In India, Ayurveda has made a major contribution in drug discovery process with new means of identification of active compounds. Recent advancement in bioavailability enhancement of drugs by compounds of herbal origin has developed a revolutionary shift in the field of therapeutics. Herbal bio-enhancers have been shown to enhance bioavailability and bio-efficacy of different classes of drugs, such as antibiotics, anti-tuberculosis, antiviral, antifungal, and anti-cancerous drugs at low doses. They have also improved oral absorption of nutraceuticals like vitamins, minerals, amino acids, and certain herbal compounds. These molecules enhance the systemic availability of drugs through various possible mechanisms but this paper emphasizes on the two major mechanisms such as inhibition of drug metabolizing cytochrome enzymes and P-glycoprotein efflux pump which have not been described in detail earlier as reviewed through literature. Further this review clearly indicates that scientific researchers and pharmaceutical industries have to give emphasis on experimental studies to find out novel active constituents from such a vast array of unexploited plants having a role as a bioavailability and bio-efficacy enhancer.
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