The herbal-based drugs have been getting wide attention over the last few decades. The herbal drugs have been used from the ancient times, but the dose accuracy, efficacy, and treatment was just based on symptomatic observatory. Modern research is focused on pure bioactive compound instead of crude. The researchers are trying to apply the current advanced nanotechnology-based knowledge on the herbal medicines to improve efficacy and reduces the unwanted pharmacological actions' adverse effects of the therapeutic molecules. The many novel drug delivery systems available used for the herbal bioactive molecules include polymeric micelle, injectable hydrogel, nano gel, nano emulsions, microsphere, polymeric nanoparticles, nano capsules, liposomes, phytosomes, transferosomes, dendrimer, and ethosomes. This chapter highlights the existing research and development of current standing of the of various novel formulations especially for the herbal bioactive molecules and summarizes their active ingredients, commercial formulations, route of drug administration, and pharmacological activity.