines / administration & dosage
  • Vaccines / immunology

Substances

  • Adjuvants, Immunologic
  • Organophosphorus Compounds
  • Polymers
  • Vaccines
  • poly(di(carboxylatophenoxy)phosphazene)
  • Serum Albumin, Bovine