Poly (lactic-co-glycolic acid) (PLGA) is one of the most effective biodegradable polymeric nanoparticles(NPs). It has been approved by the US FDA to use in drug delivery systems due to controlled and sustainedreleaseproperties, low toxicity, and biocompatibility with tissue and cells. In the present review, the structureand properties of PLGA copolymers synthesized by ring-opening polymerization of DL-lactide and glicolidewere characterized using 1H nuclear magnetic resonance spectroscopy, gel permeation chromatography,Fourier transform infrared spectroscopy and differential scanning calorimetry. Methods of preparation andcharacterization, various surface modifications, encapsulation of diverse anticancer drugs, active or passivetumor targeting and different release mechanisms of PLGA nanoparticles are discussed. Increasing experience inthe application of PLGA nanoparticles has provided a promising future for use of these nanoparticles in cancertreatment, with high efficacy and few side effects.