Hr. Moghimi et al., A LAMELLAR MATRIX MODEL FOR STRATUM-CORNEUM INTERCELLULAR LIPIDS .1. CHARACTERIZATION AND COMPARISON WITH STRATUM-CORNEUM INTERCELLULAR STRUCTURE, International journal of pharmaceutics, 131(2), 1996, pp. 103-115
The principal barrier to transdermal delivery of most drugs is the lam
ellar intercellular lipid matrix of the stratum corneum (SC). Preparat
ion of a model for this matrix provides opportunities to probe the nat
ure of the SC barrier. Here, a method has been developed to construct
a model matrix comprising 20% cholesterol, 25% water and 55% SC free f
atty acids and their soaps. X-ray diffraction studies revealed that th
e model matrix consists of both lamellar gel (L(beta)) and lamellar li
quid crystalline (L(alpha)) phases and possibly some crystalline lipid
s at ambient temperature, in good agreement with SC intercellular lipi
ds structure. The matrix provided a lamellar mesomorphic structure fro
m ambient to almost 100 degrees C, a hexagonal mesomorphic phase at ar
ound 105 degrees C and an isotropic liquid at 140 degrees C as studied
by hot-stage polarised light microscopy (PLM). The matrix showed seve
n endothermic transitions in differential scanning calorimetry (DSC) f
rom - 30 to 120 degrees C which were well correlated with PLM results
and human SC data. DSC results also revealed that around 20% of the to
tal water in the matrix was bound. These studies have provided a simpl
e matrix which models the lipid domain of human SC and should be usefu
l in probing the barrier nature of SC and drug and enhancer interactio
ns with SC intercellular lipids.