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Hydrophilic nano-drug carrying beta-carotene and application thereof in preparation of drug for treating cerebral ischemia-reperfusion injury

A technology of cerebral ischemia reperfusion and carotene, which is applied in the field of medicine, can solve the problems of easy oxidation, limited application, poor stability, etc., and achieve the effect of removing excessive active oxygen, increasing water solubility and stability, and efficient scavenging ability

Inactive Publication Date: 2020-02-07
THE SECOND AFFILIATED HOSPITAL TO NANCHANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, β-carotene has disadvantages such as insolubility in water, poor stability, and easy oxidation, which greatly limits its application in biomedicine
In addition, due to the restriction of the blood-brain barrier, intravenous injection of β-carotene cannot enter the brain through the blood-brain barrier, which further limits its application in the treatment of ischemic cerebrovascular diseases.

Method used

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  • Hydrophilic nano-drug carrying beta-carotene and application thereof in preparation of drug for treating cerebral ischemia-reperfusion injury
  • Hydrophilic nano-drug carrying beta-carotene and application thereof in preparation of drug for treating cerebral ischemia-reperfusion injury
  • Hydrophilic nano-drug carrying beta-carotene and application thereof in preparation of drug for treating cerebral ischemia-reperfusion injury

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1 Preparation and Performance Testing of Drugs for the Treatment of Cerebral Ischemia-Reperfusion Injury

[0032] By double emulsification method, DSPE-PEG was used as carrier material to prepare entrapped NP β-carotene . Wherein the dosage of polymer DSPE-PEG is 40mg, and the dosage of added β-carotene is 1mg.

[0033] The specific method is: dissolve DSPE-PEG and β-carotene in 0.5mL dichloromethane, add the β-carotene solution, and then conduct ultrasonic wave under the probe-type ultrasonic breaker (VC130 type, Sonics, U.S.) (output power 450 watts) , 30 seconds) to form the initial emulsion, the initial emulsion was added to 5mL aqueous solution, and ultrasonic emulsification again (output power 450 watts, 2min), using a rotary evaporator, under reduced pressure (1000 Pa) to make the organic solvent volatilize, centrifuged (4 °C, 30000×g, 1h), collect nanoparticles, resuspend twice with ultrapure water, centrifuge and wash, collect samples, and obtain n...

Embodiment 2

[0044] Example 2 Experiment of Treating Cerebral Ischemia-Reperfusion Injury in Mice

[0045] 1. Drug distribution study in vivo

[0046] C57 mice (10-12 weeks) with an average body weight of 26-28 g were selected and purchased from Beijing Weitong Lihua Animal Company.

[0047] Experimental method: After mice were anesthetized with isoflurane inhalation, the nanomedicine carrying β-carotene was injected intrathecally at a dose of 0.5

[0048] mg / kg. Analyze the distribution of nano-medicines carrying β-carotene in vivo at 0.5, 6, and 12 hours after injection, and analyze the distribution of drugs in living brain tissues at 6 and 12 hours.

[0049] Experimental results such as Figure 5 It can be seen from the experimental results that the nano-medicine of hydrophilic β-carotene has a high aggregation amount in the brain, and there is still a high aggregation amount at 6 and 12 hours.

[0050] 2. Animal model of cerebral ischemia-reperfusion injury

[0051] C57BL / 6 mice, we...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a hydrophilic nano-drug carrying beta-carotene and an application thereof in preparation of a drug for treating cerebral ischemia-reperfusion injury. According to the invention, the beta-carotene is carried by the high-molecular DSPE-PEG, so that the water solubility and the stability of the high-molecular DSPE-PEG are improved; an intrathecal injection method is used for increasing the aggregation of the nano-drug in the brain; beta-carotene is used for removing active oxygen, oxidative stress injury afterischemia-reperfusion of the brain is effectively reduced, the important value is achieved for developing medical application of beta-carotene, and the important significance is achieved for treating and relieving ischemia-reperfusion injury of the brain.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a hydrophilic nano-medicine carrying beta-carotene and its application in preparing medicine for treating cerebral ischemia-reperfusion injury. Background technique [0002] Ischemic cerebrovascular disease has a high morbidity rate, high disability rate, and high mortality rate, and is a type of disease that seriously affects human health. Restoring cerebral blood flow as early as possible is the most effective way to treat patients with ischemic cerebrovascular disease, but limited by the short "time window" of treatment, only a small number of patients (less than 5%) can receive effective thrombolytic therapy. After the blood supply is restored in most patients, a large amount of reactive oxygen species will be generated rapidly, and the excessive reactive oxygen species will further aggravate the apoptosis of neurons and the damage of brain tissue, namely: cerebr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/10A61K47/24A61K31/015A61P9/10
CPCA61K9/0019A61K9/5146A61K31/015A61P9/10
Inventor 李士勇罗军王晔袁真
Owner THE SECOND AFFILIATED HOSPITAL TO NANCHANG UNIV
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