摘要
在高相转变温度的脂质体中插入偶氮苯两亲分子(GalAzoCns),利用偶氮苯基团的光异构化实现药物的可控释放。以主动载药法包载阿霉素DOX,包封率可达95%。实验表明,黑暗环境中的脂质体对DOX有很好的防泄漏效果(RR≈5%),而经紫外线照射的脂质体对DOX具有突释作用,释放量受很多影响因素的影响。实验表明,脂质体组成中胆固醇的含量较高时,偶氮苯两亲分子的结构及含量起主导作用。当偶氮苯两亲分子的含量固定时,脂质体膜的性质对DOX的释放量较大影响,胆固醇含量的减少紫外光照后DOX的释放量增加,且在脂质体中不含胆固醇时达到100%。
Azobenzene glycolipids GalAzoCns which have an azobenzene moiety between the galactosyl and various sized carbon chains,have been incorporated into liposome bilayer with high phase transition temperature.The GalAzoCns suffered photoinduced isomerization in the liposomal bilayer,which could realize the controllable release of drugs.Doxorubicin was loaded into the liposome via ammonium sulfate gradient method.The encapsulate efficiency reached up to 95%.Leakage of DOX indicated that unmodified liposome and modified liposome without UV light irradiation can preserve its cargo stably.However,when modified liposome was exposed to UV light,DOX was burst released.The release efficiency was decided by the molecular structure and percentage of GalAzoCns with the same lipid composition,while decided by the percentage of cholesterol with the same proportion of GalAzoCns.DOX could be totally released from liposomes when the percentage of cholesterol decreases to 0.
引文