Ocular biopharmaceutics: impact of modeling and simulation on topical ophthalmic formulation development

•Historical and emerging computational tools to support ophthalmic drug discovery.•Preclinical ocular pharmacokinetics burden animal use, while clinically impractical.•Therapeutic bioequivalence studies between ophthalmic products are challenging.•Topical and injectable ophthalmic products require full disposition understanding. The estimation of ocular pharmacokinetics (PK) in various eye tissues is limited because of sampling challenges. Computational modeling and simulation (M&S) tools underpinning the elucidation of drug access routes and prediction of ocular exposure are essential for the mechanistic assessment of biopharmaceutics in the eye. Therefore, theoretical and experimental evaluation of ocular absorption and transit models is necessary. Biopharmaceutical parameter sensitivity analysis based on permeability and drug dose illustrates utility in ocular drug delivery assessment, which could have innovative and cost-saving impacts on ophthalmic product development and therapeutic bioequivalence (BE) evaluations.