Controlled release delivery system for nasal applications and methods of treatment
View Patent ↗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. A formulation for nasal application comprising:
a) testosterone, wherein said testosterone is present within the formulation in an amount of from about 0.2% to about 6% by weight of the formulation;
b) at least one lipophilic or partly lipophilic carrier present in an amount of from about 60% to about 98% by weight of the formulation;
c) at least one compound having surface tension decreasing activity present in an amount of from about 1% to about 20% by weight of the formulation; and
d) at least one viscosity regulating agent present in an amount of from about 0.5% to about 10% by weight of the formulation.
2. The formulation according to claim 1 , wherein the lipophilic carrier comprises castor oil.
3. The formulation according to claim 1 , wherein the at least one compound having surface tension decreasing activity comprises at least one surfactant selected from the group consisting of lecithin, fatty acid ester of polyvalent alcohols, of sorbitanes, of polyoxyethylensorbitans, of polyoxyethylene, of sucrose, of polyglycerol and/or at least one humectant selected from the group consisting of sorbitol, glycerine, polyethylene glycol, and macrogol glycerol fatty acid ester, or a mixture thereof.
4. The formulation according to claim 3 , wherein the at least one compound having surface tension decreasing activity comprises an oleoyl macrogolglyceride or a mixture of oleoyl macrogolglycerides.
5. The formulation according to claim 1 , wherein said viscosity regulating agent comprises a thickener or gelling agent selected from the group consisting of cellulose and cellulose derivatives, polysaccharides, carbomers, polyvinyl alcohol, povidone, colloidal silicon dioxide, cetyl alcohols, stearic acid, beeswax, petrolatum, triglycerides and lanolin, or a mixture thereof.
6. The formulation according to claim 5 , wherein said viscosity increasing agent is colloidal silicon dioxide.
7. A method for the treatment of Female Sexual Dysfunction (FSD) comprising nasally administering to a patient in need of such treatment an effective amount of a formulation according to claim 1 .
8. A method for the treatment of female arousal disorder comprising nasally administering to a patient in need of such treatment an effective amount of a formulation according to claim 1 .
9. A method of increasing an amygdala response in women comprising the step of nasally administering to a woman an effective amount of a formulation according to claim 1 .