Cardiolipin molecules and method of synthesis

Abstract

The present invention provides a new synthesis route for cardiolipin, especially short-chain cardiolipin, having different fatty acids and / or alkyl chains of different chain lengths, with or without unsaturation. The method comprises: reacting 1,2-O-sn-diacyl / 1,2-O-sn-dialkylglycerol or 2-O-protected glycerol with phosphoramidite reagent or phosphotriester to generate protected Cardiolipin, which is deprotected to prepare short-chain cardiolipin. This reaction scheme can be used to generate new variants of cardiolipin. Cardiolipin prepared by this method may be contained in liposomes, which may also contain active agents, such as hydrophobic or hydrophilic drugs. Such liposomes may be used in the treatment of diseases or in diagnostic and / or analytical assays. Liposomes can also contain ligands for targeting to specific cell types or specific tissues.

Description

field of invention

[0001] The present invention relates to novel synthetic methods for the preparation of cardiolipin analogs / variants and compositions containing them. The invention also relates to liposomal formulations or complexes or emulsions containing active agents or drugs and their use in the treatment of human and animal diseases. Background of the invention

[0002] Liposome formulations have the ability to increase the solubility of hydrophobic drugs in aqueous solutions. They often reduce side effects associated with drug therapy and provide a resilient tool for developing new formulations of active agents.

[0003] Liposomes are generally prepared from natural phospholipids, such as phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylglycerol, phosphatidic acid and phosphatidylinositol. Anionic phospholipids, such as phosphatidylglycerol and cardiolipin, can be added to create a net negative surface charge which provides colloidal s...

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