Bionic acid-sensitive nano drug as well as preparation method and application method thereof

A nano-drug and biomimetic acid technology, which is applied in the direction of drug combination, pharmaceutical formula, anti-tumor drug, etc., to achieve the effect of prolonging the time of internal circulation and simple process

Active Publication Date: 2018-08-03
HENAN UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In addition, the use of chemotherapeutic drugs for the treatment of tumors faces other challenges

Method used

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  • Bionic acid-sensitive nano drug as well as preparation method and application method thereof
  • Bionic acid-sensitive nano drug as well as preparation method and application method thereof
  • Bionic acid-sensitive nano drug as well as preparation method and application method thereof

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preparation example Construction

[0065] In a preferred embodiment of the present invention, the above-mentioned preparation method of a biomimetic acid-sensitive nano-medicine comprises: after mixing the inner core and the outer shell in proportion, using an Avanti liposome extruder to repeat the process under the polycarbonate membrane Squeeze 7 times to get a biomimetic acid-sensitive nano-medicine.

[0066] The preparation method of the biomimetic acid-sensitive nano-medicine of the present invention has simple process and is suitable for large-scale production.

[0067] In a preferred embodiment of the present invention, the erythrocyte membrane obtained from 100 μL of mouse blood uses less than 0.5 mg of drug, preferably corresponding to 0.5 mg of drug.

[0068] In a preferred embodiment of the present invention, the pore size of the filter membrane is less than 200 nm, preferably 200 nm.

[0069] In a preferred embodiment of the present invention, the preparation method of the inner core comprises:

...

Embodiment 1

[0099] A preparation method of biomimetic acid-sensitive nano-medicine, comprising:

[0100] (1) Synthesis of acetal grafted dextran (m-dextran):

[0101] The target product m-dextran can be obtained in one step reaction. Specific steps are as follows:

[0102] Under the condition of nitrogen protection, dry dextran (dextran, 10kDa, 0.5g) and ethoxypropylene (2.08mL, 18.5mmol) in anhydrous dimethyl sulfoxide (DMSO, 5mL) solvent at room temperature The reaction was 0.5h, and the catalyst was added pyridinium p-toluenesulfonate (7.8mg). After the reaction was completed, the reaction was terminated with triethylamine (0.5 mL), precipitated in deionized water with a pH of 8, and washed three times to prevent the degradation of the acetal bond. The final product m-dextran was obtained by freeze-drying the precipitate after centrifugation at -80°C . The main raw materials such as dextran, ethoxypropylene and pyridinium tosylate used in the synthesis process can be purchased and ...

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Abstract

The invention a bionic acid-sensitive nano drug as well as a preparation method and an application method thereof. The bionic acid-sensitive nano drug comprises an inner core and an outer shell, wherein the outer shell comprises a targeted modified red blood cell membrane. The bionic acid-sensitive nano drug has immune-free natural biological characteristics, and can greatly prolong in-vivo circulating time of the nano drug; and the inner core comprises a carrier with a sensitive bond on a side chain, and can effectively release the drug to achieve the purpose of targeted treatment of tumors.The preparation method for the bionic acid-sensitive nano drug is simple, is suitable for large-scale production, is suitable for preparing the targeted treatment drug, is preferably suitable for preparing the tumor targeted treatment drug, and is especially suitable for preparing a brain glioma targeted treatment drug, and effectively solves the key problems that the existing nano-drug is short in in-vivo circulating time, has difficulty in crossing BBB, is low intake amount by tumor cells, is low in release at a focus, and the like.

Description

technical field [0001] The invention relates to the technical field of targeted drugs, in particular to a biomimetic acid-sensitive nano drug and its preparation and application method. Background technique [0002] At present, malignant tumors have surpassed cardiovascular and cerebrovascular diseases to become the number one killer of Chinese residents, accounting for more than 25% of the death rate. With the rapid increase of its morbidity and mortality, it is urgent to seek efficient and safe treatment. [0003] Brainstem tumors (brainstem gliomas) account for 1.4% of intracranial tumors. Mainly glioma, of which astrocytoma and polar glioblastoma are more common, followed by oligodendroglioma, ependymal glioma, medulloblastoma, and also Hemangioma, cyst, teratoma, tuberculoma, metastatic tumor, etc. Children and adolescents are prone to hair loss, especially children aged 5-9 have the highest incidence rate. Pediatric patients often have poorly differentiated polar g...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K31/704A61K31/7076A61K47/46A61K47/42A61P35/00
CPCA61K31/704A61K31/7076A61K47/42A61K47/46A61K47/61A61P35/00A61K2300/00
Inventor 师冰洋刘艳杰邹艳郑蒙
Owner HENAN UNIVERSITY
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