Acid-sensitive controlled-release anti-inflammatory gel as well as preparation method and application thereof

An inflammatory gel and acid-sensitive technology, applied in the field of acid-sensitive controlled-release anti-inflammatory gel and its preparation, to achieve the effects of relieving joint stress, inhibiting the body's hypermetabolic response, and inhibiting excessive inflammatory response

Inactive Publication Date: 2018-06-19
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, no research has focused on the characteristics of the pH drop caused by the accumulation of inflammatory metabolites in the joint cavity Design material structure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Prepare 20mg / mL hyaluronic acid (HA, molecular weight 375kDa) aqueous solution, prepare 2.24mg / mL 3-aminophenyl borate hydrochloride (APBA) solution, mix 10mL APBA solution with 25mL HA solution, stir at room temperature for 10min, then add 10mL Freshly prepared 17.9 mg / mL 4-(4,6-dimethoxytriazin-2-yl)-4-methylmorpholine hydrochloride (DMTMM) solution was stirred and reacted at room temperature for 24 hours. After the product was precipitated in 800 mL of cold ethanol, it was collected by centrifugation and dried in vacuum. The resulting solid was dissolved in 50 mL of aqueous solution, dialyzed through a dialysis bag (molecular weight cut-off 8 kDa) for 96 hours, and then freeze-dried to obtain about 400 mg of phenylboronic acid-modified hyaluronic acid solid.

[0024] The prepared phenylboronic acid-modified hyaluronic acid (HA-APBA) was made into a 2mg / mL aqueous solution, and a series of tannic acid (TA) solutions with concentrations of 1mM, 2mM, 5mM, 10mM, 20mM, and...

Embodiment 2

[0026] Prepare 50mg / mL HA (molecular weight 50kDa) aqueous solution, prepare 11.2mg / mL APBA solution, mix 20mL APBA solution and 50mL HA solution, stir at room temperature for 10min, add 100mL freshly prepared 17.9mg / mL DMTMM solution, and stir at room temperature for 12 Hour. After the product was precipitated in 1 L of cold ethanol, it was collected by centrifugation and dried in vacuo. The resulting solid was dissolved in 50 mL of aqueous solution, dialyzed through a dialysis bag (molecular weight cut-off 8 kDa) for 48 hours, and then freeze-dried to obtain about 2 g of a solid.

[0027] The prepared HA-APBA was made into a 5mg / mL aqueous solution, and a 125mM TA solution was prepared. Mix 0.5mL HA-APBA solution with 0.5mL TA solution, adjust the initial pH value of the mixture to 5 with 100mM hydrochloric acid solution, and stir magnetically for 10min. Phosphate buffer solution with pH 7.4 was slowly added dropwise to increase the pH value of the solution to prepare hyalu...

Embodiment 3

[0030] Prepare 10mg / mL HA (molecular weight 1000kDa) aqueous solution, prepare 6.72mg / mL APBA solution, mix 10mL APBA solution with 20mL HA solution, stir at room temperature for 10min, then add 15mL freshly prepared 17.9mg / mL DMTMM solution, stir and react at room temperature for 24 hours . After the product was precipitated in 500 mL of cold ethanol, it was collected by centrifugation and dried in vacuo. The resulting solid was dissolved in 60 mL of aqueous solution, dialyzed through a dialysis bag (molecular weight cut-off 100 kDa) for 96 hours, and then freeze-dried to obtain a white solid.

[0031] The prepared HA-APBA was formulated into a 2mg / mL aqueous solution, stirred thoroughly to dissolve, and a 2mM TA solution was prepared. Mix 0.5mL HA-APBA solution with 0.5mL TA solution, adjust the initial pH value of the mixture to 5 with 100mM hydrochloric acid solution, and stir magnetically for 10min. Slowly add pH7.4 phosphate buffer solution dropwise to increase the pH v...

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Abstract

The invention discloses acid-sensitive controlled-release anti-inflammatory gel. The gel is formed by phenylboronic acid modified hyaluronic acid and tannic acid under the neutral to slightly alkalinecondition, and tannic acid can be released under the acidic condition. Amiloride and analogues or non-steroidal anti-inflammatory drugs thereof can be added to the anti-inflammatory gel. The invention also discloses a preparation method of the acid-sensitive controlled-release anti-inflammatory gel. The method comprises two steps including preparation of phenylboronic acid modified hyaluronic acid and preparation of the acid-sensitive controlled-release anti-inflammatory gel. The invention also discloses an application of the acid-sensitive controlled-release anti-inflammatory gel in preparation of drugs for treating physiological and pathologic change related diseases caused by decrease of pH value due to gathering of inflammatory metabolites. The gel has the lubricating function of hyaluronic acid, can relieve the stress of joints and promote backflow and update of metabolism, also has the non-specific anti-inflammatory, antioxidation, anti-effusion and analgesia functions of tannicacid, can inhibit excessive inflammatory response and body hypermetabolic reaction and is a new controlled-release anti-inflammatory gel.

Description

technical field [0001] The invention belongs to biomedical materials, in particular to an acid-sensitive controlled-release anti-inflammatory gel and its preparation method and application. Background technique [0002] Rheumatoid arthritis is a clinical syndrome of unknown etiology, characterized by chronic, polyarticular synovial inflammation, and extra-articular lesions. %, is one of the main causes of loss of labor force and disability. The destruction of articular cartilage and bone tissue is the root cause of disability, so actively looking for the key links leading to articular cartilage destruction and pathophysiological changes of bone tissue is the focus of prevention and treatment. In the normal physiological environment of the body, the pH is very precisely regulated to achieve a stable internal environment. Under some physiological and pathological conditions such as inflammation, ischemia and tumor tissue, the acidification of the tissue can reduce the pH valu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61K31/4965A61K31/7024A61K31/728A61K9/06A61K47/61A61P29/00A61P19/02
Inventor 姚琛范东晓周宾
Owner SOUTHEAST UNIV
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