Microemulsion topical delivery platform
Provided are pharmaceutical carriers based on oil-in-water microemulsions and methods of making same. Also provided are pharmaceutical compositions comprising a carrier of the invention and a lipophilic active pharmaceutical ingredient (API), as well as methods for making same. The pharmaceutical compositions are particularly suitable for use in formulating lipophilic APIs for topical administration to the eye. Specifically included are pharmaceutical compositions comprising fenofibrate or fenofibric acid as API. Also provided is a method of treating a disease of the posterior segment of the eye. Also provided is a pharmaceutical composition comprising a compound represented by formulated for topical administration to the eye.
1. A method of treating a disease of the posterior segment of the eye, comprising:
topically administering to an eye of a subject in need thereof a composition comprising
an oil-in-water microemulsion comprising
(i) an oil selected from the group consisting of isopropyl myristate, isopropyl palmitate, and medium chain triglycerides;
(ii) a pair of surfactants selected from the group consisting of two polysorbates, a polysorbate and propylene glycol, a polysorbate and glycerol, a polysorbate and 1,2,3-triacetoxypropane, polyethoxylated castor oil and 1,2,3-triacetoxypropane, and polyethoxylated castor oil and propylene glycol;
(iii) water; and
(iv) a therapeutically effective amount, for treating a disease of the posterior segment of the eye, of a lipophilic active pharmaceutical ingredient (API),
wherein:
the API represents about 0.01 to about 5 percent (w/v) of the composition;
the water represents 50 to about 95 percent (w/w) of the composition;
the oil and the pair of surfactants represent substantially all of the remainder of the composition;
the ratio of percent (w/w) the pair of surfactant to percent (w/w) the oil is at least about 10:1; and
the composition is formulated for topical administration to the eye.
2. The method of claim 1 , wherein the lipophilic API is selected from the group consisting of adaprolol maleate, cyclosporine A, fenofibrate, fenofibric acid, indomethacin, miconazole, pilocarpine, piroxicam, and Δ 8 -THC.
3. The method of claim 1 , wherein the lipophilic API is fenofibrate.
4. The method of claim 1 , wherein the lipophilic API is fenofibric acid.
5. The method of claim 1 , wherein the lipophilic API is represented by
6. The method of claim 1 , wherein the disease of the posterior segment of the eye is characterized by inflammation, neovascularization, vascular leakage, fibrosis, or any combination thereof.
7. The method of claim 1 , wherein the disease of the posterior segment of the eye is selected from the group consisting of: age-related macular degeneration, diabetic retinopathy, posterior uveitis, retinal edema, macular edema, and retinal vein occlusion.
8. The method of claim 1 , wherein the disease of the posterior segment of the eye is age-related macular degeneration.
9. The method of claim 1 , wherein the disease of the posterior segment of the eye is diabetic retinopathy.