چكيده فارسي :
Dendrimers are the emerging polymeric architectures that are known for their defined structures, versatility in drug delivery and high functionality whose properties resemble with biomolecules. Controlled drug delivery systems have various advantages compared to conventional treatment ways, such as high efficacy, reduced toxicity, and improved quality of life of patient. Dendrimers offer advantages including a lower polydispersity index, multiple sites of attachment, and a controllable, well-defined size and structure that can be easily modified to change the chemical properties of the system[1]. Procarbazine HCl is a ‗nonclassical‘ oral alkylating anticancer agent that was first synthesized in the late 1950s. It has been used in the treatment of many cancers, but its main use is in the treatment of Hodgkin‘s lymphoma and brain tumors and, to a lesser extent, Non-Hodgkin‘s lymphoma and primary central nervous system lymphoma. Procarbazine is a prodrug that undergoes metabolic transformation into active intermediates that are thought to inhibit DNA, RNA, and protein synthesis[2] The aim of this study synthesis of new polyamidoamine (PAMAM) dendrimer having polyethylene glycol grafts as novel drug carrier for procarbazine delivery. In this study we successfully synthesized and conjugated PEGylated PAMAM dendrimers with procarbazine. Cytotoxicity was measured by MTT assay on A549 cell line. In this study, the second generation polyamide amine(PAMAM) dendrimers were synthesized by divergent method[l]. Then The carboxyl terminal functional groups of PEG activated with DCC and Conguated with G2PAMAM. Their positive ammonium surfaces were modified and , the drug is covalently attached to the periphery of the dendrimer to form dendrimer prodrugs[3]. Moreover surface were characterization of PEGylated PAMAM dendrimers was carried out TEM micrographs. Further physiochemical , physiological and biological properties such as drug entrapment , drug release, characterization of structures and cytotoxicity were carried out by UV,FTIR, NMR and MTT assay techniques for PEGylated and non PEGylated PAMAM dendrimer. The results showed that The physicochemical and biopharmaceutical properties of PEGylated G2PAMAM dendrimer better than and non PEGylated G2PAMAM dendrimer.
