Transdermal delivery of sodium nonivamide propionate by iontophoresis.
The aim of this study was to investigate the transdermal iontophoresis of a newly designed capsaicin derivative, sodium nonivamide propionate (SNP). The iontophoretic permeation of SNP from various pH buffers increased following the decrease of pH values. This trend was consistent with that of sodium nonivamide acetate (SNA) which is another synthetic analogue of capsaicin. However, the iontophoretic permeability of SNP was much lower than that of SNA. SNP was also delivered iontophoretically from hydrogel formulations. It is suggested that ionizable polymers should be avoided for iontophoretic delivery to maintain good penetration capacity of drugs. Both nonionic cellulose polymers of methylcellulose (MC) and hydroxypropyl methylcellulose (HPMC) showed higher iontophoretic flux for SNP than the others did. Furthermore, the flux of SNP leveled off with an increase in the amount of polymers in hydrogel, indicating that the viscosity of vehicles plays an important role in the permeation of SNP. Comparing the various iontophoretic application modes, the discontinuous on/off cyclic mode showed higher penetration capacity than did the continuous mode although they possessed the same electrical energy. Moreover, the desorption time of SNP from skin was approximately 20 min which was longer than that of SNA.
Fang
J Y
JY
School of Pharmacy, Kaohsiung Medical College, Taiwan.
Kuo
C T
CT
Huang
Y B
YB
Wu
P C
PC
Tsai
Y H
YH
D000279:Administration, Cutaneous; D000818:Animals; D002211:Capsaicin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D002482:Cellulose; D004791:Enzyme Inhibitors / Q000008:administration & dosage* / Q000737:chemistry; D020100:Hydrogels; D006863:Hydrogen-Ion Concentration; D007478:Iontophoresis / Q000379:methods*; D008747:Methylcellulose; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption
D004791:Enzyme Inhibitors; D020100:Hydrogels; D002482:Cellulose; D008747:Methylcellulose; D002211:Capsaicin; C040937:nonivamide