Bdellosomes

A monomolecular solid particle for transportation of hydrophobic or hydrophobed active substances obtainable by a process, in which an unbranched or at most triple-branched polymer backbone composed of monomers having at least one bonding group (x) on each monomer is brought into contact with

• a) chain-forming side-chain monomers each of which has at least one bonding group (y) and at least one bonding group (x′), where (x′) is a group capable of forming a a covalent bond both with (x) and with (y),
• b) a mixture of chain-forming side-chain monomers, of which at least one monomer has at least two bonding groups (y) and, on at least one different monomer, at least two bonding groups (x′), where (x′) is a group which can form a covalent bond both with (x) and with (y), or
• c) a mixture of chain-forming side-chain monomers, of which at least one monomer has at least two bonding groups (y), at least one different monomer has at least two bonding groups (x′) and at least one other monomer has at least one bonding group (y) and at least one bonding group (x′), where (x′) is a group which can form a covalent bond both with (x) and with (y),
• and also at least one side-chain terminator having at least one bonding group (y′), no bonding group (y), and at least one free group (z) optionally provided with a protective group, where (y′) is a group which can form a covalent bond with (y),
• under conditions permitting bonding between the monomers or monomer mixtures of the side chains and the polymer backbone and the chain terminators and also permitting polycondensation of the monomers or monomer mixtures in the side chains, characterized in that
• the molar ratio of the monomers in the molecular side chains (b) to the side-chain terminators (c) is >>1,
• group y≠group z and group x′≠group z,
• the molar ratio of the monomers in the molecular backbone to the side-chain terminators (c) is approximately equimolar
• x, x′, y, and y′ are independently selected from the group comprising OH, SH, COOH, or NH2 with the proviso that x/x′, x′/y, or y/y′ form corresponding bond pairs x/x′, x′/y, or y/y′ (with the corresponding bond) selected from the group comprising OH/COOH (ester bond —O—C(O)—), NH2/COOH (amide linkage —NH—C(O)—), SH/COOH (thioester bond —S—C(O)—), COOH/OH (ester bond —O—C(O)—), COOH/NH2 (amide linkage —NH—C(O)—) or COOH/SH (thioester bond S—C(O)—),
• z is selected from the group comprising CH3, OH, SH, COOH, NH2, and the vinyl or epoxide group, optionally protected by a protective group, and
• the side-chain monomers can be used in the form of pure monomers or derivatives such as inner anhydrides or lactones, provided they are still capable of forming chains with themselves and/or with other side-chain monomers.

A monomolecular solid particle for transportation of hydrophobic or hydrophobed active substances obtainable by a process, in which an unbranched or at most triple-branched polymer backbone composed of monomers having at least one bonding group (x) on each monomer is brought into contact with

• polycondensed molecular side chains composed of monomers, of which each monomer has at least one bonding group (y) and at least one bonding group (x′), or composed of different monomers, of which one monomer has at least two bonding groups (y) and a different monomer has at least two bonding groups (x′), or composed of different monomers, of which one monomer has at least two bonding groups (y), a different monomer has at least two bonding groups (x′), and another monomer has at least one bonding group (y) and at least one bonding group (x′), where (x′) is a group which can form a covalent bond both with (x) and with (y), in which side-chain terminators are covalently bonded to the end of each of the molecular side chains via a (y)-(y′) bond, which terminators have at least one bonding group (y′), no bonding group (y) and at least one free group (z) optionally provided with a protective group, where (y′) is a group which can form a covalent bond with (y), under conditions which allow for linkage between the polycondensed molecular side chains and the polymer, characterized in that
• the molar ratio of the monomers in the molecular side chains (b) to the side-chain terminators (c) is >>1,
• group y≠group z and group x′≠group z,
• the molar ratio of the monomers in the molecular backbone to the side-chain terminators (c) is approximately equimolar
• x, x′, y, and y′ are independently selected from the group comprising OH, SH, COOH, and NH2 with the proviso that x/x′, x/y, or y/y′ form corresponding bond pairs x/x′, x′/y, or y/y′ (with the corresponding bond) selected from the group comprising OH/COOH (ester bond —O—C(O)—), NH2/COOH (amide linkage —NH—C(O)—), SH/COOH (thioester bond —S—C(O)—), COOH/OH (ester bond —O—C(O)—), COOH/NH2 (amide linkage —NH—C(O)—) or COOH/SH (thioester bond S—C(O)—) and
• z is selected from the group comprising CH3, OH, SH, COOH, and NH2, and also the vinyl or epoxide group optionally protected by a protective group.

A solid particles for transportation of hydrophobic or hydrophobed pharmaceutically active substances, synthesized by a process comprising the following steps:

• (a) preparation of a solution in an organic solvent or a mixture of organic solvents containing at least one hydrophobic or hydrophobed pharmaceutically active substance, water-insoluble organic polymeric material and amphiphilic organic polymeric material, and optionally supplementary substances,
• (b) treatment of the solution with supersonics,
• (c) dialysis of the solution against H2O
• (d) separation of the resulting particles from the resulting aqueous solution.