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ROS-responsive controlled-release ophthalmic preparation and preparation method thereof

A technology of ophthalmic preparations and responsive groups, applied in the field of biomedicine, can solve problems such as eye trauma, long-term wearing, drug side effects, etc., and achieve the effect of improving utilization, avoiding side effects, and safe and effective treatment

Active Publication Date: 2022-05-06
山东第一医科大学附属眼科医院(山东省眼科医院)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Among them, corneal stroma injection not only has the risk of causing ocular trauma and penetrating the anterior chamber, but may also cause endophthalmitis and visual impairment; drug-loaded contact lenses need to be worn for a long time, which is not conducive to the discharge of harmful substances produced in the eye, and at the same time become invisible Glasses are also one of the risk factors for keratitis, and the wearing process also affects vision and causes inconvenience in life; eye drops are non-invasive treatment and relatively convenient to use, which is generally accepted by patients
[0003] At present, the active ingredients of external ophthalmic drugs commonly used in clinical practice cannot be released in a controlled manner. After the ocular inflammation subsides, the active ingredients of external ocular drugs continue to precipitate in the eyes, which will cause drug-related side effects, such as secondary glaucoma, concurrent cataract, Corneal epithelial disease, etc.

Method used

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  • ROS-responsive controlled-release ophthalmic preparation and preparation method thereof
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  • ROS-responsive controlled-release ophthalmic preparation and preparation method thereof

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preparation example Construction

[0029] In the present invention, the preparation method of the ROS-responsive nano drug carrier preferably includes the following steps: mixing the carboxyl ROS-responsive group, ethylene glycol chitosan aqueous solution and a coupling agent, performing amidation reaction, dialysis, The intercepted product of the dialysis is dried to obtain a ROS-responsive nano drug carrier.

[0030] In the present invention, the solvent of the carboxyl ROS responsive group is preferably methanol; the concentration of the biodegradable carbohydrate compound in the biodegradable carbohydrate compound solution is preferably 5-20 μg / mL; more preferably 13.59 μg / mL.

[0031] In the present invention, the concentration of ethylene glycol chitosan in the ethylene glycol chitosan aqueous solution is preferably 0.01-1 μg / mL; more preferably 0.417 μg / mL.

[0032] In the present invention, the coupling agent is preferably N-hydroxysuccinimide (NHS) and (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide h...

Embodiment 1

[0046] Dissolve 0.816g 4-carboxyphenylboronic acid pinacol ester (EB) in 45mL methanol, add 0.025mg / mL ethylene glycol chitosan (GC) aqueous solution to 15mL, stir well, add 0.563g N-hydroxysuccinyl Imine (NHS) and 0.761g (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride) (EDC), heated to 70°C, and kept stirring for 24h. After three days of dialysis, EB-modified GC-EB was obtained by freeze-drying.

[0047] Characterized by infrared spectroscopy at 1725cm -1 A new boronic ester C=O bond appeared after the modification of phenylboronic acid, and at 714cm -1 At the B-O bond, at 1544 and 902cm -1 The stretching vibration peak of the C=C bond of the benzene ring is at the peak, which proves that the modification of phenylboronic acid for ROS-responsive molecules is successful.

Embodiment 2

[0055] Dissolve 0.01 g of GC-EB prepared in Example 1 in 15 mL of distilled water, ultrasonicate for 15 min, add 0.030 g of dexamethasone sodium phosphate (DSP) into the above solution system, and continue stirring for 24 h. GC-EB-DSP ROS-responsive nano-drug carriers were prepared by dialysis and freeze-drying.

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Abstract

The invention provides an ROS-responsive controlled-release ophthalmic preparation and a preparation method thereof, and belongs to the technical field of biological medicines. According to the invention, the ROS-responsive nano-drug carrier is adopted to entrap the active component of the externally applied drug for the eyes to obtain the controlled-release ophthalmic preparation. When the controlled-release ophthalmic preparation encounters high-content reactive oxygen species (ROS) at the eye inflammation part, the wrapping structure of the ROS response type nano-drug carrier is opened, the active ingredients of the external-use eye medicine are released, after inflammation fades, the ROS level is reduced, the ROS opening switch is closed, the release of the active ingredients of the external-use eye medicine is stopped, and the release of the active ingredients of the external-use eye medicine is stopped. Therefore, the controllable release of the active ingredients of the external medicine for eyes is realized. The ROS response type nano-drug carrier can effectively improve the utilization degree of the active ingredients of the eye external medicine, and can reduce or stop releasing after eye inflammation fades, so that side effects of the active ingredients of the eye external medicine on eyes are avoided, and safe and effective treatment of eye diseases is realized.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a ROS-responsive controllable-release ophthalmic preparation and a preparation method thereof. Background technique [0002] Corneal inflammation caused by various factors is collectively called keratitis, which is one of the common diseases in ophthalmology and one of the main blinding eye diseases in my country. The cornea is located at the front of the eyeball and is in direct contact with the outside world. It is vulnerable to damage from microorganisms, trauma, and physical and chemical stimuli and inflammation. Common treatments for corneal inflammation include eye drops, corneal stromal injections, and medicated contact lenses. Among them, corneal stroma injection not only has the risk of causing ocular trauma and penetrating the anterior chamber, but may also cause endophthalmitis and visual impairment; drug-loaded contact lenses need to be worn for a lon...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/06A61K31/661A61K31/506A61K47/36A61K47/22A61P27/02A61P29/00
CPCA61K9/08A61K9/06A61K9/0048A61K31/661A61K31/506A61K47/36A61K47/22A61P27/02A61P29/00
Inventor 高华张书平牛盼红韦超吴跃兰曾繁星刘思金
Owner 山东第一医科大学附属眼科医院(山东省眼科医院)
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