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Application of resveratrol-polylactic acid long-acting nano-microspheres in preparation of anti-osteoarthritis drug

A technology for osteoarthritis and resveratrol, which is applied in the application field of resveratrol-polylactic acid long-acting nano-microspheres in the preparation of anti-osteoarthritis drugs, which can solve the problem of low bioavailability and short half-life. , hinder the application and other problems, to optimize the preparation conditions, improve the stability, improve the effect of the effect

Pending Publication Date: 2022-01-25
LUOYANG ORTHOPEDIC TRAUMATOLOGICAL HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, a large number of in vitro and in vivo anti-cancer studies have shown that resveratrol has potential anti-cancer activity against various tumors, such as breast cancer, prostate cancer, and colon cancer. After oral administration, the bioavailability is low, the half-life is short, the clearance is fast, and frequent administration is required, which hinders the clinical application
At present, there are no relevant reports on the application of resveratrol long-acting intra-articular injection preparations in the treatment of OA. To study the correlation between resveratrol and OA, and how to improve the long-acting effect of resveratrol in the body is crucial for the development of OA. The importance of treating OA

Method used

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  • Application of resveratrol-polylactic acid long-acting nano-microspheres in preparation of anti-osteoarthritis drug
  • Application of resveratrol-polylactic acid long-acting nano-microspheres in preparation of anti-osteoarthritis drug
  • Application of resveratrol-polylactic acid long-acting nano-microspheres in preparation of anti-osteoarthritis drug

Examples

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Effect test

Embodiment 1

[0033] Preparation method of resveratrol-polylactic acid long-term nano microspheres, including the following steps:

[0034] (1) 3 mg of resveratrol and 10 mg of polylactic acid were dissolved in 0.5 ml of dichloromethane, mix well, formed organic phase;

[0035] (2) Mix the above organic phase to 2% PVA solution I and other volume, under ice bath conditions, 10,000 high speed cut 3 min to form emulsion, then slowly dropped into a 5-fold volume of 2% PVA solution II, 200 rpm low speed Mix 4H organic solvent, collect microspheres;

[0036] (3) Crominrate 15 minutes of the collected microspheres in 8000 rpm, discard the supernatant, wash three nano microspheres with distilled water, then freeze and dry, collect dry powder, to obtain resveratrol-polylactic acid Nano microspheres.

Embodiment 2

[0038] Preparation method of resveratrol-polylactic acid long-term nano microspheres, including the following steps:

[0039] (1) 4.2 mg of resveratrol and 30 mg of polylactic acid were dissolved in 1 ml of dichloromethane, mix well, formed organic phase;

[0040] (2) Mix the above organic phase and 2% PVA solution I and other volume, 11000 rpm high speed cut 4 min to form emulsions, then slowly dropped into a 5-fold volume of 2% PVA solution II, 250 rpm low speed Mix 4H organic solvent, collect microspheres;

[0041] (3) Centrifuge the collected microspheres at 9000 rpm for 15 minutes, discard the supernatant, wash three nano microspheres with distilled water, then freeze and dry, collect dry powder, to obtain resveratrol-polylactic acid Nano microspheres.

Embodiment 3

[0043] Preparation method of resveratrol-polylactic acid long-term nano microspheres, including the following steps:

[0044] (1) 5 mg of resveratrol and 45 mg of polylactic acid were dissolved in 1 ml of dichloromethane, mix well, formed organic phase;

[0045] (2) Mix the above organic phase with 2% PVA solution I and other volume, under ice bath conditions, 12500 rpm high speed cut 5 min forming emulsion, then slowly dropped into a 5-fold volume of 2% PVA solution II, 300 rpm low speed Mix 4H organic solvent, collect microspheres;

[0046] (3) Centrifuge the collected microspheres for 20 minutes, discard the supernatant, wash three nano microspheres with distilled water, then freeze and dry, collect dry powder, to obtain resveratrol-polylactic acid Nano microspheres.

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Abstract

The invention discloses application of resveratrol-polylactic acid long-acting nano-microspheres in preparation of an anti-osteoarthritis drug, and belongs to the field of osteoarthritis treatment. The preparation method of the nano-microspheres comprises the following steps of: jointly dissolving resveratrol and polylactic acid in dichloromethane to form an organic phase; mixing the organic phase with a PVA solution I, performing high-speed shearing under an ice bath condition to form an emulsion, then slowly dripping the emulsion into a PVA solution II, performing stirring at a low speed to volatilize an organic solvent, and collecting microspheres; and centrifuging the collected microspheres, discarding the supernate, cleaning the nano-microspheres, and performing freeze-drying to obtain the resveratrol-polylactic acid long-acting nano-microspheres. The preparation method is simple and easy to operate; the stability of the resveratrol-polylactic acid nano-microspheres is improved by optimizing preparation conditions; the resveratrol-polylactic acid nano-microspheres are suitable for industrial popularization and application; and the nano-microspheres can remarkably relieve cartilage injury, synovitis and other symptoms after knee joint cavity injection and can be used for development of drugs for treating knee osteoarthritis.

Description

Technical field [0001] The present invention relates to the use of osteophageal arthritis, and in particular to resveratrol-polylactic acid long-term nano-microspheres in preparing antibiotic arthritis drugs. Background technique [0002] OsteoartHritis, OA is a chronic muscle skeletal system disease. In the clinical, pain is the main symptoms of its performance, specifically the pain, joint stiffness and joint friction. According to reports, the diseased population of the disease has gradually increased with age growth, and the prevalence of women is significantly higher than that in men. OA features cartilage degradation, joint cartilage degenerative injury, joint edge and cartilage lysontal reactive hyperplasia, the current treatment drug mainly includes analgesics, non-steroidal anti-inflammatory drugs, adrenal corticosteroids, hyaluronic acid, peroxidation The drug disaster enzyme (SOD) and D-glutinum, etc., these drugs can relieve symptoms, but do not change the process of ...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K47/34A61K31/05A61P19/02A61P29/00A61P19/04B82Y5/00B82Y40/00
CPCA61K9/5146A61K9/5192A61K9/0019A61K31/05A61P19/02A61P29/00A61P19/04B82Y5/00B82Y40/00
Inventor 秦娜魏立伟张虹
Owner LUOYANG ORTHOPEDIC TRAUMATOLOGICAL HOSPITAL
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