Skin-compatible lecithin drug delivery systems for fluconazole: effect of phosphatidylethanolamine and oleic acid on skin permeation

Abstract

The purpose of the present study was to evaluate skin-compatible drug delivery systems for fluconazole. Pseudoternary phase diagrams were constructed, composed of different soybean lecithins/oil/isopropanol and water. The role of the various lecithin compositions was expressed in the different resulting isotropic areas. Based on these phase diagrams, two systems were chosen as drug delivery systems for fluconazole. The influence of phosphatidylethanolamine and of the oil component on the skin permeation of fluconazole was investigated. The more phosphatidylethanolamine, the greater was the fluconazole skin permeation, independent of the hydrophilicity of the system. The influence of oleic acid and isopropylmyristate as the oil component was compared and a greater penetration enhancing effect was found for the microemulsion containing oleic acid.

Investigation of microemulsion microstructure and its impact on skin delivery of flufenamic acid

“…The NSAID flufenamic acid represents an appropriate model drug for skin studies since it is dermally applied in commercially available products (Schwarz et al, 2012). Moreover, fluorine containing compounds were chosen as the 19 F isotope is a very sensitive NMR probe that is also suitable for self-diffusion studies (Hoeller et al, 2008). Fluorocarbon surfactants are surface active materials in which some or all hydrogen atoms in the hydrophobic moiety are replaced by fluorine atoms (Szymczyk, 2013).…”

Multinuclear NMR Characterisation and Dermal Delivery of Fluorinated Drugs in Soybean-Microemulsion Systems

“…8 Also, the compositions of commercially available lecithins may affect the microstructure and thus the permeation of the incorporated drugs. 9 In this study we are therefore evaluating the physical properties of microemulsion systems containing different commercially available soybean lecithins regarding their phosphatidylcholine content, their composition and their capability to transport different entrapped lipophilic drugs through the skin. In order to evaluate the microstructure the resulting systems should also be characterised by generating self-diffusion coefficients of the individual components of the vehicle by 1 H and 31 P NMR.…”

Engineering plant membranes using droplet interface bilayers

“…While previous studies have shown that the addition of cerebrosides 37,38 or cholesterol 38,39 reduces the permeability of liposomes, these reports also indicate that cerebrosides have a more potent effect compared to cholesterol, which is in-line with our findings. The presence of unknown components in SPLE makes it difficult to speculate why DOPC:SPLE DIBs were significantly more permeable compared to DOPC:DOPC DIBs, although this could be due to the presence of 22.1% PE which has been shown to increase the permeability to fluconazole in skin membranes 40 . In any case, our data confirms the presence of asymmetric DIBs made from our plant lipid formulations and clearly shows that our different membrane compositions can give rise to differences in the effective membrane permeability, suggesting that membrane permeability could be specifically tuned to replicate other plant membranes.…”