Polymer lipid hybrid (PLH) formulations: A synergistic approach to oral delivery of challenging therapeutics. A synergistic approach to oral delivery of challenging therapeutics

Book chapter, 2020

In recent decades, lipid-based formulations and polymeric systems have emerged concurrently as the predominant approaches for overcoming low gastrointestinal stability/solubility and rate-limiting dissolution drawbacks that are associated with a wide range of therapeutics, including lipophilic small molecules and sensitive macromolecules. While these conventional approaches have demonstrated the ability to overcome drug absorption barriers and subsequently improve oral biopharmaceutical performance, a number of fundamental limitations have restricted the translation of promising preclinical and clinical findings into commercial success. Furthermore, the increasing complexity of novel therapeutics has amplified the demand for innovative and intelligent carrier systems that effectively transport drug molecules to the primary site of absorption. Consequently, recent focus has been attributed to designing and engineering polymer-lipid hybrid (PLH) formulations that combine the solubilization capacity of lipids with the stabilizing matrix of polymeric systems. This presents a synergistic approach to oral drug delivery with proven potential for overcoming limitations associated with the precursor systems. This chapter focuses specifically on the development of PLH systems, with emphasis placed on the relationship between nanostructure/surface chemistry and the physicochemical and biopharmaceutical performance of the hybrid formulation.