Herbal medicines are defined by WHO as medicines inclusive of “herbs, herbal materials, herbal preparations and finished herbal products, that contain as active ingredients parts of plants, or other plant materials, or combinations” (1). Herbal medicines have been used in many developing countries as a primary source of medicinal treatment (1). As 80 % of the population in developing countries is still dependent on natural medicines, researchers are investigating the medicinal potential of natural plants extracts using modern scientific approaches (2). Herbal medicines often tend to have broad complementary actions on physiological systems or tend to have wide synergistic actions on physical systems at the same time. These are usually not specific and not directed, some are even shown to be toxic. Thus, researchers have moved from using the whole plant, to using plant extracts with a narrower range of phytochemicals often with an increased biological effect in assays due to concentration of active agents. Unfortunately, plant extracts often suffer from low solubility, this results in low absorption, which reduces the bioavailability and efficacy that was meant to be enhanced by fractionation. Thus, to overcome these challenges novel drug delivery systems like polymer drug conjugation have been investigated to improve the solubility, stability and bioavailability while by reducing toxicity of the active constituents/plant extracts. Thus, in this work we will show the benefit of using polymer drug-conjugation to eliminate some of the challenges associated with active constituents of plant extracts. This work will discuss the synthesis and challenges associated with the synthesis of polymer-drug conjugates, their characterization and preliminary biological work conducted. 1.World Health Organization (WHO). National Policy on Traditional Medicine and Regulation of Herbal Medicines. Geneva: 2005. 2.Bonifàcio, B.V.; da Silva, P.B.; dos Santos Ramos, M.A.; Negri, K.M.