Polyamidoamine (PAMAM) dendrimers is a new non viral drug carrier. However their high surface toxicity limits PAMAM dendrimers application in drug delivery. The purpose of present work was aimed to developing and exploring PEGylated G4 and G5 PAMAM dendrimers for anti HIV drug lamivudine. In this study we successfully prepared G4 and G5 PAMAM dendrimers with ethylene diamine core and PEGylated with MPEG for surface modifications. Further physiochemical and physiological parameter such as UV, IR, TEM, DSC, drug entrapment, drug release and hemolytic toxicity of both PEGylated and non PEGylated PAMAM dendrimers were determined and compared. Here the PEGylation of PAMAM dendrimers reduce the surface toxicity and increase the drug loading capacity of PAMAM dendrimers. Moreover PEGylated PAMAM dendrimers had released then drug in controlled and prolonged time. Hence the PEGylated PAMAM dendrimers were found as suitable drug delivery carrier for anti HIV drug lamivudine