O/W lipid emulsions for parenteral drug delivery. III. Lipophilicity necessary for incorporation in oil particles even after intravenous injection

Journal of Drug Targeting

Volumn 6, Issue 2, 1998, Pages 119-127

  Sakaeda, Toshiyuki ^a   Hirano, Koichiro ^a  

^a SHIONOGI AND CO LTD   (Japan)

Author keywords

Drug delivery system; Lipophilic drug; O W lipid emulsion; Partition coefficient

Indexed keywords

DEXTRAN SULFATE; LIPID EMULSION; MENATETRENONE; OCTANOL; OIL; PHOSPHOLIPID; SOYBEAN OIL; SUDAN II; TRIACYLGLYCEROL; UNCLASSIFIED DRUG; WATER;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG DELIVERY SYSTEM; DRUG DISTRIBUTION; DRUG RELEASE; INTRAVENOUS DRUG ADMINISTRATION; LIGHT SCATTERING; LIPOPHILICITY; LIVER; LUNG; MALE; MICELLE; NONHUMAN; PARTICLE SIZE; PARTITION COEFFICIENT; PHOSPHOLIPID BLOOD LEVEL; PLASMA CLEARANCE; PRIORITY JOURNAL; RAT; RETICULOENDOTHELIAL SYSTEM; SPLEEN; TIME; TRIACYLGLYCEROL BLOOD LEVEL;

EID: 0032437204     PISSN: 1061186X     EISSN: None     Source Type: Journal    
DOI: 10.3109/10611869808997887     Document Type: Article

References (29)

