Injectable hydrogel particles for amorphous solid formulation of biologics

Abstract

The fast pace of breakthroughs in cancer immunotherapy, combined with the new paradigm of moving toward high-concentration dosages and combinatorial treatments, is generating new challenges in the formulation of biologics. To address these challenges, we describe a method of formulation that enables high-concentration injectable and stable formulation of biologics as amorphous solids in aqueous suspension. This technology combines the benefits of liquid formulation with the stability of solid formulation and eliminates the need for drying and reconstitution. This widely applicable formulation integrates the amorphous solid forms of antibodies with the injectability, lubricity, and tunability of soft alginate hydrogel particles using a minimal process. The platform was evaluated for anti-PD-1 antibody pembrolizumab and human immunoglobulin G at concentrations up to 300 mg/mL with confirmed quality after release. The soft nature of the hydrogel matrix allowed packing the particles to high volume fractions.