Porous silicon nanoparticles have been established as excellent candidates for medical applications as drug delivery devices, due to their excellent biocompatibility, biodegradability, and high surface area. The simple fabrication method by electrochemical anodization of silicon and its photoluminescent properties are some of the merits that have contributed to the increasing interest given to porous silicon. This paper presents the methods of fabrication, which can be customized to control the pore size, various chemical treatments used for the modification of silicon surfaces, and the characterization and pore morphology of silicon structures. Different approaches used for drug loading and the variety of coatings used for the controlled released are revised. The monitoring of the toxicity of silicon degradation products and the in vivo release of a drug in a specific site are described taking into account its significance on medical applications, specifically on cancer therapy.