1. Collins-Gold, L.C., Lyons, R.T. and Bartholow, L.C. (1990). "Parenteral emulsions for drug delivery", Adv. Drug Delivery Rev., 5, 189-208.
2. Davis, S.S., Hadgraft, J. and Palin, K.J. (1985). "Medical and pharmaceutical applications of emulsions", In Becher, P. (ed.), Encyclopedia of Emulsion Technology (Marcel Dekker, New York), pp. 159-238.
3. Davis, S.S., Washington, C., West, P., Illum, L., Liversidge, G., Sternson, L. and Kirsh, R. (1987). "Lipid emulsions as drug delivery systems", Ann. N.Y. Acad. Sci., 507, 75-88.
4. Davis, S.S., Illum, L., Moghimi, S.M., Davies, M.C., Porter, C.J.H., Muir, I.S., Brindley, A., Christy, N.M., Norman, M.E., Williams, P. and Dunn, S.E. (1993). "Microspheres for targeting drugs to specific body sites", J. Controlled Release, 24, 157-163.
5. Hansch, C., Leo, A., Unger, S.H., Kim, K.H., Nikaitani, D. and Lien, E.J. (1973). "Aromatic substituent constants for structure-activity correlations", J. Med. Chem., 16, 1207-1216.
6. Heeg, J.F., Miser, M.F., Satonin, D.K. and Rose, J.Q. (1984). "Pharmacokinetics of probucol in male rats", J. Pharm. Sci., 73, 1758-1763.
7. 1 and the application of them to lipid microsphere (LM) preparations", Jpn. J. Inflamm., 8, 243-246.
8. Iriyama, K. (1996). "The metabolic distinctiveness of emulsified lipid particles in the bloodstream and its clinical implications", Surg. Today, 26, 673-678.
9. Kakutani, T., Nishihara, Y., Takahashi, K. and Hirano, K. (1991). "O/W lipid microemulsion for parenteral drug delivery", Proc. Int. Symp. Control Rel. Bioact. Mater., 18, 359-360.
10. Kurihara, A., Shibayama, Y., Yasuno, A., Ikeda, M. and Hisaoka, M. (1996a). "Lipid emulsions of palmitoylrhizoxin: effects of particle size on blood dispositions of emulsion lipid and incorporated compound in rats", Biopharm. Drug Dispos., 17, 343-353.
11. Kurihara, A., Shibayama, Y., Mizota, A., Yasuno, A., Ikeda, M. and Hisaoka, M. (1996b). "Pharmacokinetics of highly lipophilic antitumor agent palmitoyl rhizoxin incorporated in lipid emulsions in rats", Biol. Pharm. Bull., 19, 252-258.
12. Leo, A., Jow, P.Y.C., Silipo, C. and Hansch, C. (1975). "Calculation of hydrophobic constant (log P) from π and f constants", J. Med. Chem., 18, 865-868.
13. Mizushima, Y. (1991). "Lipo-prostaglandin preparations", Prostagl. Leukotr. Essent. Fatty Acids, 42, 1-6.
14. Mizushima, Y., Shoji, Y., Kato, T., Fukushima, M. and Kurozumi, S. (1986). "Use of lipid microspheres as a drug carrier for antitumor drugs", J. Pharm. Pharmacol., 38, 132-134.
15. Mizushima, Y., Igarashi, R., Hoshi, K., Sim, A.K., Cleland, M.E., Hayashi, H. and Goto, J. (1987). "Marked enhancement in antithrombotic activity of isocarbacyclin following its incorporation into lipid microspheres", Prostaglandins, 33, 161-168.
16. Moghimi, S.M., Porter, C.J.H., Muir, I.S., Illum, L. and Davis, S.S. (1991). "Non-phagocytic uptake of intravenously injected microspheres in rat spleen: influence of particle size and hydrophilic coating", Biochem. Biophys. Res. Commun., 177, 861-866.
17. Moghimi, S.M. and Davis, S.S. (1994). "Innovations in avoiding particle clearance from blood by Kupffer cells: cause for reflection", Crit. Rev. Ther. Drug Carrier Systems, 11, 31-59.
18. Oku, N. and Namba, Y. (1994). "Long-circulating liposomes", Crit. Rev. Ther. Drug Carrier Systems, 11, 231-270.
19. Patel, K.R., Li, M.P. and Baldeschwieler, J.D. (1983). "Suppression of liver uptake of liposomes by dextran sulfate 500", Proc. Natl. Acad. Sci. USA, 80, 6518-6522.
20. Prankerd, R.J. and Stella, V.J. (1990). "The use of oil-in-water emulsions as a vehicle for parenteral drug administation", J. Parent. Sci. Technol., 44, 139-149.
21. Sakaeda (nee Kakutani), T., Takahashi, K., Nishihara, Y. and Hirano, K. (1994). "O/W lipid emulsions for parenteral drug delivery. I. Pharmacokinetics of the oil particles and incorporated sudan II", Biol. Pharm. Bull., 17, 1490-1495.
22. Sakaeda (nee Kakutani), T. and Hirano, K. (1995). "O/W lipid emulsions for parenteral drug delivery. II. Effect of composition on pharmacokinetics of incorporated drug", J. Drug Targeting, 3, 221-230.
23. Singh, M. and Ravin, L.J. (1986). "Parenteral emulsions as drug carrier systems", J. Parent. Sci. Technol., 40, 34-41.
24. Souhami, R.L., Patel, H.M. and Ryman, B.E. (1981). "The effect of reticuloendothelial blockade on the blood clearance and tissue distribution of liposomes", Biochim. Biophys. Acta, 674, 354-371.
25. Takino, T., Konishi, K., Takakura, Y. and Hashida, M. (1994). "Long circulating emulsion carrier systems for highly lipophilic drugs", Biol. Pharm. Bull., 17, 121-125.
26. Washington, C. and Evans, K. (1995). "Release rate measurements of model hydrophobic solutes from submicron triglyceride emulsions", J. Controlled Release, 33, 383-390.
27. Xu, R. (1996). "Particle size distribution analysis using light scattering", In Knapp, J.Z., Barber, T.A. and Lieberman, A. (eds.), Liquid- and Surface-borne Particle Measurement Handbook (Marcel Dekker, New York), pp. 745-777.
28. Yamaguchi, T. and Mizushima, Y. (1994). "Lipid microspheres for drug delivery from the pharmaceutical viewpoint", Crit. Rev. Ther. Drug Carrier Systems, 11, 215-229.
29. Yamaoka, K., Tanigawara, Y., Nakagawa, T. and Uno, T. (1981). "A pharmacokinetic analysis program (MULTI) for microcomputer", J. Pharmacobio-Dyn., 4, 879-885.