M. Fresta et G. Puglisi, APPLICATION OF LIPOSOMES AS POTENTIAL CUTANEOUS DRUG-DELIVERY SYSTEMS- IN-VITRO AND IN-VIVO INVESTIGATION WITH RADIOACTIVELY LABELED VESICLES, Journal of drug targeting., 4(2), 1996, pp. 95-101
The potential application of Liposomes as dermal delivery systems was
investigated, with regard to vesicle composition and size. Liposomes w
ere made up of phospholipids or skin lipids, referred to as phospholip
id-based liposomes and stratum corneum lipid-based liposomes, respecti
vely. A stripping procedure from stratum corneum to dermis by means of
adhesive tape was carried out to evaluate the extent of accumulation
in the superficial layers of the skin. The various liposomes were radi
olabelled both in the bilayer structures with [H-3]cholesterol, [C-14]
dipalmitoylphosphatidylcholine and [C-14]palmitic acid, depending on V
esicle type, and in the aqueous compartments with [C-14]inulin. Inulin
absorption and elimination was also evaluated. Stratum corneum lipid-
based liposomes could permeate the stratum corneum to a greater extent
than phospholipid-based liposomes. Stratum corneum lipid-based liposo
mes could deliver a greater amount of aqueous radiolabelled marker ([C
-14]inulin) to the deeper skin strata (epidermis and dermis), while av
oiding systemic absorption and, hence, organ distribution and renal el
imination of [C-14]inulin. Another important parameter in determining
the extent of absorption is the vesicle size: the greater the mean siz
e of Liposomes, the poorer the permeation through stratum corneum laye
rs. When fluid liposomes made up of unsaturated lecithins were used, a
percutaneous absorption was obtained instead of dermal delivery. Stra
tum corneum lipid-based unilamellar liposomes may be suitable devices
for dermal delivery.