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Erythrocyte membrane-encapsulated tetrandrine PLGA nanoparticle and preparation method and application thereof

A technology of erythrocyte membrane and tetrandrine, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problems of short maintenance time of blood drug concentration, local pain or phlebitis, biological Problems such as low utilization can achieve the effects of prolonging blood half-life, delaying release, and reducing irritation

Inactive Publication Date: 2019-03-01
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still some problems, mainly: tablets are incompletely absorbed and have low bioavailability due to their poor water solubility and the first-pass effect of the liver; while ordinary injections are quickly metabolized in the body, blood drugs The concentration maintenance time is short, and tetrandrine is irritating to a certain extent, and intravenous injection may cause local pain or phlebitis

Method used

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  • Erythrocyte membrane-encapsulated tetrandrine PLGA nanoparticle and preparation method and application thereof
  • Erythrocyte membrane-encapsulated tetrandrine PLGA nanoparticle and preparation method and application thereof
  • Erythrocyte membrane-encapsulated tetrandrine PLGA nanoparticle and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0054] The preparation of embodiment 1 nanoemulsion (PTNs)

[0055] Weigh TET and PLGA (molecular weight: 30,000) respectively, add acetone to dissolve, so that the concentrations of TET and PLGA are 1mg / mL and 20mg / ml respectively, and then slowly add 1mL of the organic phase under the condition of magnetic stirring (300rpm) In the 20mL water phase, (the emulsifier in the water phase is poloxamer, and the emulsifier quality is 0.2g), so that the mass ratio of tetrandrine, PLGA, and emulsifier is that the mass ratio of the three is 1:20:200, The acetone was volatilized and removed by magnetic stirring at room temperature for 3 hours to obtain a nanoemulsion solution.

Embodiment 2

[0056] Example 2. Preparation of erythrocyte membrane

[0057] Take healthy rats, weigh them, anesthetize with 100g / 0.7mL intraperitoneal injection of chloral hydrate, take blood from the abdominal aorta, divide the blood into EP tubes containing 0.05mL heparin sodium, and centrifuge (3800rpm, 5min, 4°C) Remove the supernatant and white blood cell layer, add PBS solution to mix, repeat washing three times, and dilute to 1mL with PBS. Divide each tube of the mixed solution obtained at the above constant volume into four EP tubes containing 0.01mL heparin sodium, then add 0.9mL LEDTA solution (0.2mM), mix well, and lyse the red blood cells in the hypotonic medium to release hemoglobin, and then Then add 0.1mL 10 times concentration PBS and mix well, centrifuge (13200r / min, 10min, 4°C) to wash, remove the supernatant, keep the red blood cell membrane at the bottom, repeat this process more than three times until the supernatant is colorless. After removing the supernatant, add 0...

Embodiment 3

[0058] Example 3. Preparation of erythrocyte membrane vesicles (RVs)

[0059] Take the two tubes of red blood cell membranes prepared according to Example 2, thaw them in a 37°C water bath, first ultrasonicate the red blood cell membranes at a power of 100W and a frequency of 40KHz for 2min, and then use a thin film extruder to pass the vesicles obtained by ultrasound through 800 , 400 and 200nm polycarbonate films were extruded, and the extrusion was repeated 10 times under each particle size to obtain RVs.

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Abstract

The invention belongs to the technical field of pharmacy and particularly relates to an erythrocyte membrane-encapsulated tetrandrine PLGA nanoparticle and a preparation method and application thereof. The nanoparticle structurally includes an erythrocyte membrane, PLGA and tetrandrine, the tetrandrine is combined with PLGA to form a tetrandrine-PLGA nanocore, and the erythrocyte membrane is encapsulated outside the tetrandrine-PLGA nanocore. The preparation method is simple and efficient. The nano preparation improves the biocompatibility of a whole drug delivery system, long circulation andsustained release of the tetrandrine in the human body are achieved, toxic and side effects caused by too high blood medicine peak concentration of common injections are avoided, and the nanoparticlehas a good application prospect.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to tetrandrine PLGA nanoparticles encapsulated by red blood cell membranes and a preparation method and application thereof. Background technique [0002] Tetrandrine (TET), also known as Tetrandrine, is a bisbenzylisoquinoline alkaloid extracted from the tuber root of Stephaniatetrandra S. Moore. Modern pharmacological research has found that tetrandrine has good effects in anti-inflammatory analgesia, anti-virus, anti-pulmonary fibrosis, anti-silicosis, anti-tumor, anti-hypertension, anti-myocardial ischemia, anti-arrhythmia, etc. It has been widely used in the treatment of rheumatic pain, joint pain, silicosis, inflammatory lung disease, autoimmune disease and high blood pressure. [0003] The preparations of tetrandrine already on the market include "tetrandrine tablet" and "tetrandrine injection". However, there are still some problems, mainly: tablets are incomp...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K9/51A61K47/46A61K47/34A61K31/4748A61P9/06A61P9/10A61P9/12A61P11/00A61P29/00A61P31/12A61P35/00
CPCA61K9/5153A61K9/5176A61K31/4748A61P9/06A61P9/10A61P9/12A61P11/00A61P29/00A61P31/12A61P35/00
Inventor 邱明丰阙晓苏靖徐恩格刘思雨吴欣怡
Owner SHANGHAI JIAO TONG UNIV
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