P. Cornwell, Joe Tubek, Hans A.H.P van Gompel
Sep 15, 1998
Citations
0
Influential Citations
22
Citations
Journal
International Journal of Pharmaceutics
Abstract
Abstract Eleven widely used lipophilic formulation excipients have been screened for their skin penetration enhancing effects. The excipients tested were glyceryl tricaprylate/caprate, isopropyl myristate, glyceryl monocaprylate/caprate, decyl oleate, polyethylene glycol-6 glyceryl dicaprylate/caprate, isopropyl isostearate, isostearyl isostearate, glyceryl monoisostearate, polyglyceryl-3 diisostearate, vegetable squalane and isostearyl alcohol. Excipient effects were evaluated by measuring skin permeability coefficients towards a model hydrophilic drug, 5-fluorouracil (5-FU), before and after a 6-h treatment with neat excipient. The skin penetration enhancing mixture, 10% (w/w) Azone® in propylene glycol, was used as a positive control. Only one excipient, glyceryl monocaprylate/caprate, had enhancement effects significantly above the buffer control ( p P octanol/water and hydrophilic–lipophilic balance values were calculated for each of the excipients. It was concluded that, of the excipients screened, glyceryl monocaprylate/caprate is the only penetration enhancer because (1) it is the least lipophilic, (2) it has surfactant properties, and (3) it has the optimum alkyl chain length for surfactant-type skin penetration enhancers. Since glyceryl monocaprylate/caprate has only moderate enhancement effects, it should be useful as a mild, well-tolerated skin penetration enhancer.