Besides being a rich for vitamins and fibre, the skin and seeds of grapes are highly rich in Polyphenols specifically proanthocyanidins, which can be used as a functional ingredient to address various health issues by boosting the natural bio-processes of the body. Antioxidant power of proanthocyanidins is 20 times greater than vitamin E and 50 times greater than vitamin C. Proanthocyanidins in Grape seeds have been shown to exhibit strong antioxidant, antimutagenic, anti-inflammatory, anticarcinogenic and antiviral activity. Through different and various studies, it was proved that the proanthocyanidin rich grape seed extract provides benefits against many diseases i.e. inflammation, cardiovascular disease, hypertension, diabetes, cancer, peptic ulcer, microbial infections, etc. Therefore, beside from using it as a nutraceutical or cosmeceutical, as a result they may have a potential to substitute or complement in currently used drugs in the treatment of diseases by developing it into other successful pharmaceutical formulations for better future prospective. This current review, disscussed about the grapeseed extract uses, its formulation into tablet dosage form and evaluation parameters.