Ocular therapy using glucocorticoid derivatives selectively penetrating posterior segment tissues
Ophthalmically therapeutic materials, such as liquid-containing compositions and polymeric drug delivery systems, include a therapeutic component that includes an Glucocorticoid Derivative which, upon delivery to the posterior segment of a mammalian eye, does not significantly diffuse to the anterior segment of said eye. Methods of making and using the present materials are also described.
1. An ophthalmic composition comprising: a therapeutically effective amount of a Glucocorticoid Derivative (GD) comprising an acyl group linked to C 17 , C 21 , or combination thereof via an ester linkage, and a viscosity-inducing component.
2. The composition of claim 1 wherein said GD has a lipophilicity greater than 2.53.
3. The composition of claim 1 wherein said GD has an aqueous solubility less than 10 mg/ml.
4. The composition of claim 1 , wherein the viscosity-inducing component comprises hyaluronic acid, carbomers, polyacrylic acid, cellulosic derivatives, polycarbophil, polyvinylpyrrolidone, gelatin, dextrin, polysaccharides, polyacrylamide, polyvinyl alcohol, polyvinyl acetate, derivatives thereof and mixtures thereof.
5. The composition of claim 4 , wherein the viscosity-inducing component comprises a polymeric hyaluronate component.
6. The composition of claim 1 wherein said acyl group is selected from the group consisting of an acetyl, butyryl, valeryl, propionyl, furoyl, and benzoyl group.
7. The composition of claim 1 wherein said composition is suitable for administration to a patient by at least one of intravitreal administration and periocular administration.
8. The composition of claim 1 wherein said ophthalmic composition is an implant.
9. The composition of claim 8 wherein said implant further comprises a polymeric component.
10. The composition of claim 9 wherein said polymeric component is selected from the group consisting of poly (lactide-co-glycolide) polymer (PLGA), poly-lactic acid (PLA), poly-glycolic acid (PGA), polyesters, poly (ortho ester), poly(phosphazine), poly (phosphate ester), polycaprolactones, gelatin, and collagen, and derivatives and combinations thereof.
11. The composition of claim 1 , wherein the GD is beclomethasone propionate.
12. The composition of claim 1 , wherein the GD is beclomethasone dipropionate.