Over the last few eras, the plant-based drugs have been receiving extensive attention as these were used from the ancient times for the cure of diseases. However, the dose accuracy, dose efficacy and treatment has been based on the observed symptoms only. Instead of crude drug, current research mainly focused on medicinal active phytoconstituents. Several novel drug formulations like nano-capsules, polymer micelles, liposomes, nanogel, phytosomes, nano-emulsions, transferosomes, microsphere, ethosomes, injectable hydrogels, polymeric nanoparticles, dendrimers etc. has been developed using bioactive molecules and plant extracts. The tremendous applications of the novel formulations are enhancement in solubility, therapeutic efficacy, bioavailability, stability, tissue distribution, protection from physical and chemical damage and sustained and targeted delivery. Most of the material used are eco-friendly, biodegradable, plant-based material and bioadhesive, that provides extensive benefits as well as distinctive size to the nano-formulations. The present review is a concise representation of various herbal bioactive nano-formulations and pharmacological activity.