Elastic liposomes for skin delivery of dipotassium glycyrrhizinate.
The aim of this study was to evaluate the possibility of using liposomes for skin delivery of dipotassium glycyrrhizinate (KG), an anti-inflammatory agent employed in treating acute and chronic dermatitis, and of formulating such liposomes in an oil-in-water emulsion (O/W). KG had emulsifying properties and the possibility of producing elastic liposomes was verified. Liposomes containing soya lecithin (PC) or hydrogenated soya lecithin (HPC) mixed with KG in w/w ratios of 2:1, 4:1 or 8:1 were prepared by the solvent evaporation method and then passed through a high pressure homogeniser. Liposome size and entrapment efficiency were determined and the interaction between KG and HPC was investigated using differential scanning calorimetry (DSC). Transepidermal permeation through intact pig skin and skin deposition of KG from liposomes and O/W emulsion containing liposomes were assessed and compared with values for aqueous control solutions. No marked differences were observed between PC and HPC liposomes. Liposome sizes ranged from 90 to 120 nm. Entrapment efficiency depended on the lipid:KG ratio; the maximum efficiency was obtained at 4:1 w/w. KG interacted with liposomes disrupting and fluidising the lipid bilayer, forming elastic liposomes able to penetrate through membrane pores of diameter much smaller than their own diameter. The liposome structure was maintained when dispersed in an O/W emulsion. The skin fluxes were less than the HPLC detection limit for all systems, while skin deposition increased 4.5-fold compared with aqueous solutions when KG was formulated in liposomes.
Trotta
M
M
Dipartimento di Scienza e Tecnologia del Farmaco, Universita di Tornio, via P. Giuria 9, 10125 Turin, Italy. trotta@pharm.unito.it
Peira
E
E
Debernardi
F
F
Gallarate
M
M
D000287:Administration, Topical; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000032:analysis; D002152:Calorimetry, Differential Scanning; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems; D004548:Elasticity; D019695:Glycyrrhizic Acid / Q000008:administration & dosage* / Q000032:analysis; D008081:Liposomes; D012869:Skin Absorption; D013552:Swine
D000894:Anti-Inflammatory Agents, Non-Steroidal; D008081:Liposomes; D019695:Glycyrrhizic Acid