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A kind of zl006 liposome and preparation method thereof

A technology of liposomes and lipid bilayers, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations of inactive ingredients, etc., can solve the problems of limited ability to penetrate the blood-brain barrier and limited therapeutic effects, To achieve the effect of simple and reliable preparation method, stable quality and clear appearance

Inactive Publication Date: 2015-10-28
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the strong hydrophilicity of ZL006, the ability to penetrate the blood-brain barrier is limited, which limits its therapeutic effect to a certain extent

Method used

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  • A kind of zl006 liposome and preparation method thereof
  • A kind of zl006 liposome and preparation method thereof
  • A kind of zl006 liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the preparation of ZL006 liposome

[0032] Using the ethanol injection method, accurately weigh 16.7mg of ZL006, 80mg of phospholipids (the phospholipids in the content of the invention can be used, soybean phospholipids are easier to obtain), 20mg of cholesterol, add 7.5mL of absolute ethanol, vortex to dissolve and mix evenly to obtain Organic phase; add the organic phase dropwise to the continuously stirring water phase at a temperature of 50°C and a stirring speed of 550rpm, wherein the water phase is an acetic acid-sodium acetate buffer solution with a pH of 4.0 and a concentration of 0.1mol / L; drop Continue to stir for 10 minutes under the same conditions after the addition is complete; then use an ultrasonic cell pulverizer to reduce the particle size, the ultrasonic conditions are ultrasonic power 475W, intermittent ultrasonic, ultrasonic 2s stop 3s, ultrasonic 5min in total; then reduce the organic solvent by rotary evaporation under reduced pressu...

Embodiment 2

[0035] Embodiment 2: the quality evaluation of ZL006 liposome

[0036] Appearance of liposome: relatively clear with blue opalescence.

[0037] Encapsulation efficiency (EE%) and drug loading (DL%) determination.

[0038] (1) HPLC method to establish ZL006 standard curve:

[0039] Chromatographic conditions, chromatographic column: Hanbon Phecda C18 (4.6mm×150mm, 5μm; Jiangsu Hanbon Technology Co., Ltd.); mobile phase: methanol-0.25mol / L pH6.0 acetate buffer (65:35; v / v ); Flow rate: 1.0ml / min; UV detection wavelength: 284nm; Column temperature: 30°C; Injection volume: 20μL.

[0040]Standard curve drawing: Accurately weigh 0.0252g of ZL006 dried at 105°C to constant weight in a 50mL volumetric flask, and dilute to the mark with mobile phase to obtain a standard stock solution with a concentration of about 504μg / 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 ...

Embodiment 3

[0050] Example 3: In vitro release of ZL006 liposomes

[0051] Precisely pipette 2mL of the prepared ZL006 liposome (containing about 2.5mg of ZL006) into the treated dialysis bag, tie both ends with a rope and put it into 50mL of release medium (add 0.5% Tween 80 acetate Buffer solution, pH 4.0 and pH 7.4, two parallel groups for each pH) Erlenmeyer flasks, shaking at a constant temperature at 37°C on a shaker, with a rotation speed of 160rpm, at 0, 0.25, 0.5, 0.75, 1, 1.5 , 2, 3, 5, 8, 12, 24, 36, and 48 h to take 0.5 mL of medium, and at the same time add fresh release medium of the same temperature and volume. After the medium taken out was filtered through a 0.22 μm microporous membrane, it was determined by HPLC.

[0052] Calculation of cumulative release (Q n ):

[0053] Q n = C n × V 0 + Σ i ...

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Abstract

The invention relates to a ZL006 liposome and a preparation method thereof. The liposome consists of a lipid bilayer and ZL006, wherein the weight ratio of the lipid material of the lipid bilayer to the ZL006 is (10-4):1. The ZL006 liposome can be prepared by a pouring method or a film dispersion method. The preparation using the pouring method comprises the following steps: dissolving the ZL006 and the lipid material into an organic solvent, and uniformly mixing to obtain an organic phase; adding the organic phase into a water phase, reducing the particle size and removing the organic solvent; and filtering through microfiltration membranes with different pore diameters to obtain the ZL006 liposome. According to the ZL006 liposome and the preparation method thereof provided by the invention, by selecting proper material composition and proper preparation technology, the ZL006 liposome with good quality is obtained, the particle size of the liposome is small, the encapsulation efficiency is high, and the stability is good.

Description

technical field [0001] The invention relates to a liposome substance and its preparation, especially the liposome of the new compound ZL006, its preparation method and application. Background technique [0002] Stroke is a neurological disease with high fatality, disability, and recurrence. Clinically, more than 80% of strokes are ischemic strokes. Studies have shown that under ischemic conditions, the excessive release of excitatory amino acids (such as glutamate) in brain tissue causes excessive activation of N-methyl-D-aspartate receptors (NMDAR), leading to NMDAR-PSD-95- The release of pathological nitric oxide (NO) increased through the nNOS pathway, suggesting that the generation of ischemic stroke may be related to the increased combination of nNOS in the cytoplasm and new PSD95 on the cell membrane. ZL006 is a small molecule nNOS-PSD-95 uncoupler with the chemical name 4-(2-hydroxy-3,5-dichlorobenzylamino)-2-hydroxybenzoic acid. The structure is shown in the figure...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/606A61K47/24A61K47/28A61P9/10
Inventor 徐群为辛洪亮吴琳王中元王宝彦赵越吕玲燕
Owner NANJING MEDICAL UNIV
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