Because of the increasing demand for natural products, the development of nanoformulations containing natural active ingredients requires in‐depth knowledge of the substances used, methods of obtaining, and stability profiles to ensure product quality, efficacy, and safety. Considering this, the bibliography of the last five years presented in databases (PubMed and Science Direct) was discussed in this work, discussing the study with medicinal plants to obtain active metabolites with therapeutic properties, as well as the different nano‐systems responsible for carrying these molecules. Due to the wealth of biodiversity found in the world, many species are submitted to the extraction process for several purposes. However, identifying, classifying, and quantifying the constituents of herbal matrices are crucial steps to verify their therapeutic potential. In addition, knowing the techniques of production and elaboration of nanotechnology products allows the optimization of the incorporation of herbal extracts as an innovation target. For studies to be successful, it is necessary to exhaust experimental results that guarantee the efficacy, safety, and quality of natural nanosystems, with the objective of obtaining reliable answers in nanotechnology therapy.