Lipid nanoparticles for the treatment of ocular diseases
OwnerElena SÁNCHEZ LÓPEZ, María Luisa GARCÍA LÓPEZ +2inventors
InventorsElena SÁNCHEZ LÓPEZ, María Luisa GARCÍA LÓPEZ, Lorena BONILLA VIDAL, Marta ESPINA GARCÍA
Life of this patent
Estimating the term…
Abstract
The present invention relates to a composition comprising lipid nanoparticles comprising rosehip oil, at least one solid lipid, at least one surfactant, and optionally at least one active ingredient, as well as their use in a method of treating ocular diseases, such as for example dry eye disease.
Claims15
A composition comprising lipid nanoparticles, said lipid nanoparticles comprising a) rosehip oil;
- b) at least one solid lipid;
- c) at least one surfactant;
- d) optionally, at least one active ingredient;
- wherein the composition is suitable for ocular topical administration.
The composition of any one of the preceding claims, wherein the solid lipid is selected from monoglycerides, diglycerides, triglycerides, cholesterols, steroids, fatty alcohols, glycerol esters glyceryl tridecanoate, glycerol trilaurate, glyceryl trimyristate, glyceryl tripalmitate, glyceryl tristearate, Hydrogenated coco-glycerides, Hard fat types, mixtures of triglycerides and/or diglycerides and/or monoglycerides and/or glycerol, acyl glycerols, glyceryl monostearate, glyceryl distearate, glyceryl monooleate, glyceryl dibehenate, glyceryl palmitostearate, waxes, cetyl palmitate, fatty acids, stearic acid, palmitic acid, decanoic acid, behenic acid, glycerol stearate citrate, polyethylene glycol monostearate, cyclodextrin para-acyl-calix-arenes, or mixtures thereof, preferably glyceryl dibehenate.
The composition of any one of the preceding claims, wherein the cationic surfactant is selected from the group consisting of dimethyldioctadecylammonium bromide (DDAB), dioleoyl phosphatidylethanolamine, 1,2-distearyloxy-N,N-dimethyl-3-aminopropane, 1,2 dioleyl-oxy-N,N-dimethyl-3-aminopropane, 1,2-dilinoleyloxy-N,N-dimethyl-3-aminopro-pane, 1,2-dilinolenyloxy-N,N-dimethyl-3-aminopropane, cetyltri-methylammonium bromide, 3ß-[N(N′,N′-dimethylaminoethane)-carbamoyl]cholesterol, 1,2-dioleoyl-3-trimethylammonium-propane, 1,2-dimyristoyl-3-trimethylammonium-propane, 1,2-stearoyl-3-tri-methylammonium-propane, N-(4-carboxybenzyl)-N,N-dimethyl-2,3-bis(oleoyloxy) propan-1-aminium, 1-Palmitoyl-2-oleoyl-sn-glycero-3-phosphoethanol-amine, N,N-di-(P-stearoylethyl)-N,N-dimethyl-ammonium chloride, benzalkonium chloride, cetylpyridinium chloride, cetrimide, N-[1-(2,3-dioleoyloxy)propyl]-N,N,N-trimethylammonium chloride, 1,2-dilineoyl-3-dimethylammonium-propane, 1,2-dilinoleyloxy-3-N,N-dimethylaminopropane, 1,2-dilinoleyloxy-keto-N,N-dimethyl-3-aminopropane, 1,2-dilinoleyl-4-(2-dimethylaminoethyl)-[1,3]-dioxolane(3-o-[2″-(meth oxypolyethyleneglycol 2000) succinoyl]-1,2-dimyristoyl-sn-glycol, R-3-[(ω-methoxy-poly(ethyleneglycol)2000) carbamoyl]-1,2-dimyristyloxlpropyl-3-amine, cetyltrimethyl-ammonium bromide, octadecylamine, 1-oleoyl-rac-glycerol, octadecyl quaternized carboxymethyl chitosan, hexadecyl trimethyl ammonium bromide, preferably wherein the cationic surfactant is dimethyl-dioctadecyl-ammonium bromide (DDAB).
The composition of any one of the preceding claims, wherein the non-cationic surfactant is selected from the group consisting of polysorbate 80, soya lecithin, sodium dodecyl sulphate, polysorbate 20, polysorbate 40, polysorbate 60, PEG-30 glyceryl stearate, cholic acid, phosphatidyl choline, phospholipids with phosphatidycholine, egg lecithin, poloxamer 188, poloxamer 407, poloxamer 184, poloxamer 338, poloxamine 908, tyloxopol, taurocholate sodium salt, taurodeoxycholicacid sodium salt, sodium glycocholate, sodium oleate, cholesteryl hemisuccinate, butanol, sodium cholate, nonionic polyoxyethylene, non-ionic amphiphilic surfactant with an alkyl moiety and an ethylene oxide chain, palmitic acid, stearic acid, mixtures of palmitic and stearic acid, lecithin, polyglycerol 6-distearate, caprylyl/capryl glucoside, coco-glucoside, sucrose palmitate, sucrose stearate, sucrose distearate, tyloxapol, lecithin, cetylpyridinium chloride, sorbitan laurate, polyethylene glycol ether of cetyl or stearyl alcohol, castor oil polyoxyethylene ether, macrogolglycerol ricinoleate, dioctyl sodium sulfosuccinate, monooctylphosphoric acid sodium, hexadecyl trimethyl ammonium bromide, polyvinyl alcohol, polyoxyethylene (40) stearate, polyethylene glycol-polypropylene glycol-polyethylene glycol triblock copolymer, olyoxyethylene nonylphenyl ether, hexadecyltrimethylammonium bromide, sodium dodecyl sulfate, sodium cholate, stearate sodium hydrolysed polyvinyl alcohol 9000-10000 MW, dioctyl sulfosuccinate, taurocholate, 4-dodecylbenzenesulfonic acid, long chain carboxylic acid, alkyldiphenyloxide disulfonate, or mixtures thereof, preferably polysorbate 80.
The composition of any one of the preceding claims, wherein the at least one active ingredient is encapsulated in the lipid nanoparticles.
The composition of any one of the preceding claims, wherein the at least one active ingredient is apigenin.
The composition of any one of the preceding claims, wherein said lipid nanoparticles further comprise a coating, preferably wherein said coating comprises hyaluronic acid.
The composition of any one of the preceding claims, wherein said lipid nanoparticles comprise
- a. 0.01-30% (w/v) rosehip oil
- b. 1.0-50% (w/v) solid lipid, preferably glyceryl dibehenate;
- c. 0.001-10% (w/v) cationic surfactant, preferably DDAB;
- d. optionally 0.00-10% (w/v) non-cationic surfactant, preferably polysorbate 80;
- e. optionally 0.00-10% (w/v) active ingredient, preferably apigenin.
The composition of any one of the preceding claims, wherein said lipid nanoparticles comprise
- a. 2.5-12.5% (w/v) rosehip oil
- b. 1.0-30% (w/v) solid lipid, preferably glyceryl dibehenate;
- c. 0.025-0.5% (w/v) cationic surfactant, preferably DDAB;
- d. 1.0-5.0% (w/v) non-cationic surfactant, preferably polysorbate 80;
- e. optionally 0.1-2.5% (w/v) active ingredient, preferably apigenin.
The composition of any one of the preceding claims, wherein said lipid nanoparticles comprise 1.0-6.5% (w/v) solid lipid and 0.03-0.4% (w/v) cationic surfactant.
The composition of any one of the preceding claims, wherein said lipid nanoparticles comprise
- a. 2.5-10% (w/v) rosehip oil
- b. 1.0-6.5% (w/v) solid lipid, preferably glyceryl dibehenate;
- c. 0.03-0.4% (w/v) cationic surfactant, preferably DDAB;
- d. 3.0-5.0% (w/v) non-cationic surfactant, preferably polysorbate 80;
- e. optionally 0.1-2.5% (w/v) active ingredient, preferably apigenin.
The composition of any one of the preceding claims, wherein said lipid nanoparticles comprise
- a. 3.0% (w/v) rosehip oil,
- b. 4.5% (w/v) glyceryl dibehenate,
- c. 0.05% (w/v) DDAB,
- d. 3.5% (w/v) polysorbate 80,
- e. optionally 0.1% (w/v) apigenin.
The composition of any one of the preceding claims, wherein the lipid nanoparticles further comprise from 0.00001%-0.001% (w/v), preferably 0.0001% (w/v) hyaluronic acid, more preferably wherein said hyaluronic acid coats the lipid nanoparticles.
A composition comprising lipid nanoparticles according to any one of the preceding claims for use in the treatment, amelioration or prevention of ocular diseases, such as ocular inflammation, glaucoma, ocular tumors, bacterial and viral infections of the eye, age-related macular degeneration, cataracts, diabetic retinopathy, or Dry Eye Disease (DED).
Dependencies are inferred from the claim text.