Herbal drug discovery based on biomarkers is an emerging area in complementary and alternative medicine that has tremendous potential in healthcare. Conventional medications have limited efficacy and high toxicity, whereas herbal drugs are said to provide wide structural diversity that is not usually seen with conventional/synthetic drug molecules. Recognition of various herbal constituents, such as terpenoids, fatty acids, flavonoids and steroids, are well explored in the management and treatment of various disorders in this volume. These agents target various biomarkers such as nitric oxide (NO), cytokines, chemokines, adhesion molecules, NF- kβ, lipoxygenase (LOX), and arachidonic acid. discusses phytoconstituent-based nanotherapeutics with applications for some specific health issues, such as arthritis, leishmanicidal, cardiovascular diseases, cancer, ocular disorders, etc.