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Functional curcumin nano-drug for diagnosis and treatment of cerebral diseases and application of nano-drug

A technology of nano-drugs and curcumin derivatives, which is applied in drug combination, drug delivery, nervous system diseases, etc., can solve the problems of poor water solubility and chemical instability of curcumin, and achieve improved water solubility and stability, Increased pharmacological activity, increased permeability

Inactive Publication Date: 2017-08-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically, curcumin's poor water solubility and chemical instability affect its practical application

Method used

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  • Functional curcumin nano-drug for diagnosis and treatment of cerebral diseases and application of nano-drug
  • Functional curcumin nano-drug for diagnosis and treatment of cerebral diseases and application of nano-drug
  • Functional curcumin nano-drug for diagnosis and treatment of cerebral diseases and application of nano-drug

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: ester bond is the synthesis and grafting rate of the curcumin derivative of linking arm

[0035] Curcumin and low-molecular-weight heparin were dissolved in appropriate solvents as 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDCI), N-hydroxysuccinimide (NHS) , 4-dimethylaminopyridine (DMAP) as an activator. Dissolve low-molecular-weight heparin in formamide in an oil bath at 40°C for about 1 hour, then add EDCI under ice-cooling, add NHS after activation for 30 minutes, activate in ice-bathing for 2 hours, then add curcumin and DMAP, protected from light, activated in an ice bath for 30 minutes, then moved to room temperature and protected from light for 24 hours. The above process was protected with nitrogen. After the reaction was completed, excess ice acetone (3-5 times the amount) was added to precipitate the product, and the precipitate was obtained by suction filtration. The resulting precipitate was redissolved in water, sonicated b...

Embodiment 2

[0038] Embodiment 2: ether bond is the synthesis and grafting rate of the curcumin derivative of linking arm

[0039] Low-molecular-weight heparin and curcumin were placed in round-bottomed flasks respectively, N,N-dimethylformamide was added, stirred to make it dissolve, alkalizing reagent 4-dimethylaminopyridine (DMAP) was added in the curcumin solution, To achieve the purpose of activating the phenolic hydroxyl group; slowly add the activated curcumin to the low molecular weight heparin solution at an interval of 5 seconds per drop, and at the same time add concentrated sulfuric acid as a water-absorbing agent, and stir at room temperature for 24 hours. After the reaction is completed, add ice acetone to precipitate the product, pump Filter the precipitate; add water to redissolve the precipitate, dialyze in water for 1 day, and freeze-dry to obtain the final product - curcumin derivative. The grafting ratio of the obtained product is shown in Table 2.

[0040] Table 2 eth...

Embodiment 3

[0042] Embodiment 3: Ethylenediamine is the synthesis of the curcumin derivative of connecting arm

[0043] Take 2 mol of low molecular weight heparin and place it in a round bottom flask, add 50 mL of formamide to dissolve it, add 8 mol of ethylenediamine, stir for 2 min with magnetic force, then add 3 mol of 1-ethyl-(3-dimethylaminopropyl) carbodiimide ( EDC) and 4.5mol hydroxysuccinimide (NHS), reacted at room temperature for 12 hours, added acetone to precipitate the product after the reaction, filtered to obtain the precipitate, redissolved in water, dialyzed for 2 days, and freeze-dried to obtain a heparin active intermediate with a free one-terminal amino group . Dissolve the heparin active intermediate obtained above in a methanol-water mixed solution, avoid light, and slowly add 6 mol of curcumin in methanol solution dropwise under magnetic stirring at 50°C for 1.5 hours. Take the product by rotary evaporator to remove methanol, add a small amount of water to mix, an...

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Abstract

The invention relates to a functional curcumin nano-drug for diagnosis and treatment of cerebral diseases and application of the nano-drug. An amphipathic curcumin derivative is synthesized through a chemical method, and the nano-drug with curative activity and a drug loading function can be formed in an aqueous medium through self-assembling. The nano-drug has pharmacological activity aiming at treatment of the cerebral diseases and can achieve the effects of increasing blood-brain barrier permeability and promoting cerebral targeted drug delivery, so that the nano-drug achieves excellent effects of diagnosing and treating the cerebral diseases and has wide application prospects.

Description

technical field [0001] The invention relates to a preparation method and application of a functional curcumin nano-medicine for diagnosis and treatment of brain diseases. The nano-medicine can be applied to the diagnosis and treatment of brain diseases and belongs to the field of pharmaceutical preparations and applications thereof. Background technique [0002] Efficient drug delivery is currently one of the major hurdles in the diagnosis and treatment of brain diseases. This is mainly because the blood-brain barrier (BBB) ​​in the brain restricts the transport of drugs from the blood to the brain, resulting in most drugs not being able to enter the brain lesion and exert their curative effect. The brain drug delivery design strategy usually includes the use of A method: lipophilic pro-drugs (pro-drugs); B method: BBB open method; C method: nasal administration; D method: nanotechnology delivery, etc. However, these strategies still have deficiencies or limitations: the st...

Claims

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Application Information

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IPC IPC(8): A61K47/61A61K47/69A61K31/12A61K9/51A61K47/36A61K45/00A61K49/00A61K31/337A61K31/48A61K31/704A61K31/405A61K31/365A61K31/4745A61K31/4748A61P25/00
CPCA61K31/12A61K9/0002A61K9/0014A61K9/5161A61K31/337A61K31/365A61K31/405A61K31/4745A61K31/4748A61K31/48A61K31/704A61K45/00A61K49/0054A61K49/0093A61K2300/00
Inventor 姚静肖燕
Owner CHINA PHARM UNIV
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