Sustained release enhanced lipolytic formulation for regional adipose tissue treatment
Compositions, formulations, methods, and systems for treating regional fat deposits comprise contacting a targeted fat deposit with a composition comprising long acting beta-2 adrenergic receptor agonist and a compound that reduces desensitization of the target tissue to the long acting beta-2 adrenergic receptor agonist, for example, glucocorticosteroids and/or ketotifen. Embodiments of the composition are administered, for example, by injection, and/or transdermally.
1. An injectable formulation for treating regional adipose tissue or regional fat accumulation consisting essentially of:
an effective amount of a long acting beta-2 adrenergic receptor agonist that is selected from the group consisting of salmeterol, formoterol, and salts thereof;
an effective amount of a glucocorticosteroid that is selected from the group consisting of dexamethasone, prednisolone, fluticasone, budesonide, and salts thereof;
a liquid carrier; and
a pharmaceutically acceptable excipient;
the salmeterol, formoterol, and salts thereof, the glucocorticosteroid, the liquid carrier and the pharmaceutically acceptable excipient formulated for injection into a layer of subcutaneous fat in a human in need.
2. The formulation of claim 1 , wherein the formulation allows dispersal of (a) the salmeterol, formoterol, and salts thereof, and (b) the glucocorticosteroid, into the layer of subcutaneous fat at a regional fat site selected from a submental region, a waist, a hip, a lateral buttock or a thigh.
3. The formulation of claim 1 , wherein salmeterol is present as a salt.
4. The formulation of claim 1 , wherein the glucocorticosteroid is fluticasone propionate.
5. The formulation of claim 1 , wherein the liquid carrier is a lipophilic liquid carrier.
6. A method for treating a fat accumulation comprising
administering an injectable formulation of claim 1 .
7. The method claim 6 , wherein the pharmaceutically effective amount of salmeterol is up to about 100 μg/day.
8. The method claim 6 , wherein the pharmaceutically effective amount of formoterol is up to about 50 μg/day.
9. A method for reducing adipose tissue comprising
administering an injectable formulation of claim 1 .
10. A method for treating regional fat accumulations or cellulite comprising
administering to a regional fat accumulation or cellulite an injectable formulation of claim 1 .