Liposomes with enhanced retention on mucosal tissue

Details Liposomes with enhanced retention on mucosal tissue Liposomes with enhanced retention on mucosal tissue

1986-07-28

1989-06-13

Lovering, Richard D.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Liposomes

264 43, 424 11, 424427, 424428, 4284022, 436829, 514912, 514914, 514966, A61K 3722, A61K 966, B01J 1302

Patent

active

048391751

ABSTRACT:
A liposome composition designed for enhanced binding to mucosal tissue, The liposomes contain about 10-40 mole percent of an amine-derivatized lipid component in which a charged amine group is spaced from a lipid polar head region by a carbon-containing spacer arm at least 3 atoms in length. The liposomes preferably have a close packed lipid structure produced by inclusion of between 20-50 mole percent of cholesterol or an amine-derivatized cholesterol, and/or phospholipids with predominantly saturated acyl chain moieties. For ophthalmic use, the liposomes may be suspended in an aqueous medium containing a high-viscosity polymer, to enhance further the retention of liposomes on a corneal surface.

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patent: 4544545 (1985-10-01), Ryan et al.
patent: 4619913 (1986-10-01), Luck et al.
M. S. Wu, J. C. Robbins, R. L. Bugianesi et al. titled: Modified in vivo Behavior of Liposomes Containing Synthetic Glycolipids, Bio. Biophysica Acta, 674, (1981), 19-29, Elsevier North-Holland Biomedical Press.
Toshiyuki Nagata, Hansjorg Eibl and Georg Melchers, Fusion of Plant Protoplasts Induced by a Positively Charged Synthetic Phospholipid, pp. 460-462, 0341-0382/79/0500-0460 $01.00/0.
M. M. Ponpipom, T. Y. Shen, J. D. Baldeschwieler, and Po-Shun Wu, titled: Modification of Liposome Surface Properties by Synthetic Glycolipids, (Chapter 7), vol. III, pp. 95-115, Lipsome Technology.
M. R. Mauk, R. C. Gamble and J. D. Baldeschwieler, Titled: Targeting of Lipid Vesicles: Specificity of Carbohydrate Receptor Analogues for Leukocytes in Mice. Prc.: Natl. Acad. Sci. U.S.A., vol. 77, No. 8, pp. 4430-4434, Aug. 1980, Biochemistry.
H. E. Schaeffer and D. L. Krohn. Titled: Liposomes in Topical Drug Delivery, pp. 220-227, Invest. Ophthalmol. Vis. Sci., Feb. 1982, 0146-0404/82/020220.

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