Controlled release delivery system for nasal applications and methods of treatment

Abstract

This invention relates to a gel formulation for nasal administration of a controlled release formulation of hormones to the systemic circulation and/or to the brain. The special lipophilic or partly lipophilic system of the invention leads to higher bioavailability of the active ingredient caused by sustained serum levels in plasma but also leads to a more favorable serum level profile. The special lipophilic or partly lipophilic system also allows for the modulation of brain functioning. The invention also relates to the nasal administration of steroid hormones for treatment of female sexual dysfunction (FSD) or female arousal disorder.

1 - 26 . (canceled) 
     
     
         27 . A method for the treatment of Female Sexual Dysfunction (FSD) comprising the step of nasally administering to a patient in need of such treatment an effective amount of a formulation comprising: a) at least one sexual hormone drug; b) at least one lipophilic or partly lipophilic carrier; and c) a compound or a mixture of compounds having surface tension decreasing activity, an amount effective for in situ generation of an emulsion upon contact of the formulation with water. 
     
     
         28 . The method according to  claim 27 , wherein the sexual hormone drug is testosterone. 
     
     
         29 . The method according to  claim 27 , wherein the sexual hormone drug is comprised within the formulation in an amount of from about 0.2 to about 6% by weight. 
     
     
         30 . The method according to  claim 27 , wherein the sexual hormone drug is comprised within the formulation in an amount of from about 0.2 to about 4% by weight. 
     
     
         31 . The method according to  claim 27 , wherein the amount of oil comprises between 30% and 98% by weight. 
     
     
         32 . The method according to  claim 27 , wherein the at least one compound having surface tension decreasing activity is comprised within the formulation in an amount of from about 1 to about 20% by weight. 
     
     
         33 . The method according to  claim 27  wherein the formulation further comprises a viscosity regulating agent, wherein the viscosity regulating agent is comprised within the formulation in an amount of from about 0.5 to about 10% by weight. 
     
     
         34 . A method for the treatment of female arousal disorder comprising the step of nasally administering to a patient in need of such treatment an effective amount of a formulation comprising: a) at least one sexual hormone drug; b) at least one lipophilic or partly lipophilic carrier; and c) a compound or a mixture of compounds having surface tension decreasing activity, an amount effective for in situ generation of an emulsion upon contact of the formulation with water. 
     
     
         35 . The method according to  claim 34 , wherein the sexual hormone drug is testosterone. 
     
     
         36 . The method according to  claim 34 , wherein the sexual hormone drug is comprised within the formulation in an amount of from about 0.2 to about 6% by weight. 
     
     
         37 . The formulation according to  claim 34 , wherein the sexual hormone drug is comprised within the formulation in an amount of from about 0.2 to about 4% by weight. 
     
     
         38 . The method according to  claim 34 , wherein the amount of oil comprises between 30% and 98% by weight. 
     
     
         39 . The method according to  claim 34 , wherein the at least one compound having surface tension decreasing activity is comprised within the formulation in an amount of from about 1 to about 20% by weight. 
     
     
         40 . The method according to  claim 34 , wherein the formulation further comprises a viscosity regulating agent, wherein the viscosity regulating agent is comprised within the formulation in an amount of from about 0.5 to about 10% by weight. 
     
     
         41 . A method of increasing an amygdala response in women comprising the step of nasally administering to a woman an effective amount of a formulation comprising: a) at least one sexual hormone drug; b) at least one lipophilic or partly lipophilic carrier; and c) a compound or a mixture of compounds having surface tension decreasing activity, an amount effective for in situ generation of an emulsion upon contact of the formulation with water, wherein the increased amygdala response is associated with the treatment of Female Sexual Dysfunction. 
     
     
         42 . The method according to  claim 41 , wherein the sexual hormone drug is testosterone. 
     
     
         43 . The method according to  claim 41 , wherein the sexual hormone drug is comprised within the formulation in an amount of from about 0.2 to about 6% by weight. 
     
     
         44 . The formulation according to  claim 41 , wherein the sexual hormone drug is comprised within the formulation in an amount of from about 0.2 to about 4% by weight. 
     
     
         45 . The method according to  claim 41 , wherein the amount of oil comprises between 30% and 98% by weight. 
     
     
         46 . The method according to  claim 41 , wherein the at least one compound having surface tension decreasing activity is comprised within the formulation in an amount of from about 1 to about 20% by weight. 
     
     
         47 . The method according to  claim 41 , wherein the formulation further comprises a viscosity regulating agent, wherein the viscosity regulating agent is comprised within the formulation in an amount of from about 0.5 to about 10% by weight.