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 encapsula

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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