A method using biodegradable polylactides/polyethylene glycol for drug release with reduced initial burst

Int J Pharm. 1999 May 10;182(1):93-100. doi: 10.1016/s0378-5173(99)00060-5.

Abstract

Post-coating of biodegradable polylactides (PLA)/polyethylene glycol (PEG) microspheres with a gelatin film produced by dipping the microspheres into a gelatin solution to reduce the initial drug release burst was investigated. Biodegradable block PLA/PEG microspheres, prepared by w/o emulsion/solvent evaporation, showed that the hydrophilic segment PEG protruded to the sphere surface. However, these microspheres also showed a large burst release in the initial period. Post-coating of the PLA/PEG microspheres with a gelatin film by dipping the microspheres into a dilute gelatin solution effectively inhibited the initial burst release rate in the drug release tests. Post-coating of gelatin reduced 98% of the burst release. With thicker coatings, there were slower releasing rates, and the release rate can be simply related to the coating thickness.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Arrhythmia Agents / administration & dosage
  • Anti-Arrhythmia Agents / chemistry
  • Biocompatible Materials / chemical synthesis
  • Biocompatible Materials / chemistry*
  • Biodegradation, Environmental
  • Coated Materials, Biocompatible / chemical synthesis
  • Coated Materials, Biocompatible / chemistry*
  • Delayed-Action Preparations
  • Drug Carriers
  • Gelatin / chemistry
  • Lactates / chemical synthesis
  • Lactates / chemistry*
  • Lidocaine / administration & dosage
  • Lidocaine / chemistry
  • Microspheres
  • Polyethylene Glycols / chemical synthesis
  • Polyethylene Glycols / chemistry*
  • Propranolol / administration & dosage
  • Propranolol / chemistry

Substances

  • Anti-Arrhythmia Agents
  • Biocompatible Materials
  • Coated Materials, Biocompatible
  • Delayed-Action Preparations
  • Drug Carriers
  • Lactates
  • poly(lactic acid-ethylene glycol)
  • Polyethylene Glycols
  • Gelatin
  • Lidocaine
  • Propranolol