검색 상세

Development of an Ophthalmic formulation for the Treatment of Glaucoma using the Acrylated Chitosan coating Nanoparticles

초록/요약

Glaucoma is a typical geriatric ophthalmologic disease, and the number of patients is increasing as the aging population increases. One of several risk factors involved in the development of glaucoma is intraocular pressure. The increased pressure inside the eye and leads to degeneration of the optic nerve and gradual loss of vision. Current treatments include eye drop and intraocular injection and so on. In case of eye drops, less than 1% of the administered drug reaches the eye. There are several factors, for example, to the specific structure of cornea as stacked of water-soluble layer and the oil-soluble layer, rapid turn over rate of aqueous humor and long diffusion distance. Intraocular injection causes side effects and economic costs caused by repeated infusion to the patient. Therefore, a time-controlled drug delivery system is needed, to deliver drugs more safely and efficiently into the eyeballs and reduce the number of drug injection. The mechanism of glaucoma treatment is as follows. When the drug is dropped on the surface of the cornea, the drug permeates the cornea and flows into the anterior aqueous humor. Drugs move forward in the vitreous body, increase the amount of outflow, lower intraocular pressure, and this is the principle of the treatment. In the case of existing drugs, the efficiency is low due to the drug is a single molecule and only a 2-3% of the drug penetrates the cornea. The remaining drugs are washed by tears or moved to other organs, and there is a risk of causing side effects. The Eye drop medicine formulations using nanoparticles we made, drugs do not exist as a single molecule but it is supported on albumin particles. These nanoparticles have increased retention time at the surface of the cornea and induce sustained release of the drug with high efficiency. This can reduces the amount of drugs that diffuse throughout the body due to the circulation of the aqueous humor. We coated acrylated chitosan on the drug-loaded albumin nanoparticles and it has three purposes. First, increasing the retention time at the surface of the cornea to allow sustained release. Second, the coating layer is slowly decomposed to aim for sustained release. Third, reduces drug release when storing the drug-loaded particles before eye drop injection into the eyes. We developed a 200~300nm sized Acrylated chitosan-coated nanomedicine, loaded with latanoprost, a glaucoma treatment drug. We examined the efficiency of nanomedicine compared with ordinary eye drops and confirmed by pharmacodynamics aspect and distribution of nanoparticles in intraocular tissue as ciliary body, iris, vitreous and retina.

more