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Cartilage targeting double-drug-loaded nano-microspheres with optical thermal response characteristic and preparation method and application thereof

A photothermal response, nano-microsphere technology, applied in the field of biomedical engineering, can solve the problems of cytotoxicity, unknown efficacy, limited application, etc., and achieve the effect of delaying cartilage degeneration, good stability and strong ability

Active Publication Date: 2020-12-04
SHANGHAI FIRST PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] When chondrocytes are stimulated by a variety of external inflammatory factors, mechanical stress and other factors, the level of intracellular oxidative stress is often at a high level, and the level of intracellular reactive oxygen species is therefore high; and previous studies have shown that antioxidants play a role in the treatment of OA. has great potential, but some oxygen radical scavengers exhibit potential cytotoxicity, which also limits its further application
Recent studies have found that bilirubin, one of the metabolites of bile acids, has multiple biological functions, including free radical scavenging, but its efficacy in OA treatment is still unknown

Method used

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  • Cartilage targeting double-drug-loaded nano-microspheres with optical thermal response characteristic and preparation method and application thereof
  • Cartilage targeting double-drug-loaded nano-microspheres with optical thermal response characteristic and preparation method and application thereof
  • Cartilage targeting double-drug-loaded nano-microspheres with optical thermal response characteristic and preparation method and application thereof

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Embodiment 1

[0031] (1) Materials and methods

[0032] 1. Synthesis and characterization of nanospheres:

[0033] (1) Dissolve equal proportions of F127 and 1,3,5-trimethylbenzene (TMB) (each 0.36g) in water (65ml);

[0034] (2) Evenly dissolve 90mg Tris in 10ml of water, mix with the solution of (1), and then use ultrasonic treatment for 10 minutes;

[0035] (3) Dissolve dopamine (60 mg) evenly in 5 ml of water, and then add it dropwise to the solution of (2);

[0036] (4) Stir the mixed solution slowly (300rpm) in the dark for 4h, centrifuge the reaction system at 18000rpm, and disperse the obtained product in a mixture of ethanol (100ml) and acetone (50ml), and then wash 3 times to remove the template;

[0037] (5) After the template was removed, 20 mg of MPDA was weighed and dispersed in water, and then 5 mg of rapamycin was added. Stir overnight at room temperature in the dark. After vacuum treatment, centrifuge and collect the supernatant, and after washing, it is Rap@MPDA;

[0...

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Abstract

The invention relates to a preparation method and application of cartilage targeting double-drug-loaded nano-microspheres with the optical thermal response characteristic. According to thecartilage targeting double-drug-loaded nano-microspheres with the optical thermal response characteristic, small-particle-size mesoporous polydopamine is used as a matrix, the matrix is sequentially subjected toa cyclic reaction with FeCl3. 6H2O and H3BTC, and the surface of the mesoporous polydopamine is modified to form a metal organic framework. After the synthesized MPDA-MOF (referred to as MPM hereinafter) nano-microspheres react with EDC and NHS solution, carboxyl groups on the surface of MOF are activated, and by connection with amino groups in type II collagen targeting peptide (WYRGRL), composite nano-microspheres (MPMW) of which surfaces are loaded with a cartilage targeting peptide are formed. Double factors of bilirubin (Br) and rapamycin (Rap) are correspondingly loaded in pore passagesof an MOF shell layer and the mesoporous polydopamine, and finally, the RB@MPMW is obtained. The nano-microspheres have the advantages of high optical thermal response characteristic, good biocompatibility, active cartilage targeting, delay on in-vivo cartilage degeneration and the like, and can be used for the targeted therapy of osteoarthritis cartilage degeneration.

Description

technical field [0001] The invention relates to the technical field of biomedical engineering, in particular to a double drug-loaded nano-microsphere targeting cartilage with photothermal response characteristics, a preparation method and application thereof. Background technique [0002] Osteoarthritis (OA) is a chronic degenerative disease of cartilage. Due to the lack of nerves and blood vessels, articular cartilage has very poor proprioception of pain. After the cartilage is damaged, its self-repair ability will be further reduced, which will further aggravate the damage. Previous studies have shown that physical and drug interventions in the early stages of cartilage degeneration can prevent the progression of OA to a certain extent. Therefore, the use of imaging techniques to diagnose early osteoarthritis and implement effective interventions is an important step for the comprehensive treatment and prevention of OA. An effective solution is provided. Several therape...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/54A61K47/64A61K41/00A61K31/436A61K49/00A61P19/02A61P29/00B82Y5/00B82Y40/00A61K31/409
CPCA61K47/54A61K47/6935A61K47/6435B82Y5/00B82Y40/00A61P19/02A61P29/00A61K9/0009A61K49/0002A61K41/0042A61K31/436A61K31/409A61K2300/00Y02A50/30
Inventor 薛松马金忠周小军桑伟林
Owner SHANGHAI FIRST PEOPLES HOSPITAL
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