pH-sensitive polymeric micelles for drug delivery
AssigneeUniversity of Utah Research Foundation
InventorsDongin Kim, Zhonggao Gao, Eun Seong Lee, You Han Bae
Life of this patent
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Abstract
Mixed micelles containing poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer are a pH-sensitive drug carrier that release the drug in an acidic microenvironment, but not in the blood. Since the microenvironment of solid tumors is acidic, these mixed micelles are useful for treating cancer, including those cancers exhibiting multidrug resistance. Targeting ligands, such as folate, can also be attached to the mixed micelles for enhancing drug delivery into cells. Methods of treating a warm-blooded animal with such a drug are disclosed.
Claims19
A composition comprising poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer with a folate residue covalently bonded to the poly(ethylene glycol) portion.
A composition comprising poly(L-histidine-co-phenylalanine)-poly(ethylene glycol)block copolymer wherein a poly(ethylene glycol) block portion having a free end further comprises a targeting moiety that permits binding to a receptor on the surfaces of cells coupled to the free end.
A pH-sensitive mixed polymeric micelle composition comprising
- (a) poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer, or
- (b) poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer-folate and poly(L-lactic acid)-poly(ethylene glycol) block copolymer, or
- (c) poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer-folate, or
- (d) poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer-folate and poly(L-lactic acid)-poly(ethylene glycol) block copolymer-folate.
A method of treating cancer in a warm-blooded animal, the method comprising administering into the systemic circulation of the animal a drug-loaded mixed micelle composition comprising a mixture of a hydrophobic anticancer drug and pH-sensitive mixed polymeric micelles comprising
- (a) poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer, or
- (b) poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer-folate and poly(L-lactic acid)-poly(ethylene glycol) block copolymer, or
- (c) poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer-folate, or
- (d) poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer-folate and poly(L-lactic acid)-poly(ethylene glycol) block copolymer-folate.
Dependencies are inferred from the claim text.