Medicinal plants are sources of crude traditional herbal medicines that are utilized to reduce the risk of, treat, or manage diseases in most indigenous communities. This is due to their potent antioxidant and anti-inflammatory effects. It is estimated that about 80% of the population in developing countries rely on herbal traditional medicines for healthcare. This signifies the need for traditional herbal medicines, which are polyherbal formulations prepared by traditional health practitioners. This review examines preparatory steps to extract bioactive phytoconstituents and post-extraction processes to increase the potency of the extracted bioactive phytoconstituents. Achieving this will allow for the reduced use of plant materials and promote the sustainable use of the limited resource of medicinal plants, especially in our South African context. Electronic ethnobotanical books and online databases were used to find studies that focus on phytoconstituent extraction and post-extraction processing to enhance the potency of the extracted bioactive phytoconstituents. Modification of the extracted bioactive phytoconstituents to synthesize daughter compounds facilitates an enhancement in their potency and bioavailability. Based on the data collected through this review, the importance of understanding the properties of the targeted phytoconstituents is essential in selecting the required extraction method. This determines the quality and yield of extracted bioactive phytoconstituents.
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