A novel use of two components of Cape aloe, aloin A and aloesin, acting as stabilizers in the preparation of gold and silver nanoparticles, is reported. Stable water-soluble particles of different size and shape are prepared by varying the reaction conditions, temperature, reaction time, and reducing agents. Characterization of the obtained particles is performed using UV-visible, attenuated total reflection Fourier transform infrared (ATR-FTIR), and 1H NMR spectroscopies and transmission electron microscopy (TEM). The efficient cellular uptake of 50 nm sized aloin A and aloesin stabilized gold particles into macrophages and HeLa cells was investigated, proposing these particles as nanovehicles.