Millions of deaths are caused every year by cancer, which is one of the most widespread diseases in the world. New innovative therapies have been developed by nanomedicine in recent years to address this issue, specifically using drug delivery methods and approaches. Among the many materials used to create nanocarriers, biopolymers like chitosan are widely utilized. The aim of this work is to describe the synthesis of chitosan nanocapsules (NCs) and the encapsulation of anticancer compounds. Two substances have been chosen: doxorubicin (DOX), a drug largely employed in the treatment of cancer for decades, and aloe-emodin (AE), an anthraquinone isolated from the plant of Aloe vera L., that has been shown to have a strong anti-carcinogenic effect. The commercially available A.vera latex was used to extract AE. The obtained Dox-loaded and AE-loaded chitosan NCs were characterized by Scanning Electron Microscopy (SEM), Atomic Force Microscopy (AFM), and Dynamic Light Scattering (DLS). Moreover, UV-vis spectroscopy was used to analyze the encapsulation efficiency of these nanomaterials. Finally, cytotoxicity and in vitro release studies of active agents have been conducted on the cell line of human adenocarcinoma breast MDA-MB-231. The results obtained showed that doxorubicin and aloe-emodin were released gradually from NCs over time and with a dose-dependent effect, resulting in a significant reduction in cellular viability. Moreover, immunofluorescence observations have revealed the uptake of DOX-NCs and AE-NCs in MDA-MB-231 cells and their localization both in the cytoplasm and in the nuclear region.