The current study aims to improve drug release properties of orotic acid loaded with chitosan inclusion complex (OA/CS). The OA/CS inclusion complex was synthesized using the freeze-drying technique. The characterization of inclusion OA/CS was carried out using fourier transform infrared spectroscopy (FTIR), X-ray diffractometry (XRD), differential scanning calorimetry (DSC), zeta sizer, and transmission electron microscopy (TEM). Furthermore, the size of OA/CS ranged between 58 nm and 200 nm, and the zeta potential was 30 mV. Thus, this study indicates that OA/CS has a promising future to develop a carrier for drug delivery systems further.