Iontophoretic microneedle device

Abstract

A medical drug devices for transdermal drug delivery systems (TDDS) comprising a novel iontophoretic polymeric microneedle device and its use in administration of drugs.

1 .- 16 . (canceled) 
     
     
         17 . A polymeric microneedle array for delivery of macromolecular compounds (API) through the skin having a plurality of micro-scaled solid microneedles, the microneedles consisting of a dried polymer composition comprising:
 15 to 40 wt. % of a water soluble polymer as a binder,   less than 2 wt. % of a humectant/softener, and   less than 2 wt. % of a surfactant;   and   1 to 15 wt. % of the macromolecular compound (API) encapsulated therein,   wherein the wt. % are given with respect to the liquid polymer composition before drying.   
     
     
         18 . The microneedle array of  claim 17 , wherein the water soluble polymer is polyvinylpyrrolidon (PVP). 
     
     
         19 . The microneedle array of  claim 18 , wherein the water soluble polymer is a medium viscosity PVP having an average molecular weight (Mw) of about 40,000. 
     
     
         20 . The microneedle array of  claim 17 , wherein the humectant and softener is glycerol. 
     
     
         21 . The microneedle array of  claim 17 , wherein the surfactant is polysorbate 80. 
     
     
         22 . The microneedle array of  claim 17 , wherein the macromolecular compound (API) is hydrophilic. 
     
     
         23 . The microneedle array of  claim 17 , wherein the macromolecular compound (API) is sumatriptan or sumatriptan succinate. 
     
     
         24 . The microneedle array of  claim 17 , wherein the water soluble polymer is present in the liquid polymer composition before drying in an amount of 20 to 30 wt. %. 
     
     
         25 . The microneedle array of  claim 17 , wherein the humectant and softener is present in the liquid polymer composition before drying in an amount of 0.5 to 1.5 wt. %. 
     
     
         26 . The microneedle array of  claim 17 , wherein the surfactant is present in the liquid polymer composition before drying in an amount of 0.05 to 1.0 wt. %. 
     
     
         27 . The microneedle array of  claim 17 , wherein the macromolecular compound (API) is present in the liquid polymer composition before drying in an amount of 5 to 10 wt. %. 
     
     
         28 . An active transdermal patch device for delivery of macromolecular compounds (API) through the skin, comprising:
 a power supply with controllable current source   a skin cathode electrically connected to the power supply, and   a skin anode electrically connected to the power supply, the anode comprising the microneedle array as characterized in  claim 17 .   
     
     
         29 . A method for the preparation of a polymeric microneedle array as characterized in  claim 17 , comprising the steps of:
 dissolving   15 to 40 wt. % of a water soluble polymer as a binder,   less than 2 wt. % of a humectant/softener, and   less than 2 wt. % of a surfactant, and   1 to 15 wt. % of a macromolecular compound (API)   in water, to prepare a liquid polymer composition; wherein the wt. % are given with respect to the liquid polymer composition before drying;   molding the liquid polymer composition in flexible molds having the negative form of the microarray to be produced;   drying the polymer composition within the mold; and   removing the dried polymeric microneedle array having formed solid microneedles from the mold.   
     
     
         30 . A method for transdermally administering a macromolecular API to a patient comprising:
 microporating the skin of the patient by placing a polymeric microneedle array with the macromolecular API encapsulated therein as characterized in  claim 17  onto the patient's skin allowing the microneedles to penetrate the stratum corneum of the skin, and   applying anodic electrical current through the microneedle array, such that the macromolecular API is released from the microneedles into the patient's skin.   
     
     
         31 . The method of  claim 30 , where the amount of API released is controlled by the level of anodic current flowing through the microarray. 
     
     
         32 . A method of prophylaxis and therapy of migraine in a patient suffering therefrom, comprising transdermally administering sumatriptan using the polymeric microneedle array according to  claim 17  with sumatriptan encapsulated therein.