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Blood-brain barrier drug delivery system and its preparation method and application

A delivery system and blood-brain barrier technology are applied in the field of cross-blood-brain barrier drug delivery system and its preparation, which can solve the problem of poor efficacy of glioma chemotherapy and achieve good drug delivery effect, easy operation, easy synthesis and controllability Effect

Active Publication Date: 2021-12-17
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the inherent sensitivity of tumors to drugs, the limited absorption of tumor cells to drugs, intracellular drug metabolism and cellular drug resistance mechanisms are all important reasons for the poor efficacy of glioma chemotherapy.

Method used

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  • Blood-brain barrier drug delivery system and its preparation method and application
  • Blood-brain barrier drug delivery system and its preparation method and application
  • Blood-brain barrier drug delivery system and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Preparation of polydopamine nanoparticles. Mix 3 milliliters of ammonia water, 40 milliliters of ethanol, and 90 milliliters of distilled water, and stir for 30 minutes at a temperature of 30 degrees Celsius and a magnetic stirrer speed of 500 rpm. After stirring, take 0.5 gram of dopamine hydrochloride and dissolve it in 10 milliliters of ultrapure water, and add it to the solution described in step 1), at a temperature of 30 degrees Celsius, a magnetic stirrer rotating speed of 500 rpm , reacted for 24 hours. After the reaction, centrifuge with a high-speed centrifuge (13800 rpm) and wash with water, repeating three times.

[0033] The polydopamine nanoparticles have a diameter of 176.24 nanometers and a potential of -51.5 millivolts.

Embodiment 2

[0034] Example 2: Preparation of polydopamine nanoparticles, 75 mg of dopamine hydrochloride was weighed and dissolved in 55 ml of ultrapure water, and 350 microliters of 1 mole per liter of sodium hydroxide solution was added dropwise to adjust the pH of the solution to 8.5. The mixture was reacted for 5 hours at a temperature of 45 degrees Celsius and a magnetic stirrer with a rotational speed of 500 rpm. After the reaction, centrifuge (13800 rev / min) with high-speed centrifuge and wash with water, repeat three times.

[0035] The polydopamine nanoparticles have a diameter of 135.34 nanometers and a potential of -30.9 millivolts.

Embodiment 3

[0036] Example 3: Preparation of polydopamine nanoparticles, 10 mg of dopamine hydrochloride was weighed and dissolved in 30 ml of 100 mmol / L tris buffer solution, the pH of the solution was controlled to be 8.5, and the reaction was carried out for 6 hours. After the reaction, centrifuge (13000-20000 revolutions per minute) and wash with water, repeat three times.

[0037] The polydopamine nanoparticles have a diameter of 160.83 nanometers and a potential of 22.8 millivolts.

[0038] figure 1 The particle size diagrams of polydopamine nanoparticles prepared in Experimental Examples 1-3 are shown; Examples 1-3 correspond to methods 1, 2, and 3, respectively.

[0039] Example 2 is the optimal example, and Example 2 is used as the preparation method of polydopamine nanoparticles to prepare highly efficient drug-loading composite nanomicelles for glioma:

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Abstract

The invention belongs to the field of drug delivery systems, and in particular relates to a novel cross-blood-brain barrier drug delivery system and its preparation method and application. A novel cross-blood-brain barrier drug delivery system consists of amphiphilic peptide-encapsulated micelles of polydopamine nanoparticles. The diameter of the micelles is 160-270 nanometers, and the potential is 10-30 millivolts. The diameter of polydopamine nanoparticles is 120-200 nanometers, and the potential is -60-40 millivolts. The novel trans-blood-brain barrier drug delivery system of the present application has: (1) good biocompatibility and biodegradability. (2) Easy operation and controllable synthesis enable large-scale production of nanoparticles. (3) The strong functionalization ability makes the nanoparticles easy to be modified by some targeting molecules and has good drug delivery effect. (4) It has high diagnosis and treatment efficiency.

Description

technical field [0001] The invention belongs to the field of drug delivery systems, in particular to a blood-brain barrier drug delivery system and its preparation method and application. Background technique [0002] One of the most common and aggressive primary brain malignancies is glioma arising from glial cells, and the treatment of these malignant gliomas is one of the most daunting challenges in oncology. Despite the combination of radiotherapy, chemotherapy and surgery, the prognosis of patients with malignant glioma is still poor, with an average survival period of 15 to 22 months. Due to the infiltrative growth of glioma, it is difficult to completely resect the tumor while preserving important brain functions. Non-invasive treatment is a promising direction to improve the living conditions of glioma. However, one of the most notable hurdles behind the disappointing results in glioma treatment is the presence of the blood-brain barrier (BBB) ​​and blood-tumor bar...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/42A61K47/34A61K41/00A61P35/00
CPCA61K9/1075A61K47/42A61K47/34A61K41/0052A61P35/00
Inventor 刘哲张晨刘晨熙何文心焦典
Owner TIANJIN UNIV
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