Nowadays, nanofibers have various applications in the field of medical biology including drug delivery systems (DDSs) and tissue engineering. Many methods have been developed to produce drug release polymers; the most important and applicable of which is known as electrospinning. In this method, the nanoscale and microscale fibers are used as the functional polymers in the DDSs. A variety of electrospinning methods can be used for delivery systems and tissue engineering. The nanofibers loaded with anticancer drugs have attracted a lot of attention in the last decade. Electrospun parameters include voltage, feed rate, rotary collector, pipette or needle hole diameter, the distance between nozzle tip to collector plate, viscosity and molecular weight of the polymer, surface tension, solubility of polymer, soluble electrical conductivity, dielectric constant, and evaporability of the solution; all could be manipulated to regulate the drug release rate in order via changing the diameter of the nanofibers. In addition to directly loading the drug on nanofibers, the nanoparticles are also used to improve the drug efficacy and reduce the required dose, especially in the case of harmful drugs. Depending on the need, various nanoparticles and nanocarriers are being applied along with the drug. Nanocarriers such as viruses, micelles, and liposomes function highly specific since they carry specific ligands on their surface. Magnetic nanoparticles also have a great therapeutic effect on cancer cells when exposed to heat and magnetic fields. Carbon nanoparticles, such as graphene and graphene oxide, due to their layering, can pass through the cell membrane and deliver the drug to the intracellular space.