Co-amorphous Drug Delivery Systems: a Review of Physical Stability, In Vitro and In Vivo Performance

Abstract

Over the past few decades, co-amorphous solids have been used as a promising approach for delivering poorly water-soluble drugs. Co-amorphous solids, comprising pharmacologically relevant drug substances or excipients, improve physical stability, solubility, dissolution, and bioavailability compared with single amorphous ingredients. In this review, we have summarized recent advances in physical stability and in vitro and in vivo performances of co-amorphous solids. We have highlighted the role of molar ratio, molecular interaction, and mobility that affects the physical stability of co-amorphous solids. This review delves deep as to how co-amorphous solids affect the physicochemical properties in vitro and in vivo. We also described the challenges to the formulation of co-amorphous solids. A better understanding of the mechanisms of the physical stability, in vitro and in vivo performance of co-amorphous solids, and proper selection of the co-former is likely to expedite the development of robust co-amorphous-based pharmaceutical formulations and can address the challenges associated with the delivery of poorly soluble drugs.

Keywords: co-amorphous solids; in vitro dissolution; in vivo performance; physical stability; supersaturation.