Abstract��OBJECTIVE To synthesize a novel cationic lipid,N,N-dimethyl-[N��,N��-di-(stearoyl-1-ethyl)] 1,3-diaminopropane (DMSP),and evaluate its feasibility as methotrexate(MTX) carrier. METHODS DMSP and phosphatidylcholine were employed to prepare liposomes by reverse phase evaporation method,and then MTX was entrapped by physical mixing. The entrapment efficiency was determined by ultracentrifugation,and its release ratio was evaluated by dialysis. The morphology of liposomes was observed under transmission electron microscope. The average diameter and Zeta potential were determined by laser particle size analyzer. MTT test was used to evaluate the cytotoxicity of liposomes as drug carrier and the inhibition of cancer cells growth. RESULTS The obtained liposomes showed regular shape and uniform size,with a mean Zeta potential of +(36.26��4.77)mV and average diameter of 120 nm. The liposomes had low hemolytic activity and cytotoxicity. With the help of DMSP the cationic liposomes achieved a very high entrapment efficiency for the hydrophilic drug MTX (91.50��1.02)%. The inhibition of the MTX liposomes on cancer cells growth was much higher than that of MTX solution. CONCLUSION DMSP is a novel cationic lipid with low cytotoxicity and high entrapment efficiency,which has a great application potential in drug delivery system.
����ϲ,֣����,�Ĵ���,�۰���,����,ëӱӱ. N,N-����-[N��,N��-˫(Ӳ֬����-1-�һ�)]1,3-�������ĺϳɡ����ʼ���Ϊ�װ����������Ӧ��[J]. �й�ҩѧ��־, 2016, 51(6): 473-477.
WANG Wen-xi,ZHENG Hai-li,XIA Chun-nian,SHAO An-na,DING Min,MAO Ying-ying. Synthesis and Characterization of N,N-dimethyl-(N��,N��-di-stearoyl-1-ethyl) 1,3-Diaminopropane as Drug Delivery System of Methotrexate. Chinese Pharmaceutical Journal, 2016, 51(6): 473-477.
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2016, Vol. 51 
