Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes
Patent
1996-07-03
1997-06-10
Kishore, Gollamudi S.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Liposomes
424401, 424 43, 424 45, 264 41, 264 43, 514944, 514969, A61K 9127, A61K 700
Patent
active
056373180
DESCRIPTION:
BRIEF SUMMARY
The invention relates to a dermatological agent which penetrates into the dermal area of the skin and adjoining tissue and produces an improved supply of oxygen in this region.
U.S. Pat. No. 4,366,169 (White) claims the use of fluorocarbons for the treatment of skin injuries and wounds, in particular of burns. In this case the oxygen-containing fluorocarbon is put onto the skin, or onto appropriate dressings or similar means either directly or as an emulsion. U.S. Pat. No. 4569784 (Moore) describes the preparation of a gel with gas transport properties for use on the skin. The complicated process consists in emulsifying a water-immiscible organic liquid, e.g. a fluorocarbon, in the presence of an emulsifier by an emulsification process. A concentration process follows (e.g. ultra-centrifugation, ultrafiltration), which leads to the formation of a gel phase. In the third step which then follows, the separation of the clear liquid from the pasty solid (gel phase) is effected by decantation, filtration or evaporation. This gel is applied to the skin in suitable formulations, and it acts there without, however, penetrating the horny layer.
EP-A-296661 (Borgarello) describes a fluorocarbon-containing single phase system which can act as an isotropic or anisotropic formulation in the cosmetic field and also as a dermatological agent as an oxygen transporter. In this case, fluorocarbons having a maximum concentration of 50% are emulsified in water with perfluorinated emulsifiers of the alkanesulphonamide type in the presence of an aliphatic alcohol as an auxiliary emulsifier.
WO-A-08 459 describes a perfluorcarbon emulsion containing phospholipid vesicles as a blood substitute in which the phospholipid monomers are polymerised. In WO-A-91 00110, fluorcarbon emulsions containing phospholipids are disclosed in which the phospholipids has saturated carbon bonds. From WO-A-92 06676, oil-filled only slightly lamellar vesicles composed of phospholipids are known, whose structure corresponds to the customary vesicle structure. In the known processes described, the compositions described, which contain fluorocarbons, act on the skin in a system-related manner at the site of their application.
The present invention is based on the object of getting through the horny layer of the skin and the epidermis by penetration processes, in order to increase the oxygen concentration in the dermal area and the tissue adjoining it and to activate metabolic processes.
According to the invention, the dermatological agent for assisting the transport of oxygen in the skin consists of asymmetric lamellar aggregates which are constructed from phospholipids laving a phosphatidylcholine content of 30 to 99% by weight which in their core, in contrast to the well-known aqueous lipisomes, contain fluorocarbons or mixtures thereof. The dermatological agent according to the invention thus consists of asymmetric lamellar aggregates which consist of phospholipids having a phosphatidylcholine content of 30 to 99% by weight and oxygen-laden fluorocarbon or fluorocarbon mixture, the amount of fluorocarbon being in the range from 1 to 100% w/v (w/v=weight/volume), in a carrier which is suitable for dermatological use.
The lamellar aggregates are able, because of their phospholipid structure, which is structurally and chemically very similar or is partly identical to the cell membranes, and in combination with their aggregate size, which can be controlled during preparation, to penetrate into deeper-lying skin layers and to become active there. This takes place in contrast to the invention descriptions mentioned in the prior art, which do not permit the transport of the fluorocarbons into deeper-lying regions of the skin. The known processes are ineffective in respect of the claimed effect.
A plurality of fluorocarbons can be employed, e.g. aliphatic straight-chain and branched fluoroalkanes, mono- or bicyclic and optionally fluoroalkyl-substituted fluorocycloalkanes, perfluorinated aliphatic or bicyclic amines, bis(perfluoroalkyl)ethenes or mixtures the
REFERENCES:
patent: 4366169 (1982-12-01), White
patent: 4569784 (1986-02-01), Moore
patent: 5061484 (1991-10-01), Heldebrant
patent: 5160669 (1992-11-01), Wallach et al.
patent: 5204112 (1993-04-01), Hope
patent: 5219538 (1993-06-01), Henderson
patent: 5246703 (1993-09-01), Durfee
Lautenschlager in cosmetics & toiletries 105, May 1990.
Gross Udo
Roding Joachim
Stanzl Klaus
Zastrow Leonhard
Kishore Gollamudi S.
Lancaster Group AG
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