Intelligent cerebral stroke drug carrier for ROS (reactive oxygen species) response and preparation method of drug carrier

A stroke and carrier technology, applied in the field of medicine, can solve the problems of unsatisfactory encapsulation rate and drug loading, and achieve the effect of reducing systemic toxic and side effects, simple method, and good stability

Inactive Publication Date: 2017-01-04
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since NR2B9C is a small molecular polypeptide with strong hydrophilicity, common core-shell structures such as micelles and nanoparticles are not ideal for its encapsulation efficiency and drug loading capacity.

Method used

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  • Intelligent cerebral stroke drug carrier for ROS (reactive oxygen species) response and preparation method of drug carrier
  • Intelligent cerebral stroke drug carrier for ROS (reactive oxygen species) response and preparation method of drug carrier
  • Intelligent cerebral stroke drug carrier for ROS (reactive oxygen species) response and preparation method of drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation and Characterization of Carrier Material PHB-Dextran

[0031] 4-Hydroxymethylphenylboronic acid pinacol ester (PBAP, 7.37g, 31.5mmol) and carbonyldiimidazole (CDI, 10.20g, 62.9mmol) were dissolved in anhydrous dichloromethane, and reacted for 30min. Washed three times with pure water (3×10ml) and once with brine (1×10ml), dried overnight over magnesium sulfate, concentrated and dried under vacuum to give a white solid (PBAP-CDI). Dextran (dextran, Mw=10000g / mol) was dissolved in 4ml of formamide, then PBAP-CDI and DMAP were added respectively, and stirred overnight at room temperature. The reaction solution was dialyzed to remove formamide and free PBAP-CDI with a dialysis bag (molecular weight cut-off 500 Da, and the dialysis medium was pure water), and then freeze-dried to obtain a white powder (PHB-Dextran). NMR instrument detects its NMR spectrum, see figure 1 .

Embodiment 2

[0033] Preparation and Characterization of ROS Responsive Stroke Smart Drug Carriers

[0034] Prepared by self-assembly method, weigh 10mg PHB-Dextran dissolved in a mixed solvent of formamide and methanol (V:V=1:1) as the organic phase, weigh 1mg NR2B9C dissolved in 0.2M Tris-HCl buffer, and mix with organic After the phases were mixed, they were dispersed dropwise into 10ml of 0.5% poloxamer 188 aqueous solution under constant stirring (500rpm, 37°C), and continued to stir for 1-2h. μm microporous membrane to obtain the nanovesicle carrier (NP / NR2B9C), its morphology was characterized by transmission electron microscopy, see figure 2 . figure 2The figure shows that the nanovesicle carrier has a regular spherical appearance, uniform size, and a particle size of about 165 nm when observed under a transmission electron microscope. Laser particle size analysis showed that the obtained nanovesicle carrier had an effective diameter of 170nm and a normal distribution with a pol...

Embodiment 3

[0036] ROS response to the hydrolysis behavior of smart drug carriers in stroke

[0037] The prepared nanovesicle carrier (NP) was divided into two parts, placed in 0.01M PBS buffer system and 1mM H 2 o 2 0.01M PBS buffer system and incubated at 37°C. The digital camera took photos at 0, 0.25, 0.5, 1, 2, and 4 hours to investigate the appearance changes of the nanocarrier solution, see image 3 . Depend on image 3 Visible in , add 1mM H 2 o 2 After 15 minutes, the light blue opalescence of the nanovesicle carrier was obviously weakened, and after 30 minutes, the opalescence disappeared and became colorless and clear without H 2 o 2 The appearance of the PBS group did not change significantly, and this result verified that the hydrolysis behavior of the nanovesicle carrier has ROS response characteristics.

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Abstract

The invention discloses an intelligent cerebral stroke drug carrier for ROS (reactive oxygen species) response and a preparation method of the drug carrier. The carrier is a nano vesicle, hydrophobic boric acid ester is grafted to hydrophilic glucan framework to form amphiphilic block copolymers, the amphiphilic block copolymers serve as carrier materials to prepare the nano vesicle, and the nano vesicle encapsulates neuroprotective agents NR2B9C. The preparation method includes the steps: performing covalent grafting for the boric acid ester and glucan; preparing a nano vesicle carrier by grafting reaction carrier materials in an automatically filling manner; encapsulating the neuroprotective agents NR2B9C in the nano vesicle carrier. The weight ratio of the boric acid ester and the glucan is 10: (5-25), the carrier easily responds degradation of ROS mediation, so that drugs rapidly release at cerebral ischemia lesion positions, and release in non-lesion areas is decreased, so that the neuroprotective agents are more safely and effectively transmitted in intracerebral target areas.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a ROS-responsive cerebral apoplexy intelligent drug carrier and a preparation method thereof. Background technique [0002] With the continuous progress of human society, the problem of social aging is becoming more and more serious, and the incidence of cerebrovascular diseases is also increasing year by year, and has become the focus of disease prevention and treatment for the elderly. Among them, stroke is a common refractory disease that seriously endangers human health and life safety. There are obvious three highs (high incidence, high disability rate, and high mortality) phenomenon, and it is listed as the second largest human disease after cardiovascular disease. and the third leading killer of malignant tumors. Clinically, 87% of cerebral apoplexy is ischemic apoplexy, so the research on drug treatment of ischemic apoplexy has great clinical significance. Reactive oxy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K9/127A61K47/36A61K47/24A61P9/10
CPCA61K9/0002A61K9/1273A61K38/08A61K47/24A61K47/36
Inventor 辛洪亮徐群为吕伟江艳徐剑培
Owner NANJING MEDICAL UNIV
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