Overcoming Food Effects, Variability & Solubility for a Non-Opioid Analgesic with LBF
Summary: Poorly soluble oral small molecules often face compounded development risks, including food effects, high dose requirements, variability in exposure, and the need for rapid onset. In this case study, 91Ï㽶ÊÓƵ partnered with a developer of a non-opioid analgesic to address these challenges using a stepwise lipid-based formulation strategy. Starting with a simple lipid-based formulation to maximize API loading, 91Ï㽶ÊÓƵ systematically optimized dispersibility and applied in vitro permeability tools to establish in vivo relevance. The resulting optimized formulation minimized food effects, reduced inter-subject variability, enabled high-dose delivery, and achieved a rapid time to peak concentration. Selected for Phase 1 clinical evaluation, this formulation demonstrates how targeted lipid-based approaches can de-risk early development and accelerate progress toward the clinic.