Liposome for delivery to posterior segment of eye and pharmaceutical composition for disease in posterior segment of eye

摘要

The invention provides a liposome for delivery to the posterior segment of the eye, comprising (A) a phospholipid, (B) a charged substance, and/or (C) a membrane-reinforcing substance; the liposome having a rigidity that provides the liposome with cell membrane permeability, and having a mean particle diameter of 1 μm or less; and a pharmaceutical composition for a disease in the posterior segment of an eye, comprising a drug encapsulated in the liposome. The liposome is delivered to the posterior segment of the eye by instillation, and is non-cytotoxic; and the pharmaceutical composition for a disease in the posterior segment of the eye comprises the liposome.

主权项

1. A method for treating a disease in the posterior segment of the eye, comprising administering locally to the eye of a subject having a disease in the posterior segment a pharmaceutical composition which is in a form of an ophthalmic solution or an ophthalmic ointment and comprises a liposome encapsulating a drug, wherein the liposome comprises
(A) at least one phospholipid selected from the group consisting of distearoylphosphatidylcholine, dipalmitoylphosphatidylcholine, dimyristoylphosphatidylcholine, dilauroylphosphatidylcholine, egg phosphatidylcholine, and hydrogenated phosphatidylcholine, (B) at least one negatively charged substance selected from the group consisting of dicetyl phosphate, and dipalmitoylphosphatidylglycerol, and (C) a membrane-reinforcing substance; and wherein the liposome has a rigidity that provides the liposome with cell membrane permeability and a mean particle diameter of 1 μm or less, and wherein the disease in the posterior segment of the eye is at least one disease selected from the group consisting of age-related macular degeneration, diabetic retinopathy, and uveitis, thereby treating a disease in the posterior segment of the eye, and wherein the drug is at least one drug selected from the group consisting of carteolol hydrochloride, nipradilol, dorzolamide hydrochloride, acetazolamide, glutathione, memantine, fluorometholone, prednisolone, betamethasone, dexamethasone, indomethacin, dichlofenac sodium, and bromfenac sodium.