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Brain delivery method for nano-medicament carrier

A nano-drug carrier and nano-drug technology, applied in the field of medicine, can solve problems such as the inability to further realize molecular targeting of lesions in the brain, unsatisfactory efficiency, and lack of biological targeting characteristics, so as to overcome adverse in vivo properties and realize The effect of lesion targeting and enhancing the signal intensity of diagnostic molecules

Inactive Publication Date: 2012-07-04
SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The fly in the ointment is that for some drugs with bad properties such as poor stability and strong hydrophilicity, the efficiency of ultrasound combined with microbubble technology to mediate their entry into the brain is still not ideal.
In addition, this technology lacks biological targeting properties, and it is not yet possible to further achieve molecular targeting of the lesion in the brain

Method used

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  • Brain delivery method for nano-medicament carrier
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  • Brain delivery method for nano-medicament carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1. Intracerebral delivery of coumarin-loaded 6 nanoparticles mediated by ultrasound combined with microbubbles

[0040] Preparation of coumarin-6 nanoparticles: 10-25 mg monomethoxy polyethylene glycol-polylactic acid (MPEG-PLA) block copolymer was dissolved in 1 ml dichloromethane solution (containing 0.01-0.2 mg coumarin 6), add 2 ml of 1% sodium cholate solution, and continuously sonicate at 220 W for 30 s-2 min to obtain colostrum. Add colostrum into 8-25 ml of 0.5% sodium cholate solution, stir for 5 min, remove dichloromethane by rotary evaporation, centrifuge at 14,000 rpm at 4°C for 45 min, remove supernatant, and refill with 0.01 mol / L pH7.0 HEPES Disperse and pass through a Sepharose CL-4B gel column to remove unencapsulated coumarin 6 to obtain coumarin 6 nanoparticles.

[0041] Ultrasound devices for clinical diagnosis are used, and SonoVue (particle size about 2 μm) approved by SFDA for use in my country is used as ultrasonic microbubbles. As show...

Embodiment 2

[0045] Example 2. Ultrasound combined with microbubbles mediates the transport of coumarin-6 liposomes into the brain parenchyma

[0046] Preparation of coumarin 6-loaded liposomes: 5-30 mg DMPC, 0.01-1 mg coumarin 6 were dissolved in 2 ml chloroform, and rotary evaporation was used to obtain a lipid film, and 10 ml solution was added for hydration to obtain a multilamellar liposome plastid. Small single-lamellar liposomes were prepared by ultrasonication with a 200 W probe, high-pressure homogenization or membrane extrusion, and the unencapsulated coumarin 6 was removed by gel column separation.

[0047] Using ultrasonic devices for clinical diagnosis, SonoVue is ultrasonic microbubbles. Liposomes were administered immediately after ultrasound combined with microbubble treatment. Three hours later, the experimental mice were perfused with normal saline to remove blood and fixed with 4% paraformaldehyde. The brain was taken out, fixed with 4% paraformaldehyde for 24 h, dehyd...

Embodiment 3

[0049] Example 3. Ultrasound combined with microbubbles mediates Fe 3 o 4 Cerebrovascular endothelial and neuronal cellular uptake of nanoparticles

[0050] Using ultrasonic devices for clinical diagnosis, SonoVue is ultrasonic microbubbles. Immediately after ultrasound and microbubble treatment, Fe 3 o 4 Nanoparticles, after 3 h, the heart of experimental mice was perfused with normal saline to remove the blood, and fixed with 2.0% glutaraldehyde. Take the brain, cut 1 cm from the hippocampus 3 Tissue blocks were fixed with 2% glutaraldehyde for 24 hours, fixed with osmic acid, embedded, ultra-thin sectioned, and observed by transmission electron microscopy that ultrasound combined with microbubbles mediated the opening of BBB tight junctions and the formation of transport vesicles.

[0051] The results show( Figure 4 ), there were obvious endocytic vesicles in brain vascular endothelial cells in the ultrasound combined with microbubble group, Fe 3 o 4 Nanoparticles...

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Abstract

The invention provides a brain delivery method for a nano-medicament carrier. Brain delivery of the nano-medicament carrier carrying a diagnosis and treatment medicament is mediated by using ultrasonic waves and micro-vesicles together; the nano-medicament carrier and the micro-vesicles are administrated separately or administrated simultaneously after being mixed easily or administrated simultaneously through non-covalent and covalent connection; and in the brain delivery of the nano-medicament carrier carrying the diagnosis and treatment medicament under the mediation of ultrasonic waves and micro-vesicles, ultrasonic treatment is performed immediately or a certain time interval after micro-vesicles are applied to a mechanism. Compared with the conventional brain delivery of a medicament under the mediation of ultrasonic waves and micro-vesicles, the method has the advantages that: poor in-vivo properties (poor stability, easiness in clearing by the organism and the like) of the medicament can be eliminated, the diagnosis molecular signal strength is enhanced, the detection sensitivity is enhanced, and focus targeting can be realized; and compared with the conventional brain delivery technology for the nano-medicament carrier, the method has the advantage that: external ultrasonic waves are applied in a technology, so that more efficient and more specific brain medicament delivery can be realized.

Description

technical field [0001] The present invention relates to the field of medicine, and more specifically, relates to a technique for intracerebral delivery of nano drug carriers mediated by ultrasound combined with microbubbles. Background technique [0002] Brain diseases, including brain tumors and neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), are major diseases that endanger human life and health, and the incidence rate is increasing year by year. However, the current effective drug diagnosis and treatment of brain diseases still faces several core problems, among which drug delivery across the blood-brain barrier (BBB) ​​is the primary problem that must be overcome to achieve drug treatment of brain diseases. BBB is a layer of barrier system between blood and brain tissue, composed of polarized brain capillary endothelial cells through complex intercellular tight junctions, it is very important to maintain the relative stability of the bra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/42A61K47/24A61K47/30A61K49/18A61K49/14A61K49/12A61K49/10A61K51/12A61K51/08A61K51/06A61K51/04A61P25/28A61N7/00
Inventor 高小玲姚磊陈红专宋清香胡兵
Owner SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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