Biodegradable diblock copolymers having reverse thermal gelation properties and methods of use thereof
First Claim
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1. A biodegradable AB type diblock copolymer comprising:
- i) 61 to 85% by weight of a biodegradable, hydrophobic A block which is a member selected from the group consisting of biodegradable polyesters, biodegradable polyester amides, biodegradable polyether esters, biodegradable polyurethanes, biodegradable polyester urethanes, biodegradable polycarbonates and polyester carbonates; and
ii) 15 to 39% by weight of a biocompatible, hydrophilic B block comprising a monofunctional polyethylene glycol(PEG) having a number average molecular weight within a range of 50 Daltons to 5000 Daltons, wherein said diblock copolymer has a number average molecular weight within a range of 450 Daltons to 15000 Daltons and possesses reverse thermal gelation properties.
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Abstract
A water soluble, biodegradable AB type diblock copolymer which comprises 61 to 85% by weight of a biodegradable, hydrophobic A block comprising a biodegradable polyester, and 15 to 39% by weight of a biocompatible, hydrophilic B block comprising a monofunctional polyethylene glycol(PEG) having a number average molecular weight less than 5000, and wherein said diblock copolymer has a number average molecular weight less than 15000 and possesses reverse thermal gelation properties.
126 Citations
29 Claims
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1. A biodegradable AB type diblock copolymer comprising:
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i) 61 to 85% by weight of a biodegradable, hydrophobic A block which is a member selected from the group consisting of biodegradable polyesters, biodegradable polyester amides, biodegradable polyether esters, biodegradable polyurethanes, biodegradable polyester urethanes, biodegradable polycarbonates and polyester carbonates; and
ii) 15 to 39% by weight of a biocompatible, hydrophilic B block comprising a monofunctional polyethylene glycol(PEG) having a number average molecular weight within a range of 50 Daltons to 5000 Daltons, wherein said diblock copolymer has a number average molecular weight within a range of 450 Daltons to 15000 Daltons and possesses reverse thermal gelation properties. - View Dependent Claims (2, 3, 4)
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5. An aqueous biodegradable polymeric drug delivery composition possessing reverse thermal gelation properties comprised of an aqueous phase having uniformly contained therein:
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(a) an effective amount of a drug; and
(b) a biodegradable AB type diblock copolymer comprising;
i) 61 to 85% by weight of a biodegradable, hydrophobic A block which is a member selected from the group consisting of biodegradable polyesters, biodegradable polyester amides, biodegradable polyether esters, biodegradable polyurethanes, biodegradable polyester urethanes, biodegradable polycarbonates and polyester carbonates; and
ii) 15 to 39% by weight of a biocompatible, hydrophilic B block comprising a monofunctional polyethylene glycol(PEG) having a number average molecular weight within a range of 50 Daltons to 5000 Daltons, wherein said diblock copolymer has a number average molecular weight within a range of 450 Daltons to 15000 Daltons and possesses reverse thermal gelation properties. - View Dependent Claims (6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
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16. A method for the administration of a drug to a warm-blooded animal in a controlled release form which comprises:
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(1) providing an aqueous biodegradable polymeric drug delivery composition possessing reverse thermal gelation properties comprised of an aqueous phase having uniformly contained therein;
(a) an effective amount of a drug; and
(b) a biodegradable AB type diblock copolymer comprising;
i) 61 to 85% by weight of a biodegradable, hydrophobic A block which is a member selected from the group consisting of biodegradable polyesters, biodegradable polyester amides, biodegradable poly ether esters, biodegradable polyurethanes, biodegradable polyester urethanes, biodegradable polycarbonates and polyester carbonates; and
ii) 15 to 39% by weight of a biocompatible, hydrophilic B block comprising a monofunctional polyethylene glycol(PEG) having a number average molecular weight within a range of 50 Daltons to 5000 Daltons, and wherein said diblock copolymer has a number average molecular weight within a range of 450 Daltons to 15000 Daltons and possesses reverse thermal gelation properties;
(2) maintaining said composition as a liquid at a temperature below the gelation temperature of said diblock copolymer; and
(3) administering said composition as a liquid to said warm-blooded animal with the subsequent formation of a gel as the temperature of said composition is raised by the body temperature of said animal to above the gelation temperature of said diblock polymer. - View Dependent Claims (17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27)
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28. A method for enhancing the solubility of a drug, comprising uniformly admixing an effective amount of said drug in an aqueous biodegradable polymeric drug delivery composition possessing reverse thermal gelation properties, said aqueous composition being comprised of an aqueous phase having uniformly contained therein a biodegradable AB type diblock copolymer comprising:
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i) 61 to 85% by weight of a biodegradable, hydrophobic A block which is a member selected from the group consisting of biodegradable polyesters, biodegradable polyester amides, biodegradable polyether esters, biodegradable polyurethanes, biodegradable polyester urethanes, biodegradable polycarbonates and polyester carbonates; and
ii) 15 to 39% by weight of a biocompatible, hydrophilic B block comprising a monofunctional polyethylene glycol(PEG) having a number average molecular weight within a range of 50 Daltons to 5000 Daltons, wherein said diblock copolymer has a number average molecular weight within a range of 450 Daltons to 15000 Daltons and possesses reverse thermal gelation properties.
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29. A method for enhancing the stability of a drug comprising uniformly admixing an effective amount of said drug in an aqueous biodegradable polymeric drug delivery composition possessing reverse thermal gelation properties said aqueous composition being comprised of an aqueous phase having uniformly contained therein a biodegradable AB type diblock copolymer comprising:
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i) 61 to 85% by weight of a biodegradable, hydrophobic A block which is a member selected from the group consisting of biodegradable polyesters, biodegradable polyester amides, biodegradable polyether esters, biodegradable polyurethanes, biodegradable polyester urethanes, biodegradable polycarbonates and polyester carbonates; and
ii) 15 to 39% by weight of a biocompatible, hydrophilic B block comprising a monofunctional polyethylene glycol(PEG) having a number average molecular weight within a range of 50 Daltons to 5000 Daltons, wherein said diblock copolymer has a number average molecular weight within a range of 450 Daltons to 15000 Daltons and possesses reverse thermal gelation properties.
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Specification