Electrically-assisted skin permeation of two synthetic capsaicin derivatives, sodium nonivamide acetate and sodium nonivamide propionate, via rate-controlling polyethylene membranes.
The objective of this study was to examine the transdermal delivery of sodium nonivamide acetate (SNA) using iontophoresis and electroporation with ultra high molecular weight polyethylene membranes (Solupor) to achieve controlled transdermal drug delivery. A derivative of SNA, sodium nonivamide propionate (SNP), was also used as a model drug in this investigation. Iontophoresis increased the transdermal permeation of SNA as compared to passive diffusion. Most Solupor membranes were rate-limiting for the iontophoretic permeation of SNA except for Solupor 8P07, which showed negligible resistance to SNA delivery. The tortuosity (Gurley number), pore size, and the current density-induced attachments on the surface of the Solupor membranes may have been important for their rate-controlling effect. The trends for inhibiting or controlling SNA permeation were similar for both iontophoretic and electroporation applications. The higher molecular size and lower hydrophilicity of SNP compared to SNA resulted in lower permeation of SNP using electrically-assisted methods. Moreover, the various types of Solupor membranes showed similar trends for both SNA and SNP. This present study indicates that Solupor membranes act as rate-limiting membranes for controlling the release and skin permeation of both SNA and SNP by electrically-assisted methods.
Fang
Jia-You
JY
Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan. fajy@mail.cgu.edu.tw
Huang
Yaw-Bin
YB
Wang
Hsin-Yuan
HY
Tsai
Yi-Hung
YH
D000279:Administration, Cutaneous; D000818:Animals; D002211:Capsaicin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D018274:Electroporation; D005260:Female; D066298:In Vitro Techniques; D007478:Iontophoresis; D008567:Membranes, Artificial; D051379:Mice; D008819:Mice, Nude; D008855:Microscopy, Electron, Scanning; D008970:Molecular Weight; D011095:Polyethylenes; D012867:Skin / Q000737:chemistry / Q000648:ultrastructure
D008567:Membranes, Artificial; D011095:Polyethylenes; D002211:Capsaicin; C040937:nonivamide