High enhancer-loading polyacrylate formulation for transdermal applications

Abstract

A polyacrylate formulation suitable for delivery of drug to through a body surface of an individual. By loading the drug and permeation enhancers at a high concentration into a polyacrylate proadhesive that has inadequate adhesive properties for typical adhesive application on the skin, a formulation with desirable adhesive characteristics and effective therapeutic properties can be made. The proadhesive has higher glass transition temperature than typical pressure sensitive adhesives.

1 - 32 . (canceled) 
     
     
         33 . A device for transdermal administration of at least one drug, the device comprising:
 a reservoir matrix comprising:
 at least one permeation enhancer; and 
 an acrylate polymer, the acrylate polymer having a T g  of greater than −15° C. if without the at least one drug and without the at least one permeation enhancer, 
 wherein the acrylate polymer constitutes 40 wt % to 90 wt % of the matrix, the acrylate polymer comprising soft monomer in an amount of up to 60 wt % of the acrylate polymer, hard monomer in an amount of at least 40 wt % of the acrylate polymer, and functional monomer in an amount of between 10 wt % to 35 wt % of the acrylate polymer, and 
 wherein the at least one drug and the at least one permeation enhancer are dissolved in the acrylate polymer. 
   
     
     
         34 . The device of  claim 33 , wherein the soft monomer is an alkyl acrylate monomer having 4 to 10 carbon atoms in the alkyl group. 
     
     
         35 . The device of  claim 33 , wherein the soft monomer is selected from the group consisting of butyl acrylate, hexyl acrylate, 2-ethylhexyl acrylate, octyl acrylate, dodecyl acrylate, and isomers thereof. 
     
     
         36 . The device of  claim 33 , wherein the acrylate polymer constitutes 45 wt to 80 wt % of the matrix. 
     
     
         37 . The device of  claim 33 , wherein the acrylate polymer has a T g  of greater than −10° C. if without the at least one drug and without the at least one permeation enhancer. 
     
     
         38 . The device of  claim 33 , wherein the matrix has a T g  in the range of −10° C. to −20° C., a creep compliance of less than 1×10 −3  cm 2 /dyn, and a storage modulus in the range of 1×10 5  dyn/cm 2  to 8×10 5  dyn/cm 2 . 
     
     
         39 . The device of  claim 33 , wherein the matrix has a T g  in the range of −10° C to −40° C., a creep compliance in the range of 1×10 −4  cm 2 /dyn to 6×10 −4  cm 2 /dyn, and a storage modulus in the range of 1×10 5  dyn/cm 2  to 8×10 5  dyn/cm 2 . 
     
     
         40 . The device of  claim 33 , wherein the at least one drug is selected from the group consisting of fentanyl, fentanyl analog, galantamine, norelgestromin, and salts and esters thereof. 
     
     
         41 . A transdermal drug delivery device, comprising:
 a reservoir matrix comprising:
 at least one drug dissolved in an acrylate polymer, the acrylate polymer having a T g  of greater than −15° C. if without the at least one drug, 
 wherein the acrylate polymer constitutes 40 wt % to 90 wt % of the matrix, the acrylate polymer comprising soft monomer in an amount of up to 60 wt % of the acrylate polymer, hard monomer in an amount of at least 40 wt % of the acrylate polymer, and functional monomer in an amount of between 10 wt % to 35 wt % of the acrylate polymer. 
   
     
     
         42 . The device of  claim 41 , wherein the soft monomer is an alkyl acrylate monomer having 4 to 10 carbon atoms in the alkyl group. 
     
     
         43 . The device of  claim 41 , wherein the acrylate polymer has a T g  of greater than −10° C. if without the at least one drug. 
     
     
         44 . The device of  claim 41 , wherein the matrix has a T g  in the range of −10° C. to −20° C., a creep compliance of less than 1×10 −3  cm 2 /dyn, and a storage modulus in the range of 1×10 5  dyn/cm 2  to 8×10 5  dyn/cm 2 . 
     
     
         45 . The device of  claim 41 , wherein the matrix has a T g  in the range of −10° C. to −40° C., a creep compliance in the range of 1×10 −4  cm 2 /dyn to 6×10 −4  cm 2 /dyn, and a storage modulus in the range of 1×10 5  dyn/cm 2  to 8×10 5  dyn/cm 2 . 
     
     
         46 . The device of  claim 41 , wherein the at least one drug is selected from the group consisting of fentanyl, fentanyl analog, galantamine, norelgestromin, and salts and esters thereof. 
     
     
         47 . A transdermal drug delivery device, comprising:
 a reservoir matrix comprising:
 at least one drug; 
 at least one permeation enhancer; and 
 an acrylate polymer comprising soft monomer in an amount of up to 60 wt % of the acrylate polymer, hard monomer in an amount of at least 40 wt % of the acrylate polymer, and functional monomer in an amount of between 10 wt % to 35 wt % of the acrylate polymer, 
   wherein the at least one drug and the at least one permeation enhancer are dissolved in the acrylate polymer in a combined amount of at least 30 wt % of the matrix, and   wherein the matrix is applicable as a pressure-sensitive adhesive to a body surface of a subject for transdermal delivery of the at least one drug.   
     
     
         48 . The device of  claim 47 , wherein the acrylate polymer has a T g  of greater than −15° C. if without the at least one drug and without the at least one permeation enhancer. 
     
     
         49 . The device of  claim 47 , wherein the acrylate polymer constitutes 40 wt % to 90 wt % of the matrix. 
     
     
         50 . The device of  claim 47 , wherein the matrix has a T g  in the range of −10° C. to −20° C., a creep compliance of less than 1×10 −3  cm 2 /dyn, and a storage modulus in the range of 1×10 5  dyn/cm 2  to 8×10 5  dyn/cm 2 . 
     
     
         51 . The device of  claim 47 , wherein the matrix has a T g  in the range of −10° C. to −40° C., a creep compliance in the range of 1×10 −4  cm 2 /dyn to 6×10 −4  cm 2 /dyn, and a storage modulus in the range of 1×10 5  dyn/cm 2  to 8×10 5  dyn/cm 2 . 
     
     
         52 . The device of  claim 47 , wherein the at least one drug is selected from the group consisting of fentanyl, fentanyl analog, galantamine, norelgestromin, and salts and esters thereof.