Control of encapsulation efficiency and initial burst in polymeric microparticle systems

Arch Pharm Res. 2004 Jan;27(1):1-12. doi: 10.1007/BF02980037.

Abstract

Initial burst is one of the major challenges in protein-encapsulated microparticle systems. Since protein release during the initial stage depends mostly on the diffusional escape of the protein, major approaches to prevent the initial burst have focused on efficient encapsulation of the protein within the microparticles. For this reason, control of encapsulation efficiency and the extent of initial burst are based on common formulation parameters. The present article provides a literature review of the formulation parameters that are known to influence the two properties in the emulsion-solvent evaporation/extraction method. Physical and chemical properties of encapsulating polymers, solvent systems, polymer-drug interactions, and properties of the continuous phase are some of the influential variables. Most parameters affect encapsulation efficiency and initial burst by modifying solidification rate of the dispersed phase. In order to prevent many unfavorable events such as pore formation, drug loss, and drug migration that occur while the dispersed phase is in the semi-solid state, it is important to understand and optimize these variables.

Publication types

  • Review

MeSH terms

  • Capsules*
  • Chemistry, Pharmaceutical*
  • Drug Compounding / methods*
  • Drug Delivery Systems / methods
  • Lactic Acid / chemistry
  • Lactic Acid / pharmacokinetics
  • Microspheres*
  • Particle Size
  • Polyglycolic Acid / chemistry
  • Polyglycolic Acid / pharmacokinetics
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polymers / chemistry
  • Polymers / pharmacokinetics
  • Proteins / administration & dosage
  • Proteins / chemistry

Substances

  • Capsules
  • Polymers
  • Proteins
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid