Preliminary Studies on X-Ray-sensitive Liposome  

作　　者：MENG Fan-xu XU Hua-ping QI Yan-fei XU Kun SONG Xiu-ling NIU Shu LI Juan 

机构地区：[1]School of Public Health,Jilin University,Changchun 130021,P.R.China [2]Key Lab of Organic Optoelectronics and Molecular Engineering,Department of Chemistry,Tsinghua University,Beijing 100084,P.R.China

出　　处：《Chemical Research in Chinese Universities》2012年第2期319-322,共4页高等学校化学研究（英文版）

基　　金：Supported by the National Basic Research Program of China(No.2007CB808000);the National Natural Science Foundation of China(Nos.81072337,21074066)

摘　　要：The synthesis of a new type of X-ray-sensitive compound ＂di-（1-hydroxylundecyl） diselenide＂ and its application in the preparation of a new type of liposome with X-ray sensitivity was reported.This new liposome was synthesized to encapsulate doxorubicin hydrochloride（Dox）,with its physical and chemical properties,stability,and radiation sensitivity determined.Based on the pH-gradient method,liposomal Dox was prepared via ultrasonic emulsification and then purified on a Sephadex G50 mini-column.UV spectrophotometry and liquid chromatography were used to detect the encapsulation efficiency and radiation sensitivity of the Dox-loaded liposome.The results show that through changes in release rate,this liposome shows a relative radiosensitivity.In terms of radiation sensitivity,the drug leak rate of the X-ray-sensitive Dox-loaded liposome increased gradually and peaked at 65.4% under the X-ray radiation of a dose of 10 Gy or more than 10 Gy,which is significantly different from that of ordinary liposomes.Meanwhile,X-ray-sensitive Dox-loaded liposome has a good dispersion stability,with an average particle size of approximate 120 nm.The efficiency of this liposome encapsulating Dox was 75.84%,slightly lower than that of ordinary liposomes.The X-ray-sensitive Dox-loaded liposome exhibited suspension stability within 30 d of storage at 4 °C,without visible precipitation.Di-（1-hydroxylundecyl） diselenide is safe and noncytotoxic and compared with those of synthetic phospholipids its synthesis is low cost and does not require complex conditions.The synthesis of a new type of X-ray-sensitive compound ＂di-（1-hydroxylundecyl） diselenide＂ and its application in the preparation of a new type of liposome with X-ray sensitivity was reported.This new liposome was synthesized to encapsulate doxorubicin hydrochloride（Dox）,with its physical and chemical properties,stability,and radiation sensitivity determined.Based on the pH-gradient method,liposomal Dox was prepared via ultrasonic emulsification and then purified on a Sephadex G50 mini-column.UV spectrophotometry and liquid chromatography were used to detect the encapsulation efficiency and radiation sensitivity of the Dox-loaded liposome.The results show that through changes in release rate,this liposome shows a relative radiosensitivity.In terms of radiation sensitivity,the drug leak rate of the X-ray-sensitive Dox-loaded liposome increased gradually and peaked at 65.4% under the X-ray radiation of a dose of 10 Gy or more than 10 Gy,which is significantly different from that of ordinary liposomes.Meanwhile,X-ray-sensitive Dox-loaded liposome has a good dispersion stability,with an average particle size of approximate 120 nm.The efficiency of this liposome encapsulating Dox was 75.84%,slightly lower than that of ordinary liposomes.The X-ray-sensitive Dox-loaded liposome exhibited suspension stability within 30 d of storage at 4 °C,without visible precipitation.Di-（1-hydroxylundecyl） diselenide is safe and noncytotoxic and compared with those of synthetic phospholipids its synthesis is low cost and does not require complex conditions.

关 键 词：Drug delivery system SELENIUM Radio-chemo-concurrent LIPOSOME 

分 类 号：TQ460.4[化学工程—制药化工] S540.352[农业科学—作物学]