Chitosan, a natural biodegradable polymer obtained from deacetylation of chitin, has been used as an approbative macromolecule for the development of various novel drug delivery systems. It is one of the most favorable biodegradable carriers for nanoparticulate drug delivery due to its intrinsic properties, such as biocompatibility, biodegradability, non-toxicity, availability of free reactive amino groups, and ease of chemical modification into different active derivatives. Furthermore, interesting physical properties (film-forming, gelling and thickening) make it a suitable candidate for formulations, such as films, microcapsules, beads, nanoparticles, nanofibres, nanogel and so on. Researchers have reported that chitosan nanoparticles act as a promising vehicle for herbal actives as they provide a superior alternative to traditional carriers and improve pharmaceutical efficiency. As no review of chitosan nanoparticles encapsulating herbal extracts and bioactives has been published till date, a maiden effort has been made to collate and review the use of chitosan nanoparticles for the entrapment of phytoconstituents to yield stable, efficient and safe drug delivery systems. Additionally, the paper presents a comprehensive account of the state-of the-art in fabricating herbal chitosan nanoparticles and their current pharmacological status. A list of patents on chitosan nanoparticles of herbal actives has also been included. This review is intended to serve as a didactic discourse for the formulation scientists endeavoring to develop advanced delivery systems for herbal actives.