PDLLA microspheres containing steroids: spray-drying, o/w and w/o/w emulsifications as preparation methods

J Microencapsul. 1998 Mar-Apr;15(2):185-95. doi: 10.3109/02652049809006848.

Abstract

Hydrocortisone and its more soluble ester, hydrocortisone 21-acetate, have been incorporated into poly(D,L-lactic) acid (PDLLA) microspheres using single, double emulsion/solvent evaporation and by spray-drying techniques. This paper describes the characterization of the microparticles obtained (morphology, particle size distribution, drug content, yield of production, in vitro drug release behaviour) and a comparison of the results (drug loading, drug release, size of the microspheres) obtained from the different techniques used. These results demonstrate that by using a relatively more soluble ester of an insoluble steroid, hydrocortisone, the drug content within the microspheres can be increased, together with a high efficiency of loading, irrespective of the technique employed. In the case of hydrocortisone, spray-drying produces the highest loading and encapsulation efficiency compared to both single and double emulsion methods for microspheres of similar size (about 2-4 microns) and suitable for lung delivery, but with lower yields (about 55% versus about 33%).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Drug Compounding / methods*
  • Drug Delivery Systems
  • Emulsions / chemistry*
  • Hydrocortisone / metabolism
  • Lactic Acid / chemistry
  • Microscopy, Electron, Scanning
  • Microspheres*
  • Particle Size
  • Polyesters
  • Polymers / chemistry
  • Steroids / metabolism*
  • Temperature

Substances

  • Emulsions
  • Polyesters
  • Polymers
  • Steroids
  • Lactic Acid
  • poly(lactide)
  • Hydrocortisone