HPLC–MS/MS-based analysis of everolimus in rabbit aqueous humor: pharmacokinetics of in situ gel eye drops of suspension

Aim: Everolimus is an inhibitor of mTOR which is derived from rapamycin. Its high corneal permeability and bioavailability makes it an effective treatment for ocular disorders. To study the pharmacokinetics of in situ gel eye drops of everolimus suspension after ocular administration in rabbit aqueous humor, we developed a rapid and reliable HPLC–MS/MS method. Keywords: aqueous humor, everolimus, HPLC–MS/MS, pharmacokinetics Everolimus is a 40-O-[2-hydroxyethyl] derivative of sirolimus and an inhibitor of mTOR kinase (Figure 1). It is an active immunosuppressor and antiproliferative macrolide [1]. It has rapid absorption kinetics and its bioavailability is higher than sirolimus (everolimus 16–20% vs sirolimus 10–14%) [2,3]....