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This research explores the feasibility of the electrohydrodynamic processing using single and co-axial set-up as a single step processing tool for preparation of advanced drug delivery systems. A number of synthetic biodegradable and non-biodegradable polymers were used in order to prepare formulations incorporating drugs of different physicochemical characteristics. Based on the focus and the desired applications, the polymeric carrier and solvent system as well as the model drug of interest were selected to develop the drug delivery systems. Firstly, core-shell microparticles were prepared and optimized using co-axial electrohdrodynamic processing with precise control over the averaged particle size and size distribution. This was followed by integration of model drugs with different water-solubility. In this study, the release characteristics of the developed particles were investigated with single and simultaneous encapsulation of the drugs. Successful preparation of fixed dose combination formulation with high processing yield and encapsulation efficiency was reported. Secondly, single and co-axial electrohydrodynamic processing was utilized for preparation of smart drug delivery system for targeted release of prednisolone. Colon targeted drug delivery systems were developed using a pH-responsive polymer. Varying polymer drug ratio was applied to further enhance the release profiles and obtain an efficient delivery system whereby local delivery of prednisolone is made possible. Finally, microspheres were developed for co-encapsulation of anti-diabetic drugs with different water-solubility. The successfully developed sustained release formulations have the potential to overcome the existing limitations of conventional formulations by enhancing patient compliance and efficacy of the treatment of any chronic conditions.