Herbal drugs have been used around the world since ancient times. The effectiveness of herbal drugs depends on their active constituents such as phenolic compounds, flavonoids, terpenoids, and tannins. These compounds were proven to show many therapeutic activities such as anti-inflammatory, antimicrobial and anticancer. However, they have many drawbacks restricting their applications and therapeutic outcomes such as low absorption due to their inability to cross the lipid membrane of the cell. Therefore, they have low bioavailability and efficacy. The nanotechnology is a cutting-edge science that might give a new hope to revitalize the use of herbal drugs. Nano-carrier systems are reported to potentiate the action of herbal drugs, due to their ability to improve their bioavailability. Moreover, herbal nano-medicine could be designed with a surface decoration to be targeted to the effective sites, and thus reducing the therapeutic dose, minimizing side effects with an improvement of their therapeutic outcome.