Multi-ion-crosslinked nanoparticles with pH-responsive characteristics for oral delivery of protein drugs

J Control Release. 2008 Dec 8;132(2):141-9. doi: 10.1016/j.jconrel.2008.08.020. Epub 2008 Sep 9.

Abstract

pH-Responsive nanoparticles composed of chitosan (CS) and poly-gamma-glutamic acid (gamma-PGA) blended with tripolyphosphate (TPP) and MgSO(4) (multi-ion-crosslinked NPs) were prepared and characterized to determine their effectiveness in the oral delivery of insulin. Their counterparts without TPP and MgSO(4) (NPs) were used as a control. FT-IR and XRD results indicated that the spontaneous interaction between CS, insulin, gamma-PGA, MgSO(4) and TPP can form an ionically crosslinked network-structure, leading to the formation of nanoparticles. Multi-ion-crosslinked NPs were more compact than NPs, while their zeta potential values were comparable. During storage, multi-ion-crosslinked NPs suspended in deionized water were stable for at least 10 weeks. Multi-ion-crosslinked NPs had a superior stability over a broader pH range than NPs. In the in vitro release study, NPs failed to provide an adequate retention of loaded insulin in dissolution media compared to multi-ion-crosslinked NPs. Transepithelial-electrical-resistance and transport experiments demonstrated that multi-ion-crosslinked NPs significantly more effectively transported insulin than NPs; confocal visualization further validated the enhanced permeation of insulin via the paracellular pathway. The aforementioned results suggest that multi-ion-crosslinked NPs are a promising carrier for improved transmucosal delivery of insulin in the small intestine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Caco-2 Cells
  • Chitosan / chemistry
  • Drug Carriers / chemistry*
  • Drug Delivery Systems / methods
  • Electric Impedance
  • Humans
  • Hydrogen-Ion Concentration
  • Insulin / administration & dosage
  • Insulin / chemistry
  • Insulin / pharmacokinetics
  • Ions / chemistry
  • Magnesium Sulfate / chemistry
  • Nanoparticles / chemistry*
  • Particle Size
  • Polyglutamic Acid / chemistry
  • Polyphosphates / chemistry
  • Proteins / administration & dosage
  • Proteins / chemistry
  • Proteins / pharmacokinetics*
  • Spectroscopy, Fourier Transform Infrared
  • Tight Junctions / metabolism
  • X-Ray Diffraction

Substances

  • Drug Carriers
  • Insulin
  • Ions
  • Polyphosphates
  • Proteins
  • Polyglutamic Acid
  • Magnesium Sulfate
  • Chitosan
  • triphosphoric acid