The present invention discloses bio-efficacy and bio-availability enhancing composition comprising, an effective amount of stevia compound selected from raw powder or extract, or fraction(s) or compound(s) or combinations thereof derived from the whole plant or plant parts of genus Stevia, preferably leaves of Stevia rebaudiana for enhancing the bio-availability and bio-efficacy of therapeutic agents, cosmetic agents, supplements, food ingredients and beverages selected from but not limited to pharmaceutical drugs, nutrients (micro and macro nutrients), vitamins, minerals, Proteins, amino acids, enzymes, nutraceuticals, herbal drugs/products and antioxidants.