Curcumin micelle eye drop and preparation method thereof

Abstract

The invention discloses a curcumin micelle eye drop. The eye drop comprises curcumin as a main drug, an antiseptic, an isotonic regulator, and also comprises a polyethylene caprolactam-polyvinyl acetate-polyethylene glycol copolymer as a drug adjuvant, and dequalinium chloride as a mitochondrial targeting modifier and a stabilizer, a mass ratio of the curcumin main drug to the polyethylene caprolactam-polyvinyl acetate-polyethylene glycol block copolymer drug adjuvant is 1:12-1:20, and a mass ratio of dequalinium chloride to the polyethylene caprolactam-polyvinyl acetate-polyethylene glycol copolymer drug adjuvant is 1:20-1:40. The administration concentration of the curcumin micelle eye drop prepared in the invention can reach 5mg / ml, and the eye drop has the advantages of small micelle particle size, uniform distribution range, good drug stability, reduction of the administration irritation, improvement of the drug absorption of cornea, reduction of the administration concentration, prolongation of the action time of the drug, reduction of the administration frequency, improvement of the patient compliance, and very good economy.

Description

technical field [0001] The invention relates to a curcumin eye drop, in particular to a curcumin micelle eye drop and a preparation method thereof. Background technique [0002] The prevalence of diabetes in my country has increased rapidly in recent years, and diabetes has become a major public health problem in my country. The patient's long-term hyperglycemia state leads to lesions in various tissues and organs throughout the body, causing serious diabetes-related complications, including diabetic keratopathy. In addition, diabetic patients are prone to delayed corneal epithelial healing or even non-healing during corneal trauma or corneal surgery. Blindness is difficult to treat, the prognosis is poor, and the patient's economic and mental burden is serious. At present, the clinical treatment methods for diabetic keratopathy are limited. Therefore, it is of great clinical significance to study new therapeutic targets and effective prevention and treatment measures for ...

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Problems solved by technology

But it also has some disadvantages: (1) As a polysaccharide polymer material, chitosan itself cannot form micelles, so a large amount of surfactants and co-surfactants need to be added to help form chitosan glue However, adding a large amount of surfactants and co-surfactants will inevitably cause ocular surface irritation and safety hazards in topical ocular application; (2) Because chitosan itself cannot form micelles, adding a large amount of surfactants and co-surfactants Auxiliary formation of micelles after the surfactant leads to low drug loading of the micelles, which directly leads to a low concentration of the main drug curcumin in eye drops. Therefore, the concentration of the main drug curcumin in this invention is only 0.005%-0.02%. Treatment of diabetic keratopathy largely ineffective

[0005] Shandong Provincial Institute of Ophthalmology prepared curcumin nano-micelle eye drops by adopting its applied and authorized invention patent "A Cyclosporine A Micellar Eye Drops and Its Preparation Method" (ZL201210529616.9). In the therapeutic effect evaluation study, ocular surface administration of curcumin nanomicelles can partially correct the redox imbalance in the cornea, but the therapeutic effect is limited because the micelles cannot effectively target into the mitochondria

In addition, in the follow-up development process of the Shandong Provincial Institute of Ophthalmology, it was found that the micelles constructed solely based on polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol copolymer and its aqueous solution were stored, and cyclosporine A would gradually Freed from micelles, the effective stability of its aqueous solution at room temperature is only 3 months

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