Preparation and in vitro Transdermal Permeation Evaluation of Borneol-modified Colchicine Ethosome
10.6039/j.issn.1001-0408.2018.07.09
- VernacularTitle:冰片修饰的秋水仙碱醇质体的制备及体外扩散性评价
- Author:
Nan ZHANG
1
;
Hui SONG
;
Zhiqiang WANG
;
Yujia ZHANG
;
Wensheng ZHENG
Author Information
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
- Keywords:
Colchicine;
Borneol-modified;
Ethosome;
Preparation;
Modification rate;
in vitro diffusion;
Encapsulation rate;
Accumulative permeability
- From:
China Pharmacy
2018;29(7):902-906
- CountryChina
- Language:Chinese
-
Abstract:
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 103.52 μ g/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.
