Cutting-Edge Strategies To Enhance The Bioavailability Of Naringenin

Abstract

One of the significant concerns in drug development is the low water solubility of many drugs or active pharmaceutical ingredients (APIs), which hinders their absorption and bioavailability. Co-crystallization and nanotechnology have emerged as a promising strategy to resolve these issues by modifying the physicochemical properties of APIs without altering their pharmacological action. Pharmaceutical co-crystals are formed of an API and one or more co-formers, bind together by non-covalent interactions. This technique can be integrated with another solubility-enhancing strategies called nanotechnology to address the challenges of poor solubility. These techniques can increase solubility, dissolution, stability, and bioavailability, eventually improving drug delivery and efficacy. Various co-crystal formation methods and co-formers, including nicotinamide, succinic acid and amino acids, have shown considerable success in enhancing the therapeutic performance of APIs. Naringenin, a naturally occurring flavonoid, exhibits significant biological activities, including antioxidant, anti-cancer and anti-inflammatory effects. However, its therapeutic potential is often limited due to poor aqueous solubility and permeability, resulting in low bioavailability (approximately 15% in humans). Moreover, the integration of co-crystal technology with nanosuspensions can create a synergistic effect, where the enhanced dissolution and stability of co-crystals are further improved by the reduced particle size and increased surface area provided by nanosuspensions. This combined approach has the potential to significantly increase the bioavailability and therapeutic effectiveness of challenging APIs like naringenin. This comprehensive review attempt explores the advantages of co-crystals integrating with nanotechnology in improving the solubility and bioavailability of poorly water-soluble drugs and aim to demonstrate their capability to transform pharmaceutical formulations and optimize drug delivery systems.