Abstract
Liposomes were studied as a drug delivery system. Multilamellar vesicles, small unilamellar vesicles and large unilamellar vesicles containing cytarabine were prepared using egg yolk lecithin and cholesterol. Large unilamellar vesicles showed the highest encapsulation efficiency of all and their encapsulation efficiency increased as the buffer volume decreased. Cholesterol increased the stability of liposomal drug products as drug carriers and reduced the permeability of drug across the liposomal membrane. The release rate of cytarabine increased with incubation temperature and decreased with cholesterol incorporation in liposomal membrane. The release mechanism of cytarabine from large unilamellar vesicles in vitro was chiefly due to simple diffusion across the liposomal membrane rather than liposomal rupture.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
Literature Cited
Kurosaki, Y., Kimura, T., Muranishi, S. and Sezaki, H.: The use of liposomes as enzyme carriers: dependence of enzyme stability on the method of preparation.Chem. Pharm. Bull.,29, 1175 (1981).
Finkelstein, M.C., Maniscalco, J. and Weissmann, G.: Entrapment of soy bean trypsin inhibitor and antitrypsin by multilamellar liposomes.Anal. Biochem.,89, 400 (1978).
Gregoriadis, G., Neerunjun, E.D. and Hunt, R.: Fate of a liposome associated agent induced into normal and tumor-bearing rodents. Attempts to improved localization in tumor tissues.Life Science.21, 357 (1977).
Souhami, R.L.: The effect of colloidal carbons on the organ distribution of sheep red cells and the immune response.Immunology,22, 685 (1972).
Gregoriadis, G. and Neerunjun, D.E.: Control of the rate of hepatic uptake and catabolism of liposome-entrapped proteins injected into rats. Possible therapeutic applications.Eur. J. Biochem.,47, 179 (1974).
Widder, K.J., Senyei, A.E. and Sears, B.: Experimental methods in cancer therapeutics.J.P.S.,71, 379 (1982).
Szoka, F.Jr.: Comparative property and methods of preparation of lipid vesicles.Ann. Rev. Biophys. Bioenz.,9, 467 (1980).
Szoka, F.Jr. and Papahajopoulos, D.: Procedure for preparation of liposomes with large internal aqueous space and high capture by reverse-phase evaporation.Proc. Natl. Acad. Sci. U.S.,75, 4194 (1978).
Szoka, F., Olson, F., Heath, T., Vail, W., Mayhew, E. and Papahajopoulos, D.: Preparation of unilamellar liposomes of intermediate size (0.1–0.2 μm) by a combination of reverse phase evaporation and extrusion through polycarbonate membranes.B.B.A.,601, 559 (1980).
Rigaud, J.L., Bluzat, A. and Buschlen, S.: Incorporation of bacteriorhodopsin into large unilamellar liposomes by reverse phase evaporation.Biochem. Biophys. Res. Commun.,111, 373 (1983).
Kirby, C., Clarke, J. and Gregoriadis, G.: Effect of cholesterol content of small unilamellar liposomes on their stability in vivo and in vitro.Biochem. J.,186, 591 (1980).
Gregoriadis, G. and Davis, C.: Stability of liposomes in vivo and in vitro is promoted by their cholesterol content and the presence of blood cells.Biochem. Biophys. Res. Commun.,89, 1287 (1979).
Degier, J., Mandersloot, J.D. and Van Deenen, L.L.M.: Lipid composition and permeability of liposomes.B.B.A.,150, 666–675 (1968)>
Regan, S.L., Singh, A., Oehme, G.: Polymerized phosphatidylcholine vesicles. Stabilized and controllable time-release carriers.Biochem. Biophys. Res. Commun.,101, 131 (1981)>
Johnston, D.S., Sanphera, S., Pons, M. and chapmman, D.: Phospholipid polymer-synthesis and spectral characteristics.B.B.A.,602, 57 (1980).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Kim, CK., Park, DK. Stability and drug release properties of liposomes containing cytarabine as a drug carrier. Arch. Pharm. Res. 10, 75–79 (1987). https://doi.org/10.1007/BF02857770
Received:
Issue Date:
DOI: https://doi.org/10.1007/BF02857770