Developing High Drug Load Re-Dispersible Amorphous Formulations

27 September 2022 15:30 - 16:00

  • Formation of nanoparticles during ASD dissolution enhances oral absorption of poorly soluble drugs. The goal is to obtain amorphous nanoparticle formulation that can achieve same performance without a large amount of excipients compared to ASD.
  • Nanoparticles fabricated by solvent/anti-solvent precipitation can be stabilized by removal of organic solvent and drying. Understanding of API and formulation properties aids in design to obtain the solid form that redisperses into primary nanoparticles.
Amorphous solid dispersions can generate nanoparticles < 500nm during dissolution, which was reported to enhance oral absorption of poorly soluble drugs. However, the controlled dissolution and formation of nanoparticles require a large amount of excipients, presenting challenges for some drug product formulations. Directly engineered nanoparticles made by solvent/anti-solvent precipitation can be stabilized and dried into a solid form. This approach harnesses the effect of the drug-rich nanoparticles on oral absorption, while reducing use of the amount of excipients to obtain a high drug loading. In vivo study on animal model demonstrates this amorphous nanoparticle formulation can achieve comparable performance to commercial ASD product.

Mengqi Yu, Ph. D., Sr. Scientist I, Formulation Sciences, AbbVie