Topical Formulations of Corticosteroids with Enhanced Bioavailability
Described herein are methods and compositions for increasing the bioavailability of a corticosteroid, such as hydrocortisone 17-butyrate, in a topical formulation.
1 . A method for enhancing the bioavailability of a corticosteroid from an oil-in-water emulsion, comprising the step of varying the concentrations of surfactants, co-surfactants, emollients and water, thereby forming an improved corticosteroid-containing emulsion.
2 . The method of claim 1 , wherein the improved corticosteroid-containing emulsion comprises
a corticosteroid;
a surfactant and a co-surfactant;
an oil phase comprising at least a first emollient and a second emollient; and
water;
wherein the first emollient is a vegetable oil and the second emollient is a mineral oil; and
the weight ratio of vegetable oil-to-mineral oil is about 0.03 to about 1.00.
3 . The method of claim 2 , wherein the total concentration of surfactants and co-surfactants in the improved corticosteroid-containing emulsion is about 8.0% to about 12.0% by weight of the improved corticosteroid-containing emulsion.
4 . The method of claim 2 , wherein the surfactant is ceteth-20; and the co-surfactant is cetostearyl alcohol.
5 . The method of claim 2 , wherein the improved corticosteroid-containing emulsion does not comprise steareth-10.
6 . The method of claim 2 , wherein the emollients are safflower oil, dimethicone, light mineral oil, and white petrolatum.
7 . The method of claim 2 , wherein the corticosteroid is hydrocortisone butyrate.
8 . The method of claim 7 , wherein the hydrocortisone butyrate is hydrocortisone 17-butyrate.
9 . The method of claim 8 , wherein the concentration of hydrocortisone-17 butyrate is about 0.1% by weight of the improved corticosteroid-containing emulsion.
10 . The method of claim 8 , wherein the concentration of hydrocortisone 17-butyrate is 0.15% by weight of the improved corticosteroid-containing emulsion.
11 . The method of claim 2 , wherein the vegetable oil is safflower oil, sunflower oil, corn oil, sesame oil, peanut oil, canola oil, or olive oil.
12 . The method of claim 2 , wherein the vegetable oil is safflower oil.
13 . The method of claim 2 , wherein the mineral oil is light mineral oil.
14 . The method of claim 1 , wherein the improved corticosteroid-containing emulsion consists essentially of, by weight of the oil-in-water emulsion
Hydrocortisone 17-butyrate USP
From about 0.01% to about 0.25%
Water USP
From about 30% to about 80%
Glycerin USP
From about 2.5% to about 7.5%
Methylparaben NF
From about 0.15% to about 0.45%
Propylparaben NF
From about 0.05% to about 0.15%
Cetostearyl Alcohol NF
From about 2.5% to about 7.5%
Urea USP
From about 0.3% to about 0.9%
Dimethicone NF
From about 0.5% to about 1.5%
Safflower Oil USP
From about 3.0% to about 9.0%
White Petrolatum USP
From about 3.0% to about 9.0%
Light Mineral Oil NF
From about 6.0% to about 18.0%
Ceteth-20 NF
From about 3.0% to about 9.0%
Butylated Hydroxytoluene NF
From about 0.015% to about 0.045%
Sodium Citrate USP
From about 0.15% to about 0.45%
Citric Acid USP
From about 0.20% to about 0.60%
15 . A method of treating a skin disorder, comprising the step of:
applying topically to an area of skin of a subject in need thereof a therapeutically-effective amount of an improved corticosteroid-containing emulsion of claim 1 .
16 . The method of claim 15 , wherein the improved corticosteroid-containing emulsion or the formulation is applied once daily or twice daily.
17 . The method of claim 15 , wherein the subject is human.
18 . The method of claim 15 , wherein the skin disorder is a dermatosis.
19 . The method of claim 15 , wherein the skin disorder is atopic dermatitis.