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Method of preparing gossypol and its derivative polydopamine nano-carrier by polymerization process

A technology of polydopamine nano and derivatives, which is applied in the direction of drug combination, pharmaceutical formula, medical preparations of non-active ingredients, etc., to achieve the effect of improving water solubility, high encapsulation rate, and broadening the scope of application

Active Publication Date: 2016-01-27
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, polydopamine-related inventions are mainly focused on the surface modification of existing materials and the encapsulation of hydrophilic drugs. There is no report on the invention of dopamine polymeric nanocarriers encapsulating hydrophobic drugs.

Method used

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  • Method of preparing gossypol and its derivative polydopamine nano-carrier by polymerization process
  • Method of preparing gossypol and its derivative polydopamine nano-carrier by polymerization process
  • Method of preparing gossypol and its derivative polydopamine nano-carrier by polymerization process

Examples

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Embodiment 1

[0024] refer to figure 1 , this embodiment includes the following steps:

[0025] Step 1: Dissolve 0.3mg gossypol acetate in 0.5mL methanol, disperse under 100kHz ultrasound, and the dispersion time is 3 minutes to make a mixed solution;

[0026]Step 2: Add the mixed solution dropwise to 10 mL of tris-hydrochloric acid buffer solution with a pH value of 9 at a rate of 4 drops per minute while stirring, and the stirring speed is 200 rpm. , keep the speed and continue stirring for 5 minutes;

[0027] Step 3: Add 3.0 mg of dopamine to the above system, and keep stirring at room temperature for 4 hours;

[0028] Step 4: Put the obtained product into a dialysis bag with a molecular weight cut-off of 1000 Daltons, and dialyze in tris-hydrochloric acid buffer for 24 hours to remove uncoated drugs.

[0029] The particle size of the nanocarrier obtained in this embodiment is measured by a Malvern particle size analyzer, referring to figure 2 Middle a is the measurement result of t...

Embodiment 2

[0032] This embodiment includes the following steps:

[0033] Step 1: Dissolve 0.6mg gossypol acetate in 0.5mL ethanol, disperse under 100kHz ultrasound, and disperse for 30 minutes to make a mixed solution;

[0034] Step 2: Add the mixed solution dropwise to 20 mL of a 1 mg / mL sodium hydroxide dilute solution with a pH value of 10 at a rate of 8 drops per minute while stirring, and the stirring speed is 300 rpm. After the dropwise addition is completed, Keep stirring continuously for 10 minutes;

[0035] Step 3: Add 6.0 mg of dopamine to the above system, and keep stirring at room temperature for 8 hours;

[0036] Step 4: Put the obtained product into a dialysis bag with a molecular weight cut-off of 1000 Daltons, and dialyze in the same weak alkaline buffer as in Step 2 for 24 hours to remove uncoated drugs.

[0037] The particle size of the nanocarriers obtained in this example was measured by a Malvern particle size analyzer. refer to figure 2 Middle b is the measurem...

Embodiment 3

[0040] This embodiment includes the following steps:

[0041] Step 1: Dissolve 1.0mg of apogossypol in 1.0mL of ethanol, and disperse under 100kHz ultrasound for 5 minutes to make a mixed solution;

[0042] Step 2: Add the mixed solution dropwise to 25 mL of disodium hydrogen phosphate-sodium dihydrogen phosphate buffer solution with a pH value of 8.5 while stirring at a rate of 20 drops per minute, the stirring speed is 400 rpm, and the addition is completed After that, keep the speed and continue to stir for 10 minutes;

[0043] Step 3: Add 10 mg of dopamine to the above system, and keep stirring at room temperature for 15 hours;

[0044] Step 4: Put the obtained product into a dialysis bag with a molecular weight cut-off of 1000 Daltons, and dialyze in the same weak alkaline buffer as in Step 2 for 48 hours to remove uncoated drugs.

[0045] The particle size of the nanocarrier obtained in this embodiment is measured by a Malvern particle size analyzer, referring to fig...

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Abstract

A method of preparing gossypol and its derivative polydopamine nano-carrier by the polymerization process includes: dissolving gossypol or its derivatives in an organic solvent, dropwise adding in a weakly alkaline buffer the organic solvent in which the gossypol or its derivatives is dissolved, adding dopamine into the buffer, and allowing reacting at room temperature for 4-72 hours. The weakly alkaline buffer is used to dialyze the polydopamine nano-carrier encapsulating the gossypol and its derivative, with un-covered drugs removed; the method is simple and quick, drug covering rate and drug carrying capacity are higher, especially the need for a surfactant is avoided, and thus the method is a simple, easy novel process of encapsulating the gossypol and its derivatives with dopamine.

Description

technical field [0001] The invention relates to a preparation method of a drug-loaded nano-carrier, in particular to a method for preparing a polydopamine nano-carrier of gossypol and its derivatives by polymerization. carrier method. Background technique [0002] Gossypol is a natural yellow polyphenolic compound that exists in the roots, stems and seeds of plants of the family Gossypiaceae. Due to its molecular structure, gossypol has two optical isomers, left-handed and right-handed, and has certain antibacterial, antiviral, antitumor, anti-inflammatory and antimalarial effects. In terms of anti-tumor, gossypol exhibits inhibitory effects on the survival, growth, proliferation and metastasis of various tumor cells, including human prostate cancer PC-3 cell line, human prostate cancer DU-45 cell line, head and neck squamous cells Lines, bladder cancer cell lines, multiple myeloma cell lines, leukemia cell lines, liver cancer cell lines and gastric cancer cell lines, etc....

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/11A61P31/04A61P31/12A61P35/00A61P29/00A61P33/06C08G73/02
Inventor 吴道澄马静文吴宥伸曾鋆申世红
Owner XI AN JIAOTONG UNIV
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