Double-layer microspheres loaded with parecoxib, interleukin-4 and bovine serum albumin and used for treating osteoarthritis and preparation method of double-layer microspheres

A technology of bovine serum albumin and parecoxib, which is applied in the field of double-layer microspheres and its preparation, can solve the problems of high incidence of adverse reactions, poor patient compliance, and limited duration, and achieve good anti-inflammatory efficacy and cartilage. Protective activity, reduction in inflammatory cell infiltration, mitigating effects of erosion damage

Active Publication Date: 2022-01-04
SHANDONG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] For the treatment of osteoarthritis, selective COX-2 inhibitor NSAIDs (such as celecoxib, etoricoxib, etc.) are currently widely used clinically, but the incidence of gastrointestinal adverse reactions is still high, and oral NSAIDs The cardiovascular risk of drugs should not be underestimated, and the compliance of patients with long-term oral drugs is poor
Due to the particularity of the site of arthritis, intra-articular injections are recommended for those patients in whom non-drug interventions or symptom-relieving drugs are ineffective, in an attempt to more directly target the underlying pathophysiological process, but the effect of a single dose of direct intra-articular injection persists Time-limited, therefore, repeated applications are often required to maintain prolonged pain relief, which in turn can lead to adverse effects such as infection, muscle weakness, and hormonal imbalances

Method used

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  • Double-layer microspheres loaded with parecoxib, interleukin-4 and bovine serum albumin and used for treating osteoarthritis and preparation method of double-layer microspheres
  • Double-layer microspheres loaded with parecoxib, interleukin-4 and bovine serum albumin and used for treating osteoarthritis and preparation method of double-layer microspheres
  • Double-layer microspheres loaded with parecoxib, interleukin-4 and bovine serum albumin and used for treating osteoarthritis and preparation method of double-layer microspheres

Examples

Experimental program
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Effect test

Embodiment 1

[0035]Example 1: A method for preparing the inner layer of microspheres loaded with parecoxib, interleukin-4 and bovine serum albumin for the treatment of osteoarthritis

[0036] (1) Dissolve 1ug of interleukin-4 (IL-4) in 100ul of PBS solution containing 0.1% (w / v) model protein bovine serum albumin as the inner water phase;

[0037] (2) Weigh 50 mg of the inner carrier material ester-terminated poly(lactic-co-glycolic acid) copolymer OH-PLGA75 / 25-COOR (LA:GA is 75:25, molecular weight is 75,000) and dissolve it in 0.5 mL of dichloromethane to form a concentration 100mg / mL solution is used as the oil phase, and 1% (w / v) polyvinyl alcohol (PVA) is prepared as the external water phase;

[0038] (3) First add the inner water phase dropwise into the oil phase in which the carrier material is dissolved at a water phase / oil phase ratio of 1:5, and then cut the formed W1 / O1 type emulsion, and then add the emulsion dropwise to 2.5mL of 2% (w / v) PVA at a ratio of 1:5, and obtain W1-...

Embodiment 2

[0040] Example 2: A preparation method of bilayer microspheres loaded with parecoxib, interleukin-4 and bovine serum albumin for the treatment of osteoarthritis

[0041] (1) Redissolve the single-layer microspheres obtained in Example 1 with distilled water to make a new inner water phase with a volume of 0.5 mL. The outer carrier material is hydroxyl-terminated poly(lactic-co-glycolic acid) 50 / 50 OH-PLGA-OH50 / 50 (LA:GA 50:50, molecular weight 8000) and 10mg parecoxib were dissolved in 2.5mL dichloromethane to form a solution with a carrier concentration of 50mg / mL as the oil phase;

[0042] (2) First add the inner water phase dropwise to the oil phase in which the carrier material is dissolved at a water phase / oil phase ratio of 1:5, and cut at a speed of 10,000 rpm for 2 minutes to form a W / O emulsion, and then Add the emulsion dropwise to 25mL, 2% (w / v) PVA at a ratio of 1:10, and shear at the same speed for 2 minutes with a homogenizer to obtain a W3-O2-W4 type double emu...

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Abstract

The invention relates to double-layer microspheres loaded with parecoxib, interleukin-4 and bovine serum albumin and used for treating osteoarthritis and a preparation method of the double-layer microspheres, and belongs to the technical field of drug carrier research. Drugs carrying different physical and chemical properties are prepared by two-time multiple emulsion solvent volatilization method, the purpose of the invention is to solve the bottleneck problems of clinically restricting osteoarthritis drug treatment at present or meet urgent requirements of people for handling of pain and mobility inconvenience problems caused by inflammatory reaction during osteoarthritis attack, infection problem caused by repeated injection in articular cavity injection, and the problem of poor patient medication dependency caused by cardiotoxicity and gastrointestinal reaction caused by oral administration of non-steroidal anti-inflammatory drugs, and long-term chronic properties of osteoarthritis.

Description

technical field [0001] The invention relates to a double-layer microsphere loaded with parecoxib, interleukin-4 and bovine serum albumin for treating osteoarthritis and a preparation method thereof, belonging to the technical field of drug carrier research. Background technique [0002] For the treatment of osteoarthritis, selective COX-2 inhibitor NSAIDs (such as celecoxib, etoricoxib, etc.) are currently widely used clinically, but the incidence of gastrointestinal adverse reactions is still high, and oral NSAIDs The cardiovascular risk of drugs cannot be underestimated, and the compliance of long-term oral drug patients is poor. Due to the particularity of the site of arthritis, intra-articular injections are recommended for those patients in whom non-drug interventions or symptom-relieving drugs are ineffective, in an attempt to more directly target the underlying pathophysiological process, but the effect of a single dose of direct intra-articular injection persists Ti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/16A61K38/20A61K31/42A61K47/42A61K47/34A61K47/69A61P19/02A61P29/00A61P19/08
CPCA61K9/19A61K9/1658A61K31/42A61K38/2026A61P19/02A61P29/00A61P19/08A61K9/1682A61K9/167A61K9/1647A61K47/6927A61K2300/00
Inventor 林贵梅邱胜男傅相蕾
Owner SHANDONG UNIV
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