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.
出处
《中草药》
CAS
CSCD
北大核心
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)
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
naringenin
nanostructured lipid carriers
emulsion evaporation-solidified at low temperature method
central composite design-response surface method
sustained-release
作者简介
李静静（1990-），女，硕士研究生，主要从事药物新型给药系统的研究。E-mail：492557417@qq．com
通信作者张良珂，男，博士，教授。Tel：（023）68485161E-mail：zlkdyx@126．com
