Ayurveda involves a variety of scientific bases of harmony as well as wellbeing. The origin of Ayurveda can be traced to the ancient knowledge in Rigveda and many more. Since ancient times, Ayurveda is a traditionalistic, conservative healthcare system of Indian medicine. Many ayurvedic medicines have been exploiting for the treatment and management of various ailments in human beings. Several drugs have been developed from Ayurveda and known as 'tradition to trend'. The potential of ayurvedic drugs needs to be explored further with scientific validation approaches for better therapeutic leads. This chapter proposed the various aspects of Ayurveda and drug discovery approaches for its development and therapeutic approaches.