The present research work was designed to increase the bioavailability and cardioprotective potential of three important medicinal plants (Curcuma longa, Ginkgo biloba and Coriandrum sativum). This project was divided into different phases. In first phase of study, nanosuspensions of selected medicinal plants were prepared by choosing an appropriate stabilizer. Formulation conditions of nanosuspensions were optimized with response surface methodology. In second phase of study, optimized nanosuspensions of plants extract were characterized by atomic force microscopy (AFM), scanning electron microscopy (SEM) and Fourier-transform infrared spectroscopy (FTIR). In third phase of study, in-vitro drug release and pharmacokinetics of coarse and optimized nanosuspensions of plants extract were evaluated. In fourth phase of study, comparative bioactivities (cardioprotective potential, thrombolytic, antimicrobial and antioxidant activities) of coarse and nanosuspensions of plants were determined. Results of stabilizer screening selected sodium lauryl sulphate (stabilizer) for the preparation of nanosuspensions of selected plants. Optimized nanosuspensions of C. longa, G. biloba and C. sativum were prepared with mean particle size of 85.41 nm, 139.5 nm and 72.08 nm respectively. AFM also confirmed that particle sizes of all optimized nanosuspensions were in nanosize-range. FTIR analysis showed interaction between C. longa and stabilizer and no-interaction between other studied plants and stabilizer. In-vitro drug release and pharmacokinetics study revealed greater dissolution and bioavailability of optimized nanosuspensions of plants in comparison to their coarse suspensions/extracts. Nanosuspensions of plants showed better cardioprotective potential with reduced dose as compared to their coarse suspensions. In preventive mode of treatment, four-fold greater doses of coarse suspension of C. longa, G. biloba and double dose of coarse suspension of C. sativum were required to normalize the salbutamol elevated levels of cardiac enzymes and lipids in comparison to their nanosuspensions. Antimicrobial, thrombolytic and antioxidant activities of plants were also enhanced in nanosuspension preparation. Moreover, optimized nanosuspensions were found fairly stable for a period of three months and cytotoxicity study revealed no harmful effects of formulated nanosuspensions.