Complexing agents for compositions containing inclusion complexes

A method of preparing a composition comprising a therapeutic agent and an inclusion complex of a cyclodextrin-containing polymer and a complexing agent of the formula:

• wherein
• Host/Guest is a guest moiety;
• J is —NH—, —C(═O)NH—(CH2)d—, —NH—C(═O)—(CH2)d—, —CH2SS—, —C(═O)O—(CH2)e—O—P(═O)(O—(CH2)e—Y)O—,
• a peptide or polypeptide residue, or
• —NH—(C═O)—CH(R1)—NH—(C═O)—CH(R1)—NH—;
• Y is an additional host-guest functionality;
• R1 is —(CH2)—CO2H, an ester or salt thereof;
• or —(CH2)a—CONH2;
• PEG is —O(CH2CH2O)z—, where z varies from 2 to 500;
• L is —NH—, —NH—(C═O)—(CH2)e—(C═O)—CH2—, —S(═O)2—HC═CH—, —SS—, —C(═O)O—, or a carbohydrate residue;
• a is 0 or 1;
• b is 0 or 1;
• d ranges from 0 to 6;
• e ranges from 1 to 6;
• m is 1;
• n ranges from 1 to 6;
• q is 1;
• w ranges from 1 to 5;
• y is 1;
• and
• x is 1,
• said method comprising:
• combining the cyclodextrin-containing polymer, the complexing agent and the therapeutic agent, thereby forming the composition.

A method of treating a patient comprising administering to the patient a therapeutically effective amount of a composition comprising a therapeutic agent and an inclusion complex of a cyclodextrin-containing polymer and a complexing agent of the formula:

• wherein
• Host/Guest is a guest moiety;
• J is —NH—, —C(═O)NH—(CH2)d—, —NH—C(═O)—(CH2)d—, —CH2SS—, —C(═O)O—(CH2)e—O—P(═O)(O—(CH2)e—Y)O—,
• a peptide or polypeptide residue, or —NH—(C═O)—CH(R1)—NH—(C═O)—CH(R1)—NH—;
• Y is an additional host-guest functionality;
• R1 is —(CH2)—CO2H, an ester or salt thereof;
• or —(CH2)a—CONH2;
• PEG is —O(CH2CH2O)z—, where z varies from 2 to 500;
• L is —NH—, —NH—(C═O)—(CH2)e—(C═O)—CH2—, —S(═O)2—HC═CH—, —SS—, —C(═O)O—, or a carbohydrate residue;
• a is 0 or 1;
• b is 0 or 1;
• d ranges from 0 to 6;
• e ranges from 1 to 6;
• m is 1;
• n ranges from 1 to 6;
• q is 1;
• w ranges from 1 to 5;
• y is 1;
• and
• x is 1.