Background: Bioavailability, one of the prime pharmacokinetic properties of a drug, is defined as the
fraction of an administered dose of unchanged drug that reaches the systemic circulation and is used to describe
the systemic availability of a drug. Bioavailability assessment is imperative in order to demonstrate whether the
drug attains the desirable systemic exposure for effective therapy. In recent years, bioavailability has become
the subject of importance in drug discovery and development studies.
Methods: A systematic literature review in the field of bioavailability and the approaches towards its enhancement
have been comprehensively done, purely focusing upon recent papers. The data mining was performed
using databases like PubMed, Science Direct and general Google searches and the collected data was exhaustively
studied and summarized in a generalized manner.
Results: The main prospect of this review was to generate a comprehensive one-stop summary of the numerous
available approaches and their pharmaceutical applications in improving the stability concerns, physicochemical
and mechanical properties of the poorly water-soluble drugs which directly or indirectly augment their bioavailability.
Conclusion: The use of novel methods, including but not limited to, nano-based formulations, bio-enhancers,
solid dispersions, lipid-and polymer-based formulations which provide a wide range of applications not only
increases the solubility and permeability of the poorly bioavailable drugs but also improves their stability, and
targeting efficacy. Although, these methods have drastically changed the pharmaceutical industry demand for the
newer potential methods with better outcomes in the field of pharmaceutical science to formulate various dosage
forms with adequate systemic availability and improved patient compliance, further research is required.