Pure insulin nanoparticle agglomerates for pulmonary delivery

Langmuir. 2008 Dec 2;24(23):13614-20. doi: 10.1021/la802405p.

Abstract

Diabetes is a set of diseases characterized by defects in insulin utilization, either through autoimmune destruction of insulin-producing cells (Type I) or insulin resistance (Type II). Treatment options can include regular injections of insulin, which can be painful and inconvenient, often leading to low patient compliance. To overcome this problem, novel formulations of insulin are being investigated, such as inhaled aerosols. Sufficient deposition of powder in the peripheral lung to maximize systemic absorption requires precise control over particle size and density, with particles between 1 and 5 microm in aerodynamic diameter being within the respirable range. Insulin nanoparticles were produced by titrating insulin dissolved at low pH up to the pI of the native protein, and were then further processed into microparticles using solvent displacement. Particle size, crystallinity, dissolution properties, structural stability, and bulk powder density were characterized. We have demonstrated that pure drug insulin microparticles can be produced from nanosuspensions with minimal processing steps without excipients, and with suitable properties for deposition in the peripheral lung.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Carriers / chemistry*
  • Drug Delivery Systems*
  • Hydrogen-Ion Concentration
  • Insulin / chemistry*
  • Lung / metabolism*
  • Materials Testing
  • Nanoparticles / chemistry*
  • Particle Size
  • Powders / chemistry*
  • Surface Properties
  • Temperature
  • Time Factors

Substances

  • Drug Carriers
  • Insulin
  • Powders