TY - JOUR
T1 - Transdermal delivery of compounds with different lipophilicity and molecular weight from W/O microemulsions analyzed by UPLC-Q-TOF/MS and LC-MS/MS
AU - Lin, Hongmei
AU - Michniak-Kohn, Bozena
AU - Xia, Zhenzhen
AU - Xu, Lingyan
AU - Kang, Qian
AU - Chen, Cheng
AU - Ma, Shuwei
AU - Wu, Qing
N1 - Publisher Copyright:
© 2018 Bentham Science Publishers.
PY - 2018
Y1 - 2018
N2 - Objective: The aim of this study was to develop a novel W/O microemulsion for a natural extract of Wen-Luo-Tong (WLT) containing mainly icariin, hydroxysafflor yellow A (HSYA) and gallic acid to be applied to skin as a potential treatment for peripheral neuropathy. Methods: The oil phase was selected on the basis of affinity with the surfactant and co-surfactant. Pseudo-ternary diagrams were constructed to optimize microemulsions and finally stability studies were performed on the selected formulations. Droplet sizes were analyzed by using a zetasizer and were found to be within the desired range. Selected microemulsions with acceptable viscosities, containing 5%, 8% and 10% of water extract solution, were used for in vitro skin penetration studies using Franz diffusion cells and excised rat skin. New LC-MS/MS and UPLC-Q-TOF/MS methods were employed for quantitative and qualitative analysis. Results: The optimized formulation (ME-4) consisting of 10% (w/w) water extract solution, 60% iso-propyl myristate, 30%(w/w) Smix: Propylene glycol (5:2) significantly increased the cumulative permeated amounts of HSYA, icariin and gallic acid compared with the water extract solution controls. Conclusion: This novel formulation also increased the number of components penetrating rat skin. Ten components were detected in the Franz cell receptor solution using a UPLC-Q-TOF/MS system after the application of formulation ME-4 for 24h on the skin in vitro. However, only one component was detected after applying the control. Therefore, the microemulsion ME-4 was selected for future in vivo pharmacodynamic studies.
AB - Objective: The aim of this study was to develop a novel W/O microemulsion for a natural extract of Wen-Luo-Tong (WLT) containing mainly icariin, hydroxysafflor yellow A (HSYA) and gallic acid to be applied to skin as a potential treatment for peripheral neuropathy. Methods: The oil phase was selected on the basis of affinity with the surfactant and co-surfactant. Pseudo-ternary diagrams were constructed to optimize microemulsions and finally stability studies were performed on the selected formulations. Droplet sizes were analyzed by using a zetasizer and were found to be within the desired range. Selected microemulsions with acceptable viscosities, containing 5%, 8% and 10% of water extract solution, were used for in vitro skin penetration studies using Franz diffusion cells and excised rat skin. New LC-MS/MS and UPLC-Q-TOF/MS methods were employed for quantitative and qualitative analysis. Results: The optimized formulation (ME-4) consisting of 10% (w/w) water extract solution, 60% iso-propyl myristate, 30%(w/w) Smix: Propylene glycol (5:2) significantly increased the cumulative permeated amounts of HSYA, icariin and gallic acid compared with the water extract solution controls. Conclusion: This novel formulation also increased the number of components penetrating rat skin. Ten components were detected in the Franz cell receptor solution using a UPLC-Q-TOF/MS system after the application of formulation ME-4 for 24h on the skin in vitro. However, only one component was detected after applying the control. Therefore, the microemulsion ME-4 was selected for future in vivo pharmacodynamic studies.
KW - Gallic acid
KW - Hydroxysafflor yellow A
KW - Icariin
KW - LC-MS/MS
KW - Microemulsion
KW - Transdermal delivery
KW - UPLC-Q-TOF/MS
UR - http://www.scopus.com/inward/record.url?scp=85050232822&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85050232822&partnerID=8YFLogxK
U2 - 10.2174/1567201815666171221125411
DO - 10.2174/1567201815666171221125411
M3 - Article
C2 - 29268684
AN - SCOPUS:85050232822
SN - 1567-2018
VL - 15
SP - 1009
EP - 1019
JO - Current Drug Delivery
JF - Current Drug Delivery
IS - 7
ER -