Many biologically active compounds are unsuitable for development as drugs due to their poor bioavailability.
For hydrophilic compounds, modifications to increase lipophilicity can increase passive diffusion or increase uptake into
the lymphatic system. Alternatively, improved bioavailability of hydrophilic drug candidates may be achieved by formulation
with absorption promoters such as surfactants, penetration enhancers, or ion pairing agents. This approach to enhancing
bioavailability also has the potential to widen the range of compound categories that can be used as chemical
probes to study biological systems in cells and in vivo where membrane permeability would otherwise be a significant
limitation. Lipidic amino acids, which combine the structural properties of lipids with those of α-amino acids, represent a
relatively unexplored class of agents that can improve drug adsorption. This review discusses the potential of absorption
promoters possessing lipoamino acids for improving drug bioavailability.
Keywords: Absorption promoter, dendrimers, drug bioavailability, drug delivery, ion pairing agents, lipoamino acids, penetration enhancers, hydrophilic compounds, lymphatic system, hydrophilic drug, chemical probes, biological systems in cells, Lipidic amino acids
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