To improve delivery efficiency of anastrozole, we applied dendrimer-based stealth nanoparticles to encapsulate anastrozole to formulate stealth anastrozole nanoparticles. This work demonstrated that stealth nanoparticles composed of a PAMAM dendrimers core and a PEG layer could encapsulate anastrozole, hence causing improved water solubility of anastrozole. Anastrozole encapsulation depended on concentration of stealth nanoparticles and generation of dendrimer. The extended release of anastrozole was achieved. We envisioned that this highly structurally adaptable stealth nanoparticle could be further biofunctionalized to construct a targeted therapeutic delivery system for breast cancer treatment.