Water-in oil type emulsion for treating a disease of the eye

1. A composition comprising a water-in-oil emulsion comprising an oil phase, a lipophilic surfactant dissolved in the oil phase, an aqueous phase dispersed in the oil phase, a hydrophilic therapeutic agent dissolved in the aqueous dispersed phase, and wherein the composition:

has a density lower than the density of water;

has a viscosity ranging from 25 to 10 000 mPa·s at 20° C.;

has droplets of water ranging from 20 nm to 600 nm; and

is formulated for intraocular injection.

2. The composition of claim 1 , wherein the composition has a density ranging from 0.91 to 0.97 g/cm 3 .

3. The composition of claim 1 , wherein the oil phase comprises at least one triglyceride, monoglyceride, diglyceride, vegetable oil, or mineral oil.

4. The composition of claim 3 , further defined as comprising a medium chain or long chain triglyceride.

5. The composition of claim 1 , wherein the lipophilic surfactant comprises at least one sorbitan ester, bentonite, glycerol monostearate, or propylene glycol monolaurate.

6. The composition of claim 5 , further defined as comprising sorbitan stearate, sorbitan laurate, or sorbitan monopalmitate.

7. The composition of claim 1 , wherein the aqueous phase is present in an amount ranging from 0.1 to less than 50% in weight to the total weight of the composition.

8. The composition of claim 7 , wherein the aqueous phase is present in an amount ranging from 0.5 to 15% w/w.

9. The composition of claim 8 , wherein the aqueous phase is present in an amount ranging from 2 to 10% w/w.

10. The composition of claim 1 , wherein the hydrophilic therapeutic agent is a monoclonal antibody (full or fragment Fab), an anti-angiogenic molecule, a ROCK (Rho-kinases) inhibitor, a protein, WNT3A protein, a growth factor, a siRNA, an oligonucleotide, an iron chelating molecule, an anti-inflammatory molecule, an antibiotic, or a cortico-steroid.

11. The composition of claim 10 , wherein the hydrophilic therapeutic agent is ranibizumab, bevacizumab trastuzumab, cituximab, rituximab, pegaptanib, fasudil, anti-CD160 S-HLA-G, epithelium growth factors (EGF), anti-EGF, TGF (Transforming growth factor), siRNA anti-arginase, miRNA, antisense DNA, antisense RNA, deferiprone, salicylaldehyde isonicotinoyl hydrazone, epigallocatechin gallate, linezolide, clavulamic acid, macrolide, or dexamethasone including its hydrophilic derivatives.

12. The composition of claim 1 , further comprising a lipophilic therapeutic agent dissolved in the oil phase, the lipophilic therapeutic agent further defined as comprising cyclosporine A lutein, alpha-tocopherol, and/or dexamethasone palmitate.

13. The composition of claim 1 , further comprising viscosity modifying agents, pH buffering agents, and/or osmolality modifying agents.

14. The composition of claim 13 , further defined as comprising at least one of a hydrogel of sodium hyaluronate, carbopol gel, hydroxyethyl cellulose, dextran, carboxymethyl cellulose, PEG, polyvinyl alcohol, collagen; phosphate, citrate, tris, histidine, or acetate buffer; NaCl, KCl, CaCl 2 , glycerol, mannitol, alpha-trehalose and/or propylene glycol.

15. The composition of claim 1 , further comprising one or more pharmaceutically acceptable excipient.