Liposomes containing a cisplatin compound
First Claim
1. A liposomal composition containing an entrapped cisplatin compound, comprisingliposomes having an outer surface and an inner surface defining an aqueous liposome compartment, and being composed of a vesicle-forming lipid and between about 1-20 mole percent of a vesicle-forming lipid derivatized with a hydrophilic polymer having an uncharged end cap, said liposomes being formed such that the hydrophilic polymer forms a coating of hydrophilic polymer chains on both said inner and outer surfaces, andthe cisplatin compound entrapped in said liposomes, said compound remaining entrapped in the liposomes in its native form with substantially greater retention when compared to liposomes lacking said polymer coating.
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Abstract
A liposome composition containing an entrapped cisplatin compound is described. The liposomes have a surface coating of hydrophilic polymer chains on inner and outer surfaces and an entrapped cisplatin compound. The compound is entrapped with substantially greater retention in the liposomes, when compared to liposomes lacking the polymer coating. A method of preparing the composition is also described.
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Citations
14 Claims
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1. A liposomal composition containing an entrapped cisplatin compound, comprising
liposomes having an outer surface and an inner surface defining an aqueous liposome compartment, and being composed of a vesicle-forming lipid and between about 1-20 mole percent of a vesicle-forming lipid derivatized with a hydrophilic polymer having an uncharged end cap, said liposomes being formed such that the hydrophilic polymer forms a coating of hydrophilic polymer chains on both said inner and outer surfaces, and the cisplatin compound entrapped in said liposomes, said compound remaining entrapped in the liposomes in its native form with substantially greater retention when compared to liposomes lacking said polymer coating.
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10. A method of entrapping a cisplatin compound in liposomes, comprising
heating an aqueous solution of a cisplatin compound to a temperature sufficient to increase its solubility at least two-fold over the compound'"'"'s solubility at room temperature; -
adding to the heated solution a vesicle-forming lipid and between about 1-20 mole percent of a vesicle-forming lipid derivatized with a hydrophilic polymer having an uncharged end cap; and by said adding, forming liposomes having an inner surface coating and an outer surface coating of said hydrophilic polymer and said cisplatin compound remaining entrapped in the liposomes in its native form with substantially greater retention than in liposomes lacking said inner and outer surface coating. - View Dependent Claims (11, 12, 13, 14)
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Specification