冰片修饰的秋水仙碱醇质体的制备及体外扩散性评价  

Preparation and in vitro Transdermal Permeation Evaluation of Borneol-modified Colchicine Ethosome

作　　者：张楠[1] 宋辉 汪志强 张宇佳[1] 郑稳生[1] ZHANG Nan;SONG Hui;WANG Zhiqiang;ZHANG Yujia;ZHENG Wensheng(Peking Union Medical College/Institute of Materia Medica,Chinese Academy of Medical Sciences/Beijing Key Lab of Drug Delivery Technology and Novel Formulation,Beijing 100050,China)

机构地区：[1]北京协和医学院/中国医学科学院药物研究所/药物传输技术及新型制剂北京市重点实验室,北京100050

出　　处：《中国药房》2018年第7期902-906,共5页China Pharmacy

基　　金：国家科技重大专项子课题(No.2014ZX09507006);中国医学科学院医学与健康科技创新工程(No.2017-I2M-1-011)

摘　　要：目的:制备冰片修饰的秋水仙碱醇质体,并评价其体外扩散效果。方法:采用超声注入-探头超声法制备冰片修饰的秋水仙碱醇质体,并对其进行表征。采用气相色谱法测定冰片含量并计算其在醇质体中修饰率;高效液相色谱法测定秋水仙碱含量并计算其在醇质体中的包封率。分别考察秋水仙碱乙醇溶液、秋水仙碱-冰片乙醇溶液、未加冰片修饰的秋水仙碱醇质体和冰片修饰的秋水仙碱醇质体经皮扩散1、3、6、8、12、16、24、48 h后的累积渗透量和渗透速率。结果:所制冰片修饰的秋水仙碱醇的平均粒径约为(110.4±5.1)nm,多分散系数为0.110±0.030,Zeta电位为(2.33±0.20)mV,形状近似球形,为多层囊泡结构,秋水仙碱包封率为56.12%,冰片修饰率达9.85%。体外扩散试验表明冰片修饰的秋水仙碱醇质体经皮扩散48 h后的单位面积累积渗透量为103.52μg/cm^2,渗透速率分别是未加冰片修饰的秋水仙碱醇质体的1.26倍、秋水仙碱-冰片乙醇溶液的1.77倍、秋水仙碱乙醇溶液的5.14倍。结论:制备的冰片修饰的秋水仙碱醇质体粒径小、粒径分布窄、冰片修饰率高,且经皮渗透效果良好。OBJECTIVE:To prepare borneol-modified colchicine ethosome,and to evaluate its in vitro transdermal permeation.METHODS:Borneol-modified colchicine ethosome was prepared with ultrasonic injection-probe ultrasonic method,and its ethosome was characterized.The content and moditication rate of borneol in borneol-modified colchicine ethosome was determined by GC;content and encapsulation rate of colchicine was determined by HPLC.Accumulative permeability and permeation rate were investigated for colchicine ethanol solution,colchicine-borneol-ethanol solution,colchicine ethosome without borneol-modification,borneol-modified colchicine ethosome after diffused for 1,3,6,8,12,16,24,48 h.RESULTS:The average particle size of borneol-medified colchicine ethosome was about(110.4±5.1)nm,polydispersity index was 0.110±0.030,Zeta potential was(2.33±0.20)mV,prepared ethosome is approximately spherical in shape and multilaminar vesicles in structure.Encapsulation rate of colchicine was 56.12%,and modification rate was 9.85%.The in vitro diffusion tests showed that after diffused for 48 h,accumulative permeability per unit area of borneol-modified colchicine ethosome was 103.52μg/cm2;permeation rate was 1.26 times as colchicine ethosome without borneol-modification,1.77 times as colchicine-borneol-ethanol solution and 5.14 times as colchicine ethanol solution.CONCLUSIONS:Prepared borneol-modified colchicine ethosome has small particle size,narrow particle size distribution,high modification rate and good transdermal permeation.

关 键 词：秋水仙碱 冰片修饰 醇质体 制备 修饰率 体外扩散 包封率 累积渗透量 

分 类 号：R944[医药卫生—药剂学]