Funktionell aktive Fusionspeptide enthaltende synthetische Membranvesikeln als Arzneistoffabgabesysteme

• Main Authors: GLUECK, REINHARD., CH-3028 SPIEGEL BEI BERN, CH, HERRMANN, PETER., CH-4410 LIESTAL, CH, KLEIN, PETER, CH-4438 LANGENBRUCK, CH
• Format: Patent
• Language: German
• Published: 01.02.1996
• Edition: 6
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The phospholipid bi-layer vesicle contains at least one pharmaceutically active drug and comprises cell-specific markers on the membrane which have at least 90 % biological activity when measured according to Luescher & Glueck, Antiviral Research 14, 39-50. In the membrane, the cholesterol content is preferably less than 2% by weight, the detergent content preferably less than 1 ppb. The vesicle diameter preferably is about 80 nm. The phospholipid in the membrane may comprise 70 to 95 % by weight of phosphatidylcholine and preferably 10 to 20 % by weight of phosphatidylethanolamine; preferably 6 to 8 % by weight of a crosslinker, preferably of a sulfosuccinimidyl derivate, and at least one cell-specific fusion peptide are linked to the membrane. The vesicles are used for the preparation of pharmaceuticals against AIDS and carcinomas. The process for the preparation of phospholipid bi-layer vesicles comprises hemagglutinin as a cell-specific marker with at least one fusion peptide. The hemagglutinin is separated from a virus strain by means of a non-ionic detergent, preferably octaethylene glycol monododecyl ether. It is removed by repeatedly treating the solution with altogether about 1.5 g polystyrene beaded microcarriers per 100 mg detergent.