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Brain targeting agent as well as preparation method and application thereof

A brain-targeting and brain-targeting peptide technology is applied in pharmaceutical formulations, preparations for in vivo tests, and medical preparations with inactive ingredients, etc. It is impossible to precisely control and overcome the limitations of the spatial structure, etc., to achieve the effects of precisely controllable molecular and spatial structures, good biocompatibility, and broad application prospects.

Inactive Publication Date: 2017-11-28
SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a brain-targeted preparation and its preparation method and application, so as to solve the problem that the nanomaterials used for brain-targeted delivery in the prior art cannot accurately control the number of signal molecules and functional molecules and cannot overcome the spatial structure. limitations, and the inability to meet the requirements of biocompatibility and degradability

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  • Brain targeting agent as well as preparation method and application thereof
  • Brain targeting agent as well as preparation method and application thereof
  • Brain targeting agent as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of brain-targeted preparations based on DNA nanostructures

[0043] According to the brain-targeting preparation based on DNA nanostructures provided by the present invention, the DNA nanostructures can have various shapes such as triangles, rectangles, tetrahedrons, or tubes. By way of example and not limitation.

[0044] 1.1 Construction of DNA tetrahedral nanostructures

[0045] First, according to the shape of the constructed DNA tetrahedral nanostructure, four oligo-stranded DNAs (S1-S4) were precisely designed in strict compliance with the complementary pairing principle of DNA. The four oligo-stranded DNAs were dissolved in TM buffer (10 mM Tris-HCl, 5 mM MgCl) at a final concentration of 1 μM 2 , PH 8.0) and mixed thoroughly, the total reaction system was 100 μl, placed in a PCR instrument and heated to 95°C for denaturation for 10 minutes, and then quickly lowered to 4°C to obtain the DNA tetrahedral structure. Wherein, the specific nuc...

Embodiment 2

[0066] Example 2 Cellular uptake of brain-targeted formulations

[0067] 2.1 Cell flow cytometry detection of the uptake of brain-targeted preparations by cells

[0068] (1) The cerebrovascular endothelial cells bEnd.3 and glioma cells U87MG grown to the logarithmic phase were digested with 0.25% trypsin to make a single cell suspension, and each well was 7×10 4 cells were inoculated into 24-well culture plates, and after inoculation, the 24-well culture plates were placed at 37°C and 5% CO 2 and cultured in a constant temperature incubator with saturated humidity for 24 h. Three replicate wells were made for each group, and the experiment was repeated three times. During the inoculation process, the prepared single-cell suspension should be blown frequently to prevent cell aggregation in the suspension.

[0069] (2) After culturing for 24 hours, the old medium in the 24-well plate was discarded, washed 3 times with PBS, and the Angiopep-2-modified DNA tetrahedron labeled wi...

Embodiment 3

[0084] Example 3 Brain-targeted preparation in normal mouse midbrain imaging

[0085] According to the method in Example 1, a DNA tetrahedral nanostructure connected with 3 Angiopep-2 targeting peptides at a concentration of 2 μM is synthesized, wherein the parent chain of the DNA tetrahedral nanostructure is marked with a Berthold small animal live imager detectable Fluorescent reporter group Dlight755.

[0086] BALB / c nude mice, male, weighing 18-22g, were intraperitoneally anesthetized with 1% pentobarbital sodium (0.1ml / 10g), and injected the DNA tetrahedron modified by Angiopep-2 into the mice through the tail vein, immediately Put it into a Berthold small animal in vivo imager for real-time fluorescence detection, and record the distribution of Angiopep-2-modified DNA tetrahedrons in nude mice at different time points.

[0087] The result is as Figure 5 As shown, the same dose of Dlight755 fluorescently labeled DNA tetrahedron was injected into the two mice through th...

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Abstract

The invention provides a brain targeting agent as well as a preparation method and an application thereof. Firstly, the method for preparing the brain targeting agent by the aid of a DNA nanostructure is provided and comprises steps as follows: 1) constructing the DNA nanostructure; 2) modifying the DNA nanostructure with a brain targeting peptide to obtain the brain targeting peptide modified DNA nanostructure; 3) performing fluorescent molecular marking on the DNA nanostructure or the brain targeting peptide modified DNA nanostructure for preparation of the brain targeting agent. The invention further provides the brain targeting agent and the application of the brain targeting agent in cerebral disease diagnosis imaging and therapeutic drug delivery. The DNA nanostructure which has the characteristics of being good in bio-compatibility, degradable and accurate and controllable in molecular and spatial structure is subjected to brain targeting functional modification and fluorescent marking and crosses over a blood brain barrier to enter the brain, accordingly, the brain targeting agent has broad application prospects in diagnosis imaging and treatment of cerebral diseases as well as bioimaging of the DNA nanostructure.

Description

technical field [0001] The present invention relates to the field of brain-targeting preparations, and more particularly to a brain-targeting preparation and its preparation method and application. Background technique [0002] The Blood Brain Barrier (BBB) ​​is a unique barrier system between the blood system and brain tissue in the brain, which can ensure a relatively stable internal environment for the brain tissue, deliver nutrients to the brain tissue, and maintain normal physiological functions of the brain. However, the existence of this brain barrier system also brings considerable difficulties to the diagnosis and drug delivery of brain tumors and other diseases. Almost 100% of large molecules and 98% of small molecule drugs cannot pass through the blood-brain barrier. Therefore, it is the key to the diagnosis and treatment of brain diseases to adopt corresponding technical means to realize the targeted delivery of drugs to the brain, and it is also a difficult prob...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/64A61K49/00
CPCA61K49/0052
Inventor 樊春海王丽华孙艳红田甜李江诸颖
Owner SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
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