The purpose of this study is to screen various preformulation studies in early stages of dosage form development, in order to reach a preliminary optimized group of lamotrigine (LTG) loaded polymeric nanoparticles, with certain characteristics that would permit brain targeting through parenteral administration. Various preformulation studies were carried out including UV absorbance studies, whose data were a guide to LTG solubility in various solvents, FTIR studies, where interaction between LTG and any other preparation components was studied, investigating the appropriate cryoprotectant, “cloud point titration technique” that indicated the adequate solvent ratio in both binary and tertiary systems, and finally transmission electron microscopy to screen all preparations. LTG was most soluble in acetone whereas polymers had higher solubility in dichloromethane. Pluronic^®F68 was the most effective cryoprotectant producing dried re-suspendable stable formulations. Transmission electron microscopy indicated the success of preformulation studies in achieving spherical LTG-loaded stable nano formulations whose particle size is less than 200nm, which can pass the blood brain barrier without being stuck through the reticulo-endothelial system.