Process parameters of microsphere preparation based on propylene carbonate emulsion-precursors

J Microencapsul. 2021 Jan;38(1):1-10. doi: 10.1080/02652048.2020.1823501. Epub 2020 Nov 13.

Abstract

Aim: This study aimed for a detailed understanding of the impact of different process parameters involved during celecoxib-loaded microsphere preparation based on propylene carbonate emulsion-precursors.

Methods: Microspheres were prepared by a modified emulsification-solvent extraction method. Performed investigations included polymer solubility and viscosity, microsphere size, morphology and stability, propylene carbonate content as well as celecoxib solid state, content and release.

Results: Rough-walled round microspheres with sizes between 21 µm and 122 µm and an internal sponge-like structure filled with residual propylene carbonate (content between 1.9 ± 0.1% and 6.7 ± 0.5% w/w) were obtained. Encapsulation efficiencies varied between 28.3 ± 0.1% and 66.8 ± 1.0%. The release rates were affected by the polymer concentration, the emulsion phase ratio and the residual propylene carbonate content (t50% varied between 2.2 hours and 23.4 hours).

Conclusions: This study identified the most relevant process parameters for this new preparation method for the model drug celecoxib.

Keywords: Microencapsulation; PLGA; celecoxib; process parameters; propylene carbonate.

MeSH terms

  • Calorimetry, Differential Scanning
  • Celecoxib / administration & dosage*
  • Chemistry, Pharmaceutical / methods
  • Drug Carriers
  • Drug Compounding
  • Drug Liberation
  • Emulsions
  • Lactic Acid / chemistry
  • Microscopy, Electron, Scanning
  • Microspheres*
  • Particle Size
  • Polyglycolic Acid / chemistry
  • Polymers
  • Polypropylenes / chemistry*
  • Solubility
  • Solvents
  • Surface Properties
  • Viscosity

Substances

  • Drug Carriers
  • Emulsions
  • Polymers
  • Polypropylenes
  • Solvents
  • Polyglycolic Acid
  • Lactic Acid
  • polypropylene carbonate
  • Celecoxib