柚皮素纳米结构脂质载体的处方优化和初步评价  

Optimization and evaluation of naringenin loaded nanostructured lipid carriers

作　　者：李静静[1] 贾运涛[2] 田睿[3] 邓萍[1] 李腾[1] 张良珂[1] 

机构地区：[1]重庆医科大学重庆市生物化学与分子药理学重点实验室,重庆400016 [2]重庆医科大学附属儿童医院药剂科,重庆400010 [3]重庆医科大学实验教学中心,重庆400016

出　　处：《中草药》2015年第2期211-215,共5页Chinese Traditional and Herbal Drugs

基　　金：重庆市自然科学基金项目(cstc2012jj A10021);高等学校博士学科点专项科研基金(20125503120003);重庆市卫生局医学科研项目(2013-2-060);重庆医科大学大学生科学研究与创新实验项目(201432;201244;201217);重庆市教育委员会科学技术研究项目(KJ120307);海扶之星学生科研基金项目(XS201309)

摘　　要：目的制备一种具有缓释作用的柚皮素(NG)新型纳米结构脂质载体(NG-NLC),并对其理化性质进行初步考察。方法以乳化蒸发-低温固化法制备NG-NLC。采用星点设计-效应面法考察柚皮素-脂质材料比、单硬脂酸甘油酯-辛癸酸甘油酯比,以及乳化剂用量对包封率和载药量的影响。通过包封率、载药量、粒径、DSC分析以及体外释放度来评价NG-NLC的特性。结果经过处方优化,确定NG-NLC最佳工艺条件为柚皮素-脂质材料比为20.77,单硬脂酸甘油酯-辛癸酸甘油酯比为1.85,乳化剂用量为58.45 mg,制备的NG-NLC包封率为(80.13±1.45)%,载药量为(3.59±0.06)%,平均粒径为(134.1±9.1)nm,多分散系数(PDI)为0.152±0.044;体外释放实验表明,NG-NLC在p H 7.4的缓冲溶液中前期有突释现象,后期则有缓释特征。结论采用乳化蒸发-低温固化法成功制备了NG-NLC,为柚皮素的临床应用奠定了基础。Objective To prepare novel naringenin-loaded nanostructured lipid carriers（NG-NLC） and investigate their physicochemical properties.Methods The NG-NLC were prepared by emulsion-evaporation-solidified at low temperature（EESLT） method.Central composite design-response surface methodology（CCD-RSM） was used to optimize the formulation of NG-NLC.Naringenin/lipid materials ratio,glycerol monostearate（GMS）/medium chain triglycerides（MCT） ratio,and emulsifier concentration were identified as key factors which were responsible for entrapment efficiency（EE） and drug loading（LD） of NG-NLC.The mean diameter,DSC analysis,and in vitro release characteristics of NG-NLC were investigated to evaluate their physicochemical properties.Results After the formulation optimization,the naringenin/lipid materials ratio was 20.77,GMS/MCT ratio was 1.85,and emulsifier concentration was 58.45 mg.The EE of NG-NLC was（80.13 ± 1.45）%,LD was（3.59 ± 0.06）%,average diameter of particles was（134.1 ± 9.1） nm,and polydispersity index（PDI） was 0.152 ± 0.044.In vitro release test revealed that the drug could be sustained-released from NG-NLC in buffer solution（p H 7.4） after a burst release in initial phase.Conclusion The EESLT method could be employed to prepare NG-NLC,which may lay the foundation for its further clinical application.

关 键 词：柚皮素 纳米结构脂质载体 乳化蒸发-低温固化法 星点设计-效应面法 缓释作用 

分 类 号：R283.6[医药卫生—中药学]