Blood-stable, cholesterol-free liposomes

Details Blood-stable, cholesterol-free liposomes Blood-stable, cholesterol-free liposomes

1989-01-17

1991-08-27

Lovering, Richard D.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

264 41, 264 46, 4284022, 424450, 436829, 514970, 514971, A61K 9133, B01J 1302

Patent

active

050431641

ABSTRACT:
Small unilamellar liposomes (d<600 nm) comprising an unsaturated phosphatidylethanolamine (PE) such as dioleoyl PE (DOPE) and a fatty acid such as oleic acid (OA) are stabilized by adding to a freshly prepared liposome suspension, an amphipile which has a high tendency to form micelles. Examples are shown for the following micelle-forming amphiphiles: lysophospholipide, gangliosides (GM.sub.1 and GTlb), sulfatide, synthetic glycopholipids such as sialo-lactosyl phosphatidylethanolamine, liopohilic drugs such as cytosine arabinoside diphosphate diacyglycerol, and proteins such as cytochrome b.sub.5, human high density lipoprotein (HDL), and human glycophorin A. The stabilized liposomes are resistant to the lytic action of albumin, the major blood component which causes the lysis of this type of liposome. Prior to the present invention, liposomes comprising PE and OA were typically stabilized by the incorporation of cholesterol.

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