Herbal extracts and isolated bioactives from plants have proven their therapeutic activities, as evidenced by preclinical and clinical research. However, there seems some disconnect in their clinical utility as marked by a lack of proper delivery mechanism at desired sites of action. This glitch nowadays is a task for global research activity and being addressed in novel drug delivery systems. Steady progress is observed in integrating novel techniques of drug delivery with successful incorporation of phytochemicals marked by scores of advantages. Limitations of conventional drug delivery systems have overcome to a considerable extent by innovative drug delivery methods which show improvement in targeted drug delivery, drug distribution, protection of active substance, prolonged action, and stability. The perspective of this review thus focuses on the progress in novel drug delivery systems with a spotlight on nanocarriers for active herbal agents, their preparation methods with types, examples of active ingredients incorporated, and biomedical applications.