Interactions between liposomes and human stratum corneum in vitro: freeze fracture electron microscopical visualization and small angle X-ray scattering studies.
The interactions between three liposomal formulations and human stratum corneum were visualized using freeze fracture electron microscopy. A new replica cleaning method was introduced. Human stratum corneum was submerged for 48 h in liposome suspensions prepared from commercially available phospholipid mixtures. The size, lamellarity and lipid moieties of the liposomes were similar. The main difference between the three phospholipid formulations was the hydrophilicity of the headgroups. The composition dependence of the interactions between these vesicles and human stratum corneum was investigated. In essence, two types of interaction were observed: adsorption of the liposomes on to the outer surface of the stratum corneum, and ultrastructural changes in deeper layers of the stratum corneum caused by mixing of the liposomal constituents and the stratum corneum lipids. The electron microscopic observations were verified with small-angle X-ray scattering. It was found that liposomes composed of phospholipids containing relatively small hydrophilic headgroups showed a marked interaction with the skin lipids of human stratum corneum in vitro. The complexity of the phospholipid mixtures, however, made it very difficult to determine the exact effect each of these headgroups has on the interactions between these vesicles and human stratum corneum.
Hofland
H E
HE
Leiden/Amsterdam Center for Drug Research, Division of Pharmaceutical Technology, Leiden University, The Netherlands.
Bouwstra
J A
JA
Boddé
H E
HE
Spies
F
F
Junginger
H E
HE
D000327:Adsorption; D046508:Culture Techniques; D004337:Drug Carriers; D005614:Freeze Fracturing; D006801:Humans; D008081:Liposomes / Q000378:metabolism* / Q000493:pharmacokinetics; D008854:Microscopy, Electron; D012867:Skin / Q000378:metabolism* / Q000648:ultrastructure; D014961:X-Ray Diffraction
D004337:Drug Carriers; D008081:Liposomes