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ZL006 cyclohexyl ester polymer nanometer drug delivery system and preparation method thereof

A nano-drug delivery system and cyclohexyl ester technology are applied in the field of ZL006 cyclohexyl ester polymer nanocarriers and their preparation, which can solve the problems of poor solubility of ZL006 cyclohexyl ester, improve the anti-ischemic stroke effect, reduce the The effect of distribution and method is simple and easy to implement

Active Publication Date: 2019-02-19
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Moreover, after the present invention selects a suitable method to make ZL006 cyclohexyl ester into polymer nanoparticles, it can not only effectively solve the problem of poor solubility of ZL006 cyclohexyl ester, but also carry out targeted modification on it in the later stage to improve its resistance to deficiency. Hemorrhagic stroke effect at the same time, reduce the distribution of non-target tissues

Method used

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  • ZL006 cyclohexyl ester polymer nanometer drug delivery system and preparation method thereof
  • ZL006 cyclohexyl ester polymer nanometer drug delivery system and preparation method thereof
  • ZL006 cyclohexyl ester polymer nanometer drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: Preparation and characterization of carrier material m-Dextran

[0026] Take 1.0 g of dextran (Mn ~ 9-11kDa) into a dry round bottom flask, and blow dry with nitrogen. Add 10 mL of anhydrous dimethyl sulfoxide and stir until the dextran is fully dissolved. 4.16 mL (37 mmoL) of ethoxypropylene and 15.6 mg (0.062 mmoL) of pyridinium p-toluenesulfonate (PPTS) were added successively. Nitrogen was passed through the reaction solution, and after blowing for 2-3 minutes, it was sealed with a parafilm to prevent the solvent from volatilizing. Stir at room temperature for 30 min to obtain m-Dextran, then add 1 mL of triethylamine to terminate the reaction. The reaction resulted in a white precipitate, which was washed three times with alkaline aqueous solution (pH ~ 8) to prevent degradation, and the product was purified by high-speed centrifugation (8000 rpm, 15 min). Lyophilization to remove excess water gave the product (m-Dextran) as a white solid. Nuclear...

Embodiment 2

[0027] Example 2: Preparation and Characterization of ZL006 Cyclohexyl Ester Polymer Nano Drug Delivery System

[0028] Take 4 mg of neuroprotective agent ZL006 cyclohexyl ester and 20 mg of m-Dextran prepared in Example 1 in a 15 mL centrifuge tube, add 2 mL of dichloromethane, vortex until completely dissolved, add 4 mL of PVA solution prepared by 3% PBS (pH7.4) . Ultrasonic cell disruptor ultrasonication in ice bath (35% power, ultrasonic 2s / stop 2s, 5min). The white emulsion after sonication was slowly introduced into 15 mL of PVA solution prepared with 0.3% PBS (pH 7.4) in high-speed stirring (800 rpm). After continuous stirring for about 1-2h, the dichloromethane was completely volatilized, and the solution was clear and transparent, showing blue nanoparticle opalescence. Centrifuge at high speed (12000rpm, 40min), discard the supernatant, add water to redissolve, repeat 2-3 times to wash away the emulsifier, and finally disperse in 1mL deionized water to obtain a poly...

Embodiment 3

[0029] Embodiment 3: Encapsulation efficiency (EE%) and drug loading (DL%) determination of ZL006 cyclohexyl ester polymer nano drug delivery system

[0030](1) HPLC method to establish ZL006 standard curve:

[0031] Chromatographic conditions, column: HanbonPhecda C18 (4.6mm×150mm, 5μm; Jiangsu Hanbon Technology Co., Ltd.); mobile phase: methanol-water (90:10; v / v); flow rate: 1.0mL / min; UV detection wavelength : 311nm; column temperature: 30°C; injection volume 20μL.

[0032] Standard curve drawing: Accurately weigh 0.0252 g of ZL006 cyclohexyl ester dried at 105°C to constant weight in a 50 mL volumetric flask, dilute to the mark with mobile phase, and obtain a standard stock solution with a concentration of about 504 μg / mL. Precisely pipette 0.05, 0.1, 0.2, 0.5, 1.0, 2.0, 5.0, 8.0, 10.0mL of a series of stock solution into a 50mL volumetric flask, and dilute the mobile phase to the mark to obtain 1.0, 2.0, 5.0, 10.0, 20.0, 50.0 , 80.0, and 100.0 μg / mL sample solutions, a...

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Abstract

The invention discloses a ZL006 cyclohexyl ester polymer nanometer drug delivery system and a preparation method thereof. The nanometer drug delivery system is composed of a polymer and ZL006 cyclohexyl ester, the weight ratio of the polymer material to ZL006 cyclohexyl ester is (5-15):1. The ZL006 cyclohexyl ester polymer nanometer drug delivery system can be obtained through an emulsified solvent evaporation method. The ZL006 cyclohexyl ester polymer nanometer drug delivery system is small in particle size, high in entrapment rate and large in drug loading capacity, and the solubility of theZL006 cyclohexyl ester is effectively improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a ZL006 cyclohexyl ester polymer nanocarrier 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 four highs (high incidence rate, high disability rate, high mortality rate and high recurrence rate), and it is listed as the second largest disease in human beings. The third leading killer of cardiovascular diseases and malignant tumors. Clinically, 87% of cerebral apoplexy is ischemic apoplexy, so the research on drug treatment of ischemic apoplexy has great clinical signif...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K47/34A61K31/606A61P9/10
CPCA61K47/34A61K47/36A61P9/10A61K31/606
Inventor 辛洪亮徐剑培李新瑞尹昊媛
Owner NANJING MEDICAL UNIV
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