Ternary solid dispersions of lacidipine: Enhancing dissolution and supersaturation maintenance through strategic formulation optimization

Int J Pharm. 2024 Apr 10:654:123989. doi: 10.1016/j.ijpharm.2024.123989. Epub 2024 Mar 11.

Abstract

The study aimed to address the challenges related to insufficient dissolution and maintenance of supersaturation in binary solid dispersions. Lacidipine, categorized as a BCS class II drug, was employed as the model drug. A systematic screening of excipients was conducted to determine the most effective carriers for the formulations of the ternary solid dispersions, utilizing the solvent transfer method and equilibrium solubility measurements. Both binary and ternary solid dispersions were prepared via spray drying, and comprehensive physicochemical characterization confirmed the successful preparation of amorphous solid dispersions. In vitro dissolution tests, the ternary solid dispersion exhibited marked superiority over the binary solid dispersion in dissolution and maintenance of supersaturation. Furthermore, an exploration into the factors influencing the stability of ternary solid dispersions revealed their robust resistance under light-protected, room-temperature, and desiccated conditions. The formation of intermolecular hydrogen bonding within the molecules of the ternary solid dispersions significantly enhanced drug solubility and system stability. Strategic formulation optimization, coupled with judicious selection of suitable carrier types and ratios, may serve as a promising approach for designing supersaturated drug delivery systems.

Keywords: Lacidipine; Solid dispersion; Solubilization; Spray drying; Storage stability.

MeSH terms

  • Dihydropyridines*
  • Drug Delivery Systems
  • Excipients
  • Pharmaceutical Preparations
  • Solubility

Substances

  • lacidipine
  • Dihydropyridines
  • Pharmaceutical Preparations
  • Excipients