Preparation method and application of prodrug-supported metastatic encephaloma targeted drug-delivery system for inhibiting Mfsd2a

A technology for brain metastases and targeted drug delivery, which can be applied in pharmaceutical formulations, antineoplastic drugs, drug combinations, etc., can solve the problem of high toxicity and side effects of brain metastases in the blood-brain barrier, and achieve the reduction of normal tissue accumulation, novel design, The effect of simple production process

Active Publication Date: 2019-06-18
SUZHOU UNIV
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  • 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-supported metastatic encephaloma targeted drug-delivery system for inhibiting Mfsd2a
  • Preparation method and application of prodrug-supported metastatic encephaloma targeted drug-delivery system for inhibiting Mfsd2a
  • Preparation method and application of prodrug-supported metastatic encephaloma targeted drug-delivery system for 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 an application of a prodrug-supported metastatic encephaloma targeted drug-delivery system for inhibiting Mfsd2a. A nano drug-delivery system is constructed by adopting a biodegradable high polymer material as a basic carrier, functional molecules for inhibiting Mfsd2a and a metastatic encephaloma enzyme specificity prodrug are loaded in the nano drug-delivery system, and the nano drug-delivery system is modified with BMEC (brain microvascular endothelial cell) targeted ligands and metastatic encephaloma targeted ligands on the surface; the nanodrug-delivery system can efficiently penetrate blood brain barrier under the action of the BMEC targeted ligands and the Mfsd2a inhibiting functional molecules; after crossing the blood brain barrier, the nano drug-delivery system can enter tumor cells in a targeted manner under guidance of the metastatic encephaloma targeted ligands; the prodrug in the nano drug-delivery system can further specifically act on the tumor cells on the basis of targeted delivery and reduces side effects on normal brain tissue and surrounding tissue, and the method is simple and has operability and economic benefit.

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