India has a long hereditary usage of numerous phytochemicals, and their formulations in the officially recognized alternative system of medicine viz. Ayurveda, Homeopathy, Yoga, Siddha, Unani, and Naturopathy. The ancient system of traditional Indian medicine uses medicinal plants to extract biologically active phytochemicals and formulate in various dosage forms. Biologically active phytochemicals have enormous therapeutic potential which can be further potentiated through various beneficial novel drug delivery systems (NDDS). In the recent past, development of NDDS based strategies for phytochemicals has gained considerable attention as the NDDS based formulations and dosage forms compared to conventional dosage form are more advantageous. The use of different form like nanoparticles, liposome, nanoemulsion, ethosome, microsphere, phytosomes, solid lipid nanoparticles have contributed significantly to the enhancement of therapeutic potential of plant-derived extracts and their constituents. The introduction of all these, the actives and extracts in the formulations have demonstrated remarkable improvement in the stability, solubility, sustained release profile, targeted delivery, improved therapeutic efficacy, and reduced toxicity. The rationale behind the development of NDDS based drug delivery strategies is to enhance drug delivery and an improved safety profile in the drug delivery process along with patient compliance. The NDDS will not only increase the market of phytochemicals but will also play a major role in providing better and effective therapy to mankind. The current chapter highlights the recent developments of novel drug delivery systems in phytochemicals and their classes, methods of preparation, administration, biological/pharmacological activity, safety, and applicability.