RESUMO
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 bioavailability. 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.