US2011129422A1PendingUtilityA1

Viscous Terpolymers as Drug Delivery Platform

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Assignee: BROOKWOOD PHARMACEUTICALSPriority: Nov 13, 2007Filed: Feb 8, 2011Published: Jun 2, 2011
Est. expiryNov 13, 2027(~1.3 yrs left)· nominal 20-yr term from priority
Inventors:Peter MarklandHoward Bowman
A61P 35/00A61P 25/00A61P 29/00A61P 23/00A61P 19/00A61K 31/7088C08G 63/08C08G 63/664A61K 47/10A61K 47/34A61K 47/36A61K 47/02C08G 2261/126A61K 9/0019
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Claims

Abstract

Disclosed are terpolymer compositions of lactide, glycolide, and caprolactone and methods of making such polymers with an initiator. Methods of using the terpolymers as a drug delivery platform are also disclosed.

Claims

exact text as granted — not AI-modified
1 . A method of preparing a terpolymer composition, comprising:
 a. polymerizing lactide, glycolide, and caprolactone in the presence of an initiator, wherein the initiator is a non-crystalline primary or secondary alcohol.   
     
     
         2 . The method of  claim 1 , wherein the lactide is present in an amount of from about 10 to about 60 mole percent. 
     
     
         3 . The method of  claim 1 , wherein the glycolide is present in an amount of from about 10 to about 40 mole percent. 
     
     
         4 . The method of  claim 1 , wherein the caprolactone is present in an amount of from about 20 to about 70 mole percent. 
     
     
         5 . The method of  claim 1 , wherein the lactide is present in an amount of about 16 mole percent, the glycolide is present in an amount of about 26 mole percent, and the caprolactone is present in an amount of about 58 mole percent. 
     
     
         6 . The method of  claim 1 , wherein the initiator is a short chain alcohol, a saturated or unsaturated long chain alcohol, mono-hydroxy poly(ethylene glycol), di-hydroxy poly(ethylene glycol), multi-functionalized multi-hydroxyl poly(ethylene glycol), or a mixture thereof. 
     
     
         7 . The method of  claim 1 , wherein the initiator contains one hydroxyl group, two hydroxyl groups, or more than two hydroxyl groups. 
     
     
         8 . The method of  claim 1 , wherein the initiator comprises a polymeric alcohol. 
     
     
         9 . The method of  claim 1 , wherein the terpolymer has a Tg of less than about 20° C. and a Mw less than about 25,000 Daltons. 
     
     
         10 . The method of  claim 1 , wherein the terpolymer has an inherent viscosity at 0.5% (wt/vol) terpolymer in chloroform at 30° C. of from about 0.05 to about 0.25. 
     
     
         11 . The method of  claim 1 , wherein the terpolymer has a viscosity of less than about 30,000 poise. 
     
     
         12 . The method of  claim 1 , further comprising adding a bioactive agent prior to, during, or after step (a). 
     
     
         13 . The method of  claim 12 , wherein the bioactive agent comprises a drug, a peptide, a protein, an antibody or fragment thereof, a nucleic acid, or imaging agent. 
     
     
         14 . The method of  claim 1 , further comprising adding plasticizer prior to, during, or after step (a). 
     
     
         15 . The method of  claim 1 , further comprising adding a surfactant, excipient, or additive prior to, during, or after step (a). 
     
     
         16 . A method of delivering a bioactive agent to a subject, comprising:
 a. admixing a bioactive agent and a terpolymer composition comprising a terpolymer of lactide, glycolide, and caprolactone residues, wherein the terpolymer comprises an end group that is a residue of an initiator and wherein the initiator is a non-crystalline alcohol.   b. administering the admixture from step (a) to the subject.   
     
     
         17 . The method of  claim 16 , wherein the admixture is administered by injection. 
     
     
         18 . The method of  claim 16 , where in the amount of lactide residue in the terpolymer is from about 10 to about 60 mole percent. 
     
     
         19 . The method of  claim 16 , wherein the amount of glycolide residue in the terpolymer is from about 10 to about 40 mole percent. 
     
     
         20 . The method of  claim 16 , wherein the amount of caprolactone residue in the terpolymer is from about 20 to about 70 mole percent. 
     
     
         21 . The method of  claim 16 , wherein the amount of lactide residue in the terpolymer is about 16 mole percent, the amount of glycolide residue is about 26 mole percent, and the amount of caprolactone residue is about 58 mole percent. 
     
     
         22 . The method of  claim 16 , wherein the initiator is a short chain alcohol, a saturated or unsaturated long chain alcohol, mono-hydroxy poly(ethylene glycol), di-hydroxy poly(ethylene glycol), multi-functionalized multi-hydroxyl poly(ethylene glycol), or a mixture thereof. 
     
     
         23 . The method of  claim 16 , wherein the initiator contains one hydroxyl group, two hydroxyl groups, or more than two hydroxyl groups. 
     
     
         24 . The method of  claim 16 , wherein the initiator is a polymeric alcohol. 
     
     
         25 . The method of  claim 16 , wherein the terpolymer has a Tg of less than about 20° C. 
     
     
         26 . The method of  claim 16 , wherein the terpolymer has an inherent viscosity at 0.5% (wt/vol) terpolymer in chloroform at 30° C. of from about 0.05 to about 0.25. 
     
     
         27 . The method of  claim 16 , wherein the terpolymer has a Mw less than about 25,000 Daltons. 
     
     
         28 . The method of  claim 16 , wherein the terpolymer has a viscosity of less than about 30,000 poise. 
     
     
         29 . The method of  claim 16 , wherein the bioactive agent comprises a drug, a peptide, a protein, an antibody or fragment thereof, a nucleic acid, or imaging agent. 
     
     
         30 . The method of  claim 16 , wherein terpolymer composition further comprises a plasticizer. 
     
     
         31 . The method of  claim 16 , further the terpolymer compositions further comprises an agent, surfactant, excipient, or additive.

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