초록 ▼

A drug/liposome composition comprising an aqueous suspension of liposomes and, entrapped in the lipid bilayer region of the liposomes, an anthraquinone drug containing quinone and hydroquinone functionalities on adjacent anthracene rings. An iron-specific trihydroxamic chelating agent contained in t

A drug/liposome composition comprising an aqueous suspension of liposomes and, entrapped in the lipid bilayer region of the liposomes, an anthraquinone drug containing quinone and hydroquinone functionalities on adjacent anthracene rings. An iron-specific trihydroxamic chelating agent contained in the bulk aqueous phase of the suspension and a lipophilic free-radical scavenger contained in the bilayer region of the liposome cooperate to reduce chemical modification of both drug and lipid components of the composition. A preferred composition containing doxorubicin and alpha-tocopherol entrapped in the liposomes, and ferrioxamine in the aqueous suspension phase is effective in treating human neoplasms, with significantly reduced side effects over those produced by free-drug administration.

대표청구항 ▼

A method of treating liver neoplasms in a human patient with at least the same extent of therapeutic effectiveness, but with substantially reduced incidence of alopecia and nausea with respect to that produced by treatment with doxorubicin in free form, comprising preparing, for parenteral administr

A method of treating liver neoplasms in a human patient with at least the same extent of therapeutic effectiveness, but with substantially reduced incidence of alopecia and nausea with respect to that produced by treatment with doxorubicin in free form, comprising preparing, for parenteral administration, an aqueous suspension of liposomes (i) whose lipid bilayer region contains at least about 2.5 mole percent of doxorubicin or a pharmacologically acceptable salt thereof, and (ii) which are sized to allow for sterilization by filtration through a 0.45 micron pore size membrane, and which suspension contains less than about 20% doxorubicin in free-drug form; and parenterally administering a pharmacologically acceptable amount of the suspension to the patient.