Since there have been many difficulties in clinical administration of anticancer drugs due to their poor solubility & targeting, development of new biodegradable Nano-carriers can provide good solutions to overcome the most of recent problems to obtain a better controlled release and targeted delivery of drugs with better efficiency and less side-effects. Acidic pH is regarded as a phenotypic characteristic of cancer tumors. Under this acidic condition, it is known that the surface charge of Chitosan-modified nano-particles become more positive. On the other hand, cancer cells are negatively charged. It is worth mentioning that by loading of anticancer drugs into this novel system, a strong electrostatic interaction between negatively charged tumor cells and positively charged nano-particles will be obtained. In order to obtain desired, surface morphology and particle size of poly(lactide-co-glycolide) (PLGA) nanoparticles, and high emulsifying effects, chitosan-modified PLGA NPs were optimized as a potential carrier for drug delivery. The particle size and distribution, surface morphology, phase composition corresponding to different emulsifiers and different stirring times were characterized. Further, it was found that Chitosan could be a perfect modifier for making PLGA NPs as potential carrier for drug delivery.