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Blood brain barrier-crossing magnetic nano drug carrier and preparation method thereof

A magnetic nanometer and blood-brain barrier technology, applied in magnetic objects, magnetic materials, drug combinations, etc., can solve the problems of intracranial infection, unfavorable long-term medication, etc., and achieve simple process, treatment of central nervous system diseases, and controllable process. Effect

Active Publication Date: 2018-01-16
北京百替生物技术有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The purpose of the present invention is to provide a magnetic nano-medicine across the blood-brain barrier, so as to alleviate the current main way of sending medicine into the brain is neurosurgery methods such as intracerebral intubation and intraventricular injection, which are easy to cause intracranial infection and are not conducive to long-term medication. technical issues

Method used

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  • Blood brain barrier-crossing magnetic nano drug carrier and preparation method thereof
  • Blood brain barrier-crossing magnetic nano drug carrier and preparation method thereof
  • Blood brain barrier-crossing magnetic nano drug carrier and preparation method thereof

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preparation example Construction

[0041] In a preferred embodiment of the present invention, the preparation method of pH and thermal bisensitivity copolymer comprises the steps of: dispersing N-isopropylacrylamide, methacrylic acid and cetyl acrylate in dioxane, adding Azo initiator, react at 65-75°C for 12-14h, and then use diethyl ether and tetrahydrofuran to repeatedly precipitate and dissolve for several times to obtain a pH- and heat-sensitive copolymer.

[0042] In a preferred embodiment of the present invention, azobisisobutyronitrile or azoheptanonitrile is used as an initiator, reacted for 12-14 hours in an oxygen-free environment at 65-75°C in a water bath, and repeatedly extracted and precipitated to prepare a copolymer thing.

[0043] According to another aspect of the present invention, the present invention provides a method for preparing the above-mentioned cross-blood-brain barrier magnetic nano drug carrier, comprising the following steps:

[0044] (a) dissolving the paramagnetic substance i...

Embodiment 1

[0056] This example provides a magnetic nano-medicine carrier that crosses the blood-brain barrier, with magnetic iron ferric oxide as the core, mesoporous silica as the shell, and the outer layer of the silica is coated with a bisensitivity copolymer - liposomes, wherein the outer surface of the mesoporous silica is modified with amino groups, a bisensitivity copolymer - liposomes are prepared from pH and heat bisensitivity copolymers, soybean lecithin and cholesterol, and the three The quality is 1:10:50; the bisensitivity copolymer is copolymerized from N-isopropylacrylamide, methacrylic acid and hexadecyl acrylate, and the molar ratio of the three is 90:1:5.

Embodiment 2

[0058] This example provides a magnetic nano-medicine carrier that crosses the blood-brain barrier. The molar ratio of hexaester is 80:1:20.

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Abstract

The invention provides a blood brain barrier-crossing magnetic nano drug carrier and a preparation method thereof, and relates to the technical field of drug carriers; the blood brain barrier-crossingmagnetic nano drug carrier includes mesoporous silica, the interior of the mesoporous silica is provided with a paramagnetic substance, and the outer surface of the mesoporous silica is coated with adouble-sensitive copolymer-liposome; the technical problems that intracranial infection is easy to cause and long-term drug use is not facilitated because main paths to send a drug into a brain comprise intracerebral intubation, ventricular injection and other neurosurgery department methods at present are relieved; the blood brain barrier-crossing magnetic nano drug carrier is prepared, whereinthe blood brain barrier-crossing magnetic nano drug carrier integrates magnetic targeting and pH with heat sensitivity, can carry a drug under the guidance of an external magnetic field, crosses a blood brain barrier to directly reach a lesion site and controllably releases the drug, and the technical effect capable of effectively treating central nervous system diseases is achieved.

Description

technical field [0001] The invention relates to the technical field of drug carriers, in particular to a blood-brain barrier-crossing magnetic nanometer drug carrier and a preparation method thereof. Background technique [0002] The blood-brain barrier is mainly composed of brain capillary endothelial cells, which can prevent 98% of small molecules and almost all macromolecular compounds from entering the brain, and is a bottleneck restricting the drug treatment of central nervous system diseases. At present, the main ways to deliver drugs into the brain are neurosurgical methods such as intracerebral intubation and intraventricular injection, which are prone to intracranial infection and are not conducive to long-term drug use. Therefore, there is an urgent need to develop a drug carrier that crosses the blood-brain barrier, so that the drug can directly reach the lesion site without craniotomy, so that central nervous system diseases can be effectively treated. [0003] ...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/32A61K47/24A61K47/28A61K47/02A61K47/04A61P25/00H01F1/00H01F41/02C08F220/54C08F220/06C08F220/18
Inventor 郭磊
Owner 北京百替生物技术有限公司
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