(339) Lipophilization as a design strategy to tune the release of Tofacitinib from lipid nanoparticles

Introduction: Tofacitinib (Tofa) is an oral JAK 3 inhibitor, prescribed for the treatment of inflammatory arthritides and organ transplantation. Despite having remarkable potential, Tofa tends to have a short plasma half-life along with the tendency to cause dose-dependent toxicity. While the advent of nanoparticles has mitigated some of these challenges, premature release of drug from these systems compromises its therapeutic effect. We have developed a lipophilic Tofa prodrug that facilitates slow, sustained release rates from lipid nanoparticles with the ability to fine tune its therapeutic efficacy.