The aim of this work was to prepare composite microspheres based on chitosan and hydroxyapatite as potential carriers for targeted antitumor drug delivery. It is important to highlight the pH sensitivity of chitosan, which allows trgeted drug release around tumor site. However, chitosan can release a drug before reaching the targeted site, hence, chitosan-based composite materials could be more suitable in order to increase stability of potential drug carrier. In this work, composite microspheres were synthesized via electrospraying process. The composites microspheres were prepared with different ratio of hydroxyapatite in chitosan solution (5 – 15%) in order to improve the efficiency of the future drug encapsulation. The stability of composite microspheres was achieved through chelation of transition metal ions (copper and zinc) by chitosan macromolecules due to the high affinity of metal ions towards chitosan amino groups. The shape, size and microstructure of composite microspheres were analyzed by optical microscopy and SEM analysis, while the materials composition was identified by XRD analysis. The presence of new crystalline phases within chitosan complexes and composites with metal ions was not observed. The microscopic analysis has indicated highly porous structure of composite microspheres prepared by zinc (II) ions. The preliminary cytotoxicity assay indicated that hydroxyapatite do not influence on materials toxicity. The composites with different concentration of copper (II) ions showed cytotoxic effect, which was more evident for the materials with higher copper (II) ions concentration. On the contrary, composites with zinc (II) ions were nontoxic for cultured cell line.