Diverse approaches for the enhancement of oral drug bioavailability

Abstract In conscious and co‐operating patients, oral drug delivery remains the preferable route of drug administration. However, not all drugs possess the desirable physicochemical and pharmacokinetic properties which favor oral administration mainly due to poor bioavailability. This has in some cases led to the choice of other routes of administration, which may compromise the convenience and increase the risk of non‐compliance. Poor bioavailability has necessitated the administration of higher than normally required oral doses which often leads to economic wastages, risk of toxicity, erratic and unpredictable responses. The challenge over the years has been to design techniques that will allow oral administration of most drugs, irrespective of their properties, to achieve a therapeutic systemic availability. This will be a worthy achievement since over 90% of therapeutic compounds are known to possess oral bioavailability limitations. In this review, an attempt has been made to explore various approaches that have been used in recent years to improve oral drug bioavailability, including physical and chemical means. This review strives to provide a comprehensive overview of advances made over the past 10 years (2000–2010) in the improvement of the oral bioavailability of drugs. Briefly, the design of prodrugs to bypass metabolism or to enhance solubility as well as modification of formulation techniques such as the use of additives, permeation enhancers, solubilizers, emulsifiers and non‐aqueous vehicles have been discussed. Arising approaches, such as formulation modification techniques; novel drug delivery systems, which exploit the gastrointestinal regionality of drugs, and include the pharmaceutical application of nanotechnology as an emerging area in drug delivery; inhibition of efflux pumps; and inhibition of presystemic metabolism have been more extensively addressed. This critical review sought to assess each method aimed at enhancing the oral bioavailability of drugs in terms of the purpose, scientific basis, limitations, commercial application, as well as the areas in which current research efforts are being focused and should be focused in the future. Copyright © 2011 John Wiley & Sons, Ltd.