Background: Bioavailability is the segment of dose that is bioavailable for its therapeutic
effect on the systemic circulation without any change in its characteristics, after administration by either
route. It is one of the fundamental pharmacokinetic properties of drugs. It is important because, it
defines the amount of drug to be administered for its intended therapeutic effect. If drug is more
bioavailable, less amount of it is required to obtain therapeutic effect. However, it is also worth mentioning
that most of the newly discovered therapeutic agents have poor solubility and thus low
Objectives: In this article, various methods including conventional and advanced, have been reviewed
that could be potentially used for the enhancement of bioavailability. Moreover, the benefits and
drawbacks of all the strategies are deliberated to comprehend the probable use of each method supported
by latest references.
Methods: Various strategies have been developed to enhance the solubility and thus bioavailability of
numerous drugs, some of which are discussed here. All these strategies involve different approaches to
improve the bioavailability including physical adaptation, chemical modification and controlling particle
size of the engineered particle.
Results: These strategies, particularly the nano-particulate systems, not only improve the bioavailability
of drugs but at the same time diminish the possible toxicities of the incorporated drugs.
Conclusion: It can be concluded that this would be a new source of information for the readers.