Abstract 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.
A doxorubicin-containing liposome composition comprising liposomes containing phosphatidylglycerol:phosphatidylcholine:cholesterol in a mole ratio of 3:7:4 and 1.5 mole percent alpha-tocopherol, doxorubicin entrapped in the lipid bilayer region of the liposomes, and ferrioxamine at a concentration of 50 μm.
Claim 2
Dependent Claim
37 words
A doxorubicin-containing liposome composition comprising liposomes containing phosphatidylglycerol:phosphatidylcholine:cholesterol in a mole ratio of 3:7:4 and 1.5 mole percent alpha-tocopherol, doxorubicin entrapped in the lipid bilayer region of the liposomes, and ferrioxamine at a concentration of 50 μm.
Claim 3
Dependent Claim
26 words
The composition of claim 1, wherein the liposomes are in an aqueous suspension and ferrioxamine is present in substantially equal concentrations inside and outside the liposomes.
Claim 4
Dependent Claim
18 words
The composition of claim 2, wherein the liposomes are predominantly between about 0.05 and 0.2 microns in size.
Claim 5
Dependent Claim
26 words
The composition of claim 1, wherein the liposomes are in a aqueous suspension and the drug is present in the liposomes in a substantially saturating amount.
Claim 6
Dependent Claim
18 words
The composition of claim 4, which has been treated to remove free drug not associated with the liposomes.