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Cascade brain-targeting drug delivery system as well as preparation method and application thereof

A delivery system and brain targeting technology, applied in cascade brain targeted drug delivery system and preparation thereof, cascade targeting system, application field in preparation of preparations for treating or diagnosing brain diseases such as brain tumors and nervous system diseases , which can solve the problem of inability to accurately target brain lesions, and achieve good imaging and treatment effects.

Inactive Publication Date: 2012-07-11
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The invention can overcome the difficulty of double barriers in the diagnosis and treatment of brain diseases, and overcome the problem that the traditional brain-targeted or disease-targeted drug delivery system cannot accurately target the brain lesion,

Method used

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  • Cascade brain-targeting drug delivery system as well as preparation method and application thereof
  • Cascade brain-targeting drug delivery system as well as preparation method and application thereof
  • Cascade brain-targeting drug delivery system as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1, construction of TGN and AS1411 double modified nanoparticle drug delivery system

[0025] Nanoparticles were prepared by a single emulsification method. 28 mg of polyethylene glycol-polycaprolactone (MPEG-PCL), 1 mg of carboxy-modified PEG-PCL and 1 mg of maleimide-modified PEG-PCL were dissolved in 1 mL of dichloromethane and added to 5 mL of 0.6% Afterwards, 5s / 5s pulsed ultrasound in an ice-water bath for 15 times with a power of 200W; rotary evaporation removed methylene chloride and concentrated to an appropriate concentration to obtain unmodified nanoparticles (NP); the carboxyl groups on the surface of nanoparticles were obtained by EDC After activation with NHS in MES buffer for half an hour, the external aqueous phase was replaced with PBS at pH 7.4 by Hitrap desalting column, then 10 OD AS1411 was added and stirred in the dark for 4 hours; then 25 μg of TGN was added in the dark and filled with nitrogen to react6 hours; after that, the unbound AS14...

Embodiment 2

[0027] Example 2, Targeting of TGN and AS1411 double modified nanoparticle drug delivery system to different cells

[0028] C6 cells and bEnd.3 cells (normal rat brain capillary endothelial cell line) were mixed with 2×10 4 The concentration of cells per well was inoculated into a 24-well plate; after 24 hours, the cells were incubated with HBSS for 5 minutes, and then 1 mL of NP containing 100 μg / mL coumarin-6, AS1411 single-modified NP (AsNP), AS1411 and TGN double-modified NP (AsTNP) or TGN single-modified (TNP); after 1 hour, the cells were washed 4 times with ice-cold PBS, and then observed directly with a fluorescence microscope or digested and detected by flow cytometry.

[0029] Such as figure 2 As shown, in bEnd.3 cells, TGN can significantly increase the uptake of nanoparticles, while AS1411-modified AsNP does not significantly increase the uptake of NPs; in contrast, in C6 cells, AS1411-modified AsNP and The uptake of AsTNP was significantly higher than that of NP,...

Embodiment 3

[0031] Example 3, Targeting of TGN and AS1411 double modified nanoparticle drug delivery system to glioma

[0032] A mouse model bearing orthotopic C6 glioma was constructed. Eight days after inoculation, NP, AsNP, AsTNP and TNP loaded with fluorescent probes DiR were given respectively, and the fluorescence distribution of the animals was observed at a certain time point, and the brain was taken out at 24 hours to observe the fluorescence distribution of the brain in vitro.

[0033] Such as image 3 As shown, unmodified nanoparticles are rarely distributed in the brain, while only a small amount of AS1411-modified AsNP enters the brain, and the in vitro pictures show that they are mainly distributed in the brain tumor site; while the modified TGN has a large distribution in the brain. increased, and the degree of brain fluorescence at each time point was stronger than that of NP and AsNP; however, the fluorescence distribution of the isolated brain showed that TGN single-mod...

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Abstract

The invention belongs to the field of pharmaceuticals and relates to a cascade brain-targeting drug delivery system and the application thereof. The cascade brain-targeting drug delivery system comprises a first-stage target functional molecule, a second-stage target functional molecule and a drug carrier. The cascade target drug delivery system can identify the blood-brain barrier through the first-stage target functional molecule and identify a brain lesion through the second-stage target functional molecule, so as to achieve the accurate targeting purpose, and can also accurately transfer imaging molecules or drugs to the brain lesion, so as to achieve good imaging and therapeutic effects. The cascade brain-targeting drug delivery system can be applied to prepare formulations for treatment or diagnosis of brain diseases (such as brain tumors) and nervous system diseases.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a cascade brain-targeted drug delivery system, in particular to a cascade brain-targeted drug delivery system and its preparation method and application, especially to a cascade brain-targeted drug delivery system with brain-targeted drug delivery characteristics. A targeting system, and its application in preparing preparations for treating or diagnosing brain diseases such as brain tumors and nervous system diseases. Background technique [0002] With the aging of human society, the incidence of brain diseases is increasing year by year, seriously endangering human life and health; known brain diseases include central nervous system diseases (Parkinson's disease, senile dementia), brain Diseases such as tumors, cerebrovascular lesions, viral and bacterial infections of the brain. At present, the traditional drug therapy generally has the disadvantages of poor effect an...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/127A61K9/14A61K47/42A61K49/00A61K49/14A61P25/00A61P35/00
Inventor 高会乐蒋新国庞志清
Owner FUDAN UNIV
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