The use of albumin solid dispersion to enhance the solubility of unionizable drugs

Pharm Dev Technol. 2018 Sep;23(7):732-738. doi: 10.1080/10837450.2017.1364267. Epub 2017 Aug 24.

Abstract

In this study, solid dispersions of prednisolone (PRD) and bovine serum albumin (BSA) were prepared by spray drying and freeze drying methods using a PRD:BSA solution [20:1 molar ratio (MR)]. PRD-BSA dispersed mixtures were characterized by scanning electron microscopy (SEM), and powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC). PRD-BSA physical and dispersed mixtures showed significantly higher solubility in water than that of unprocessed drug. Enhancement factor of six was obtained in both physical mixture and solid dispersion solubility studies. In-vitro dissolution and release studies under physiological conditions showed an immediate release of PRD from the solid dispersions, with almost 90% of the drug dissolved in the first 10 min. PRD was immediately released from BSA binding complex. This study demonstrates the potential for the use of BSA to enhance the solubility and dissolution rate, hence bioavailability, of the unionizable drugs.

Keywords: Bovine serum albumin; dissolution rate; prednisolone; solid dispersion; solubility enhancer.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / chemistry*
  • Calorimetry, Differential Scanning
  • Cattle
  • Desiccation
  • Drug Carriers / chemistry*
  • Drug Compounding
  • Drug Liberation
  • Freeze Drying
  • Prednisolone / administration & dosage
  • Prednisolone / chemistry*
  • Serum Albumin, Bovine / chemistry*
  • Solubility
  • X-Ray Diffraction

Substances

  • Anti-Inflammatory Agents
  • Drug Carriers
  • Serum Albumin, Bovine
  • Prednisolone