In general, the importance of using nanoparticles as drug carriers were due to high carrier capacity, high stability, probability of incorporation of both lipophilic and lipophobic drugs, and probability of various routes of administration. Therefore, this study aims to synthesize a spiroquinazoline derivative 1'-methyl-1H'-spiro [cyclopentane-1, 2'-quinazolin]-4'(3'H)-one (compound 3) and incorporate it into chitosan nanoparticles to form compound 3-CSNPs nanocomposites. Compound 3-CSNPs nanocomposites were prepared by ionic gelation. In the same manner, the Placket Burman design was used to prepare twenty-seven formulations with three independent variables; (chitosan with various amounts (50,100, and 150 mg), tripolyphosphate with multiple amounts (50,100, and 150 mg), compound 3 with various amounts (25, 50, and 100 mg), to study the effect on loading efficiency. Minitab 18.1 statistical software was used to study the impact of independent variables to get the highest loading efficiency. A response surface model was used to analyze data by means of graphical analysis, surface plots, contour plots, and main effects plots charting. Furthermore, the current study compared experimentally obtained results and predicted values using bias values. The bias values indicate that the generated models were valid and efficient, with no statistically significant difference between the predicted and experimental values. In order to characterize the compound 3-CSNPs nanocomposites; Fourier transform infrared, X-ray diffraction, scanning electron microscopy, and thermogravimetric analysis were used to evaluate the compound 3-CSNPs nanocomposites. FTIR was used to identify the essential functional groups of compound 3-CSNPs nanocomposites. In contrast, the XRD pattern explained the interaction between compound 3 and its carrier CSNPs nanocomposites. As a result, there is a strong interaction between compound 3 and CSNPs. Besides that, the release profile of compound 3 from compound 3-CSNPs nanocomposites was studied at pH 7.4, and the result implied that the release exhibited prolonged release from nanocomposites for up to 1400 minutes. For future work, the compound 3-CSNPs could be biologically evaluated potential anti-Alzheimer disease activity in vivo and possible toxicity of the synthesized nanocomposites.