Components for producing amphoteric liposomes

An amphoteric lipid, which lipid has an isoelectric point between 4.5 and 8.5, according to general formula (I):

• Amphoteric substance-Y-spacer-amphiphilic substance (I)
• characterized in that
• (a) the amphoteric substance has at least one portion of cationic charge with a pKa value between 4 and 8 and/or at least one portion of anionic charge with a pKa value between 3 and 7 and optionally additional charge carriers,
• aa) said portion of cationic charge being selected from the group comprising imidazole, morpholine, piperazine, purine, pyridine and/or pyrimidine or derivatives thereof,
• bb) said portion of anionic charge being a carboxyl group which comprises acetic acid, bromoacetic acid, chloroacetic acid, acetoacetic acid, propionic acid, acrylic acid, butyric acid, crotonic acid, or carboxylic acids bound in the aliphatic chain which comprises dicarboxylic acids that are mono-esterified or amidated or bound in the aliphatic chain;
• which comprises oligocarboxylic acids that are mono-esterified or amidated or bound in the aliphatic chain,
• (b) the spacer is a lower alkyl residue with up to 8 C atoms, with linear, branched or cyclic structure, with 0, 1 or 2 ethylenically unsaturated bonds, and 0-4 hydroxyl groups,
• (c) Y comprises —(C═O)—O—;
• —(C═O)—NH—;
• —NH—(C═O)—O—;
• —O—:
• —NH—;
• —CH═N—;
• —O—(O═C)—;
• —S—;
• —(O═C)—;
• —NH—(O═C)—;
• —O—(O═C)—NH—, —N═CH— and/or —S—S—,
• (d) the amphiphilic substance is a structure according to general formula (II) or (III) or (IV):
• wherein
• R1 and R2 independently are C8-C30 alkyl or acyl chains with 0, 1 or 2 ethylenically unsaturated bonds, and
• X is selected from the group comprising —O—(C═O);
• —NH—(C═O)—;
• —S—(C═O)—;
• —O—;
• —NH—;
• —S—;
• —N═CH—;
• —(O═C)—O—;
• —S—(O═C)—;
• —NH—(O═C)—;
• —N═CH— and/or —S—S—;
• or
• wherein
• R1 and R2 independently are C8-C30 acyl chains with 0, 1 or 2 ethylenically unsaturated bonds, and X is —O—;
• or
• wherein
• R1 and R2 independently are C8-C30 alkyl chains with 0, 1 or 2 ethylenically unsaturated bonds, and
• X is absent or selected from the group consisting of —(C═O)—O—;
• —(C═O)—NH—;
• —(C═O)—S—;
• —NH—;
• —CH═N—;
• and/or —S—(O═C)—;
• (e) the amphiphilic substance is a 1,4- or 1,5-dicarboxylic acid such as aspartic acid, glutamic acid, malic acid, tartaric acid, citric acid, aconitic acid, citraconic acid and/or maleic acid esterified with linear C8-C30 alcohols, and/or
• (f) the amphiphilic substance is a 1,4- or 1,5-diamine of 3-aminoalanine, diaminobutyric acid, ornithine, or lysine amidated with linear C8-C30 fatty acids;
• and liposomes thereof.