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Preparation method and application of prodrug-loaded drug delivery system targeting brain metastases inhibiting mfsd2a

A technology for brain metastases and targeted drug delivery, applied in pharmaceutical formulations, drug combinations, anti-tumor drugs, etc., can solve the problems of large toxic and side effects of brain metastases at the blood-brain barrier, reduce normal tissue accumulation, and simplify the production process. , high operability effect

Active Publication Date: 2022-03-15
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The purpose of the present invention is to solve the problem that the traditional nano drug delivery system cannot effectively cross the blood-brain barrier to effectively treat brain metastases and reduce toxic side effects, that is, it cannot achieve effective therapeutic concentrations in the brain tumor area and reduce toxicity to normal brain tissue and surrounding tissues. , proposed a preparation method and application of a prodrug-loaded brain metastases targeting nano drug delivery system that can inhibit Mfsd2a and promote blood-brain barrier transcellular transport

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  • Preparation method and application of prodrug-loaded drug delivery system targeting brain metastases inhibiting mfsd2a
  • Preparation method and application of prodrug-loaded drug delivery system targeting brain metastases inhibiting mfsd2a
  • Preparation method and application of prodrug-loaded drug delivery system targeting brain metastases inhibiting mfsd2a

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preparation example Construction

[0062] The present invention selects polymer materials, functional linker molecules, brain microvascular endothelial cell targeting ligands, and brain metastases targeting ligands, which can inhibit Mfsd2a functional molecules and anti-brain metastases prodrugs, and use biodegradable polymer materials As the basic carrier, prepare internally carrying Mfsd2a inhibitory functional molecules and anti-brain metastases prodrugs, surface-modified brain microvascular endothelial cell targeting ligands and brain metastases targeting ligands, the nano drug delivery system can improve Efficiency of the nano drug delivery system crossing the blood-brain barrier and targeting brain metastases under the action of brain metastases-targeting ligands; the internally loaded anti-brain metastases prodrug can also specifically induce the apoptosis of brain metastases cells , to reduce toxicity to normal brain tissue and surrounding tissues. The invention is expected to improve the targeting effi...

Embodiment 1

[0095] Weigh 50 mg polylactic acid-glycolic acid-polylysine and dissolve it in 1 mL ethyl acetate as the oil phase, weigh 0.5 mg tunicamycin and dissolve it in 25 μL DMSO, and weigh 0.5 mg hyaluronic acid-A Dissolve tunicamycin in 75 μL water, add tunicamycin solution dropwise to the vortexed oil phase, then add 50 μL water dropwise, then add hyaluronic acid-doxorubicin solution dropwise to the vortexed oil phase, sonicate Emulsify to form a water-in-oil emulsion; then add the emulsion dropwise to the vortexed 2.5% polyvinyl alcohol solution, and ultrasonically emulsify to form a water-in-oil water-in-water emulsion; quickly pour this emulsion into a 0.3% polyvinyl alcohol solution, stir Volatilize until there is no ethyl acetate odor; the obtained nanoparticle suspension is subjected to high-speed centrifugation at 30,000 rpm for 20 minutes to obtain nanoparticle precipitation; the nanoparticle precipitation is ultrasonically dispersed in an appropriate amount of pH 7.3 phosph...

Embodiment 2

[0097] Weigh 50 mg polylactic acid-glycolic acid-polylysine and dissolve it in 1 mL ethyl acetate as the oil phase, weigh 0.5 mg tunicamycin and dissolve it in 25 μL DMSO, and weigh 0.5 mg hyaluronic acid-A Dissolve tunicamycin in 75 μL water, add tunicamycin solution dropwise to the vortexed oil phase, then add 50 μL water dropwise, then add hyaluronic acid-doxorubicin solution dropwise to the vortexed oil phase, sonicate Emulsify to form a water-in-oil emulsion; then add the emulsion dropwise to the vortexed 2.5% polyvinyl alcohol solution, and ultrasonically emulsify to form a water-in-oil water-in-water emulsion; quickly pour this emulsion into a 0.3% polyvinyl alcohol solution, stir Volatilize until there is no ethyl acetate odor; the obtained nanoparticle suspension is subjected to high-speed centrifugation at 30,000 rpm for 20 minutes to obtain nanoparticle precipitation; the nanoparticle precipitation is ultrasonically dispersed in an appropriate amount of pH 7.3 phosph...

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Abstract

The invention discloses a preparation method and application of a prodrug-loaded brain metastases targeting drug delivery system that inhibits Mfsd2a. The nano drug delivery system is constructed with a biodegradable polymer material as the basic carrier, and functional molecules are loaded inside it to Inhibition of Mfsd2a and brain metastases intracellular enzyme-specific prodrugs, surface modification of brain microvascular endothelial cell targeting ligands and brain metastases targeting ligands; the nano drug delivery system can target ligands in brain microvascular endothelial cells and Mfsd2a inhibitory functional molecules efficiently penetrate the blood-brain barrier; after crossing the blood-brain barrier, the nano-drug delivery system can target and enter tumor cells under the guidance of the brain metastases targeting ligand; On the basis of targeted delivery, the body drug can further specifically act on tumor cells and reduce side effects on normal brain tissue and surrounding tissues. The above method is simple, operable and economical.

Description

technical field [0001] The invention belongs to the technical field of nano-biomedicine, and specifically relates to a preparation method and application of a prodrug-loaded brain metastases-targeting nano drug delivery system capable of inhibiting Mfsd2a and promoting blood-brain barrier transcellular transport. Background technique [0002] Brain metastases is a disease in which malignant tumors from other parts of the body metastasize to the brain. The incidence of brain metastases in cancer patients can reach 24-45%. It has become a common clinical problem in oncology. Various treatment methods (such as surgery, stereotactic radiosurgery, whole brain radiotherapy, immunotherapy, photodynamic therapy, etc.) have a series of problems in the treatment of brain metastases, resulting in a high mortality rate and poor prognosis of brain metastases. , the recurrence rate is high, and the average survival period of patients is short. [0003] Drug therapy is an efficient clinic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/61A61K47/62A61K47/69A61K31/704A61K31/7072A61K45/06A61P35/00
Inventor 韩亮鞠秀峰
Owner SUZHOU UNIV
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