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Conventional drug delivery systems have been insufficient for treatment of several diseases especially cancer. Hydrophobic and hydrophilic polymeric nanoparticles have been developed for delivery of therapeutics such as drug or gene in order to overcome drawbacks of conventional therapy. Regardless, polymeric nanoparticles provide more effective treatment with reduced side effects of drugs. Cyclodextrins are more favorable natural polymers to prepare nano-sized drug delivery systems because of their physical and chemical properties. The other advantages of cyclodextrins are: to enhance bioavailability and stability of drug molecules, and protect them from physical conditions include pH, temperature and some enzymes. In order to overcome some disadvantages of natural cyclodextrins and enhance their solubility and interaction with biological membranes, amphiphilic cyclodextrins have been synthesized …