Objective: Biomineralization is the natural process in which organisms develop minerals such as calcium phosphate, calcium carbonate, and silica to strengthen their tissues and make bone and teeth for the body. From this biomineralization process, one can derive the idea that the mineral deposition can reinforce the assembled nanostructures. As another property, the aqueous solubility of minerals such as CaP and CaCO3 is largely dependent on pH. Biomimetic mineralized hybrid systems have attracted increasing interest in the field of nanotechnology and biomedical science for the development of novel nanocarrier systems because the introduction of bioinspired mineralization enables nanocarriers to maintain structural robustness under physiological pH (pH 7.4) and selectively dissolve under the acidic pH of the intracellular endo/lysosome or tumoral region. Therefore, from the knowledge of the biomimetic hybrid structures and biomineral characteristics, we describe a drug delivery platform technology of therapeutic drugs and biomedical applications. Methods: We have developed novel nano-formulations for therapeutic drug delivery systems. Synthesis of copolymer and preparation of nano-formulation design were conducted. The characterization of nano-formulations and in vitro therapeutic effects were also evaluated. Results: We successfully synthesized with an optimal copolymer template, and formulations were well characterized. In addition, we confirmed the therapeutic effect of nano-formulations in vitro. Conclusion: Our results indicated that these novel nano-formulations may show the effective therapeutic effects. These systems showed an excellent therapeutic character for biomedical applications.