Transdermal delivery of diclofenac using microemulsions.
A transdermal preparation containing diclofenac diethylammonium (DDA) was developed using an O/W microemulsion system. Of the oils tested, lauryl alcohol was chosen as the oil phase of the microemulsion, as it showed a good solubilizing capacity and excellent skin permeation rate of the drug. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and cosurfactant for microemulsion formation, and the effect of these additives on skin permeation of DDA was evaluated with excised rat skins. The optimum formulation of the microemulsion consisted of 1.16% of DDA, 5% of lauryl alcohol, 60% of water in combination with the 34.54% of Labrasol (surfactant)/ethanol (cosurfactant) (1:2). The efficiency of formulation in the percutaneous absorption of DDA was dependent upon the contents of water and lauryl alcohol as well as Labrasol:ethanol mixing ratio. It was concluded that the percutaneous absorption of DDA from microemulsions was enhanced with increasing the lauryl alcohol and water contents, and with decreasing the Labrasol:ethanol mixing ratio in the formulation.
Kweon
Jang-Hoon
JH
College of Pharmacy, Sungkyunkwan University, 300 Chonchon-dong, Changan-gu, Suwon, Kyonggi-do 440-746, Korea.
Chi
Sang-Cheol
SC
Park
Eun-Seok
ES
D000279:Administration, Cutaneous; D000818:Animals; D004008:Diclofenac / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D004655:Emulsions; D010316:Particle Size; D051381:Rats; D012867:Skin / Q000187:drug effects / Q000378:metabolism
D004655:Emulsions; D004008:Diclofenac