This paper deals with the effects of Paclitaxel drug on casein nanoparticles and its used in control drug therapy. Such systems have shown potential in releasing drugs controllably chemotherapy. In the present investigation casein nanoparticles were synthesized by emulsion cross linking method and characterized by various techniques such as Fourier transform–infrared spectrometry, Transmission electron microscopy, XRD. The average diameter of prepared native casein nanoparticles is 6nm to 100nm through W/O emulsification-cross linking method. The release behavior of casein nanoparticles was studied as a function of various factors such as chemical composition of nano-carrier, pH, temperature, biological fluids. The results revealed that the casein nanoparticles prove to be an excellent option for controlled and targeted delivery of Paclitaxel. Therefore, there is a strong incentive to develop a new strategy for the synthesis of casein nanoparticles and investigated their properties.