Controlled release of dexamethasone from microcapsules produced by polyelectrolyte layer-by-layer nanoassembly

Pharm Res. 2005 May;22(5):826-35. doi: 10.1007/s11095-005-2600-0. Epub 2005 May 17.

Abstract

Purpose: In an effort to expand the application of core-shell structures fabricated by electrostatic layer-by-layer (LbL) self-assembling for drug delivery, this study reports the controlled release of dexamethasone from microcrystals encapsulated with a polyelectrolyte shell.

Methods: The LbL self-assembly process was used to produce dexamethasone particles encapsulated with up to five double layers formed by alternating the adsorption of positively charged poly(dimethyldiallyl ammonium chloride), negatively charged sodium poly(styrenesulfonate) and depending on the pH positively or negatively charged gelatin A or B onto the surface of the negatively charged dexamethasone particles. The nano-thin shells were characterized by quartz crystal microbalance measurements, microelectrophoresis, microcalorimetry, confocal microscopy, and scanning electron microscopy. In vitro release of dexamethasone from the microcapsules suspended in water or carboxymethylcellulose gels were measured using vertical Franz-type diffusion cells.

Results: Sonication of a suspension of negatively charged dexamethasone microcrystals in a solution of PDDA not only reduced aggregation but also reduced the size of the sub-micrometer particles. Assembly of multiple polyelectrolyte layers around these monodispersed cores produced a polyelectrolyte multilayer shell around the drug microcrystals that allowed for controlled release depending on the composition and the number of layers.

Conclusions: Direct surface modification of dexamethasone microcrystals via the LbL process produced monodispersed suspensions with diffusion-controlled sustained drug release via the polyelectrolyte multilayer shell.

Publication types

  • Comparative Study

MeSH terms

  • Capsules / analysis
  • Capsules / chemistry
  • Cell Aggregation
  • Cell Survival / drug effects*
  • Chemistry, Pharmaceutical / methods
  • Crystallization
  • Delayed-Action Preparations / administration & dosage
  • Delayed-Action Preparations / pharmacokinetics*
  • Dexamethasone / administration & dosage
  • Dexamethasone / analysis
  • Dexamethasone / pharmacokinetics*
  • Diazonium Compounds / analysis
  • Electrolytes / analysis
  • Electrolytes / chemistry
  • Hot Temperature
  • Microspheres*
  • Nanotechnology / methods
  • Particle Size*
  • Polymers / analysis
  • Polymers / chemistry
  • Powders / analysis
  • Powders / chemistry
  • Pyridines / analysis
  • Sonication
  • Static Electricity
  • Technology, Pharmaceutical / methods

Substances

  • Capsules
  • Delayed-Action Preparations
  • Diazonium Compounds
  • Electrolytes
  • Polymers
  • Powders
  • Pyridines
  • 4-(2'-pyridyldithio)benzyldiazoacetate
  • Dexamethasone