Bile acid-inspired oral small molecules drug delivery

Abstract Most of the new drug molecules including small molecules and dosage forms developed by researchers or marketed by pharmaceutical companies. From various dosage forms, orally suitable forms of the drug remain the top choice due to the high patient acceptance. The majority of the small molecules, however, have evolved as needle-based dosage forms over the last few decades due to the pH of the stomach, ubiquitous presence of intestinal degrading enzymes, protective layer of mucus, low permeability of small molecules, and poor bioavailability. Multiple attempts have been made to overcome these physiological and biological barriers to develop oral dosage forms of small molecules and thereby enhance their pharmacokinetics and pharmacodynamics profiles. Among them, bile acids have gained considerable attention in the development of oral dosage forms of small molecular drugs due to their excellent properties. The main advantages of using bile acids as excipients are the ability to maintain structural integrity at different physiological pHs, interact with target cells through apical sodium bile acid transporters, use as absorption enhancers, activate cellular signal transduction pathways, phosphorylates of target proteins. Also, bile acids increase the water solubility and transcellular permeability of small drug molecules and thereby increase the effectiveness of oral small molecular drug treatments. In this chapter, we discuss the possibility of using bile acids to develop oral dosage forms of small molecules.