The chemically diverse assemblage of phytomolecules is fast emerging as the panacea for most modern day diseases and the resurgent infections that pose a seemingly insurmountable healthcare challenge today. Development of these versatile agents as viable therapeutic options, however, remains constrained due to their inherent limitations, including low and erratic bioavailability owing to poor aqueous solubility and/or incomplete absorption, inadequate drug exposure to the target site for the requisite period, rapid and extensive metabolism, and, at times, potentially serious side effects. Nanophytomedicine is a rapidly emerging field of nanomedicine that deals with integrating the principles of nanotechnology for overcoming these handicaps and realizing the fullest potential of phytomolecules as effective medicinal agents. This chapter endeavours to provide a brief introduction to the various nanosystems that can be deployed in the design and development of phytoformulations. An updated review of the scientific and patent literature, as well as the regulatory and clinical status of the phytopharmaceuticals, based on these nanoformulations is presented here.