Abstract
Purpose. The influence of liposome composition on the bilayer fluidity and on the transport of encapsulated substance into the skin was investigated.
Methods. Multilamellar vesicles (MLV) from dipalmitoylphosphatidylcholine (DPPC) or dimyristoylphosphatidylcholine (DMPC) with various amounts of cholesterol were prepared by the film method and characterised by photon correlation spectroscopy and electron paramagnetic resonance (EPR) methods. The transport of the hydrophilic spin probe encapsulated in MLV into pig ear skin was investigated by EPR imaging methods. The bilayer domain structure was studied by fitting the lineshape of the experimental EPR spectra with the spectra calculated by the model, which takes into account the heterogeneous structure of the bilayer with several coexisting domains.
Results. Cholesterol strongly influences the entrapped volume of liposomes, the domain structure of the lipid bilayer, and the transport of hydrophilic spin probe into the skin. Transport was not observed for liposomes composed of phospholipid:cholesterol 1:0 or 9:1 (mol:mol), not even above the phase transition temperature from the gel to the liquid crystalline phase of DMPC. A significant delivery of hydrophilic spin probe was observed only if there was 30 or 50 mol% of cholesterol in the liposome bilayer.
Conclusions. It can be concluded that the domain structure of the liposome bilayer is more important for the delivery of encapsulated substance into the skin than the liquid crystalline phase of the pure phospholipids bilayer.
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REFERENCES
G. Cevc. Transferosomes, liposomes and other lipid suspensions on the skin: permeation enhancement, vesicle penetration, and transdermal drug delivery. Crit. Rev. in Ther. Drug Carrier Sys. 13:257–388 (1996).
J. Wepierre and G. Couarraze. Topical application of liposomes. In F. Puisieux, P. Couvreur, J. Delattre, J. P. Devissaguet (eds.), Liposomes, New Systems and New Trends in Their Applications, Edition de Sante, Paris, 1995, pp. 615–643.
G. Cevc and G. Blume. Lipid vesicles penetrate into intact skin owing to the transdermal osmotic gradient hydration force. Biochim. Biophys. Acta. 1104:226–232 (1992).
H. Schreier and J. Bouwstra. Liposomes and niosomes as topical drug delivery carriers: dermal and transdermal drug delivery. J Contr. Rel. 30:1–15 (1994).
M. Šentjurc and V. Gabrijelčič. Transport of liposome-entrapped molecules into the skin as studied by electron paramagnetic resonance imaging methods. In D. D. Lasič, Y. Barenholz (eds.), Nonmedical Application of Liposomes, CRC Press, New York, 1996, pp. 91–114.
M. Šentjurc, K. Kočevar, and L. Honzak. Role of cholesterol in the transport of liposome encapsulated substances into skin. Prog. Drug Del. Sys. 5:157–160 (1996).
T. P. W. McMulen, P. N. H. A. Lewis, and R. N. McElhaney. Differential scanning calorimetric study of the effect of cholesterol on saturated phosphadidylcholines. Biochem. 32:516–522 (1993).
J. A. Rogers and T. Cheuk. Partial specific volumes of liposome systems. Chem. Phys. Lipids. 53:211–217 (1990).
V. Gabrijelčič, M. Šentjurc, and J. Kristl. Evaluation of liposomes as drug carriers into the skin by one-dimensional EPR imaging. Int. J. Pharm. 62:75–79 (1990).
V. Gabrijelčič, M. Šentjurc, and M. Schara. The measurement of liposome-entrapped molecule penetration into the skin: A 1DEPRI and EPR kinetic imaging study. Int. J. Pharm. 102:151–158 (1994).
O. H. Griffith and P. C. Jost. Lipid spin labels in biological membranes. In L. J. Berliner (ed.), Spin Labeling: Theory and Application, Academic Press, New York, 1976, pp. 347–372.
J. P. Slotte. Lateral domain formation in mixed monolayers containing cholestrol and dipalmitoylphosphatidylcholine or N-palmitoylsphingomyelin. Biochim. Biophys. Acta 1235:419–427 (1995).
J. Žel, J. Svetek, H. Černe, and M. Schara. Effects of aluminum on bilayer fluidity of the mycorrhizal fungus Amanita muscaria. Physiol. Plant. 89:172–176 (1993).
K. Vrhovnik, J. Kristl, M. Šentjurc, and J. Šmid-Korbar. Influence of liposome composition and size on the transport of encapsulated substances into the skin studied by EPR methods. Farm. Vestn. 48:324–325 (1997).
C. Michel, T. Purmann, E. Mentrup, E. Seiller, and J. Kreuter. Effect of liposomes on percutaneous penetration of lipophilic materials. Int. J. Pharm. 84:93–105 (1992).
M. Bloom. The physics of soft, natural materials. Physics in Canada 48:7–16 (1992).
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Vrhovnik, K., Kristl, J., Šentjurc, M. et al. Influence of Liposome Bilayer Fluidity on the Transport of Encapsulated Substance into the Skin as Evaluated by EPR. Pharm Res 15, 525–530 (1998). https://doi.org/10.1023/A:1011965423986
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DOI: https://doi.org/10.1023/A:1011965423986