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Method for preparing medicament carrying controlled-release nanometer material and application

A nano-material and drug-carrying technology, which is applied in pharmaceutical formulations, medical preparations of non-active ingredients, powder delivery, etc., can solve problems such as complex operation and silane coupling agent safety to be studied, and achieve strong biocompatibility , Improve drug bioavailability, effect of small particle size

Inactive Publication Date: 2011-01-26
中华人民共和国卫生部肝胆肠外科研究中心 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above process is complicated to operate, and the safety of silane coupling agent needs to be studied

Method used

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  • Method for preparing medicament carrying controlled-release nanometer material and application
  • Method for preparing medicament carrying controlled-release nanometer material and application
  • Method for preparing medicament carrying controlled-release nanometer material and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] step 1)

[0033] Prepare an aqueous solution of doxorubicin at a concentration of 5 mg / mL. Suction 3mL of silica nano-solution (average particle size 100nm, average shell thickness 15nm, shell average pore size 10nm, concentration 10mg / mL) for ultrasonic dispersion. The aqueous solution of doxorubicin was dripped (1ml / min) into the silica nano-solution, and after stirring at room temperature for 24 hours, the free drug was removed by dialysis to obtain the drug-loaded sandwich silica nano-solution.

[0034] step 2)

[0035] To prepare a polymer solution, first dissolve γ-PGA in deionized aqueous solution at a concentration of 1 mg / mL. At the same time, chitosan was dissolved in 1% acetic acid solution with a concentration of 1 mg / mL.

[0036] Inject the γ-PGA solution dropwise into step 1) to make the concentration of γ-PGA in the system reach 0.1% mg / mL, stir at room temperature for 1 hour, centrifuge the product, and wash it with deionized water for 2-3 times to fu...

Embodiment 2

[0040] Use a sandwich silica nanometer with an average particle size of 75nm (the average shell thickness is 12nm, the average pore diameter of the shell layer is 5nm, and the concentration is 9mg / mL) to replace the sandwich silica nanometer in step 1, and the concentration of doxorubicin is 1mg / mL instead of the doxorubicin concentration in step 1. Repeat the adsorption and washing process in step 2 alternately until four bilayer outer layers of γ-polyglutamic acid and chitosan membranes are obtained.

[0041] The sustained-release performance evaluation of the drug was the same as that in Example 1. The results showed that when pH=7.4, 25% was released within 180 hours; when pH=5, 30% was released within 180 hours. The composite support material is thus pH responsive. The drug loading of the composite carrier is 40%.

Embodiment 3

[0043] Use sandwich silica nanometers with an average particle size of 260nm (the average shell thickness is 20nm, the average pore diameter of the shell layer is 15nm, and the concentration is 15mg / mL) to replace the sandwich silica nanometers in step 1, and the concentration of doxorubicin is 15mg / mL instead of the doxorubicin concentration in step 1. The adsorption and washing process in step 2 were alternately repeated until three bilayer outer layers of γ-polyglutamic acid and chitosan films were obtained.

[0044] The sustained-release property evaluation of the drug was the same as in Example 1, and the results showed that, when pH=7.4, 65% was released within 180 hours; when pH=5, 50% was released within 180 hours. The composite support material is thus pH responsive. The drug loading of the composite carrier is 60%.

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Abstract

The invention relates to the field of medicaments, and mainly provides a method for preparing a medicament carrying controlled-release nanometer material and application. In the medicament carrying controlled-release nanometer material, sandwich silicon dioxide nanometer particles are taken as a carrier, and after medicaments are loaded into a cavity, gamma-polyglutamic acid and chitosan serving as outer-layer membranes are coated outside the nanometer material. The medicament carrying controlled-release nanometer material has the high medicament carrying rate, and the gamma-polyglutamic acid membrane and the chitosan serving as the outer-layer membranes can regulate the release of the medicaments in the cavity according to the change of external conditions so as to achieve the effect of releasing the medicament slowly and