Phytocompounds isolated from plants are well appraised for their broad pharmacological propensities in several pathologies. One key benefit of phytoconstituents is their relatively low toxicity and adverse effects. Nonetheless, poor solubility, permeation, and poor specificity at the target site tend to hinder its therapeutic efficacy. Hence, novel technologies for drug delivery systems are being developed via the use of various nanoformulation strategies to overcome these challenges and give uniform medication focusing at the dynamic site in desired concentration and improved therapeutic efficacy. Such approaches comprise of novel drug delivery systems (NDDS). The utilisation of herbal formulations for NDDS is more beneficial and advantageous as opposed to others. The utilisation of ethosome, liposome, emulsion, phytosomes, microsphere, and strong lipid nanoparticles of herbal formulation has improved the remedial impacts of plant extricates. With the utilisation of all these, directed delivery of the formulation is accomplished, because of which the formulation exhibits impact on the site, and its’ bioavailability is, likewise, expanded. With these novel medication conveyance frameworks, the actives and concentrates, which are utilised as part of natural formulations, exhibit a sustained release, enhancement in stability, improved therapeutic efficacy, and protection from toxicity. The primary motivation behind creating alternative drug delivery technologies is to expand the effectiveness of drug conveyance and safety in the process and give more comfort to the patient. In this review, the importance of various phytocompounds in the delivery of drugs is highlighted as well as their importance in reducing the risk or diseases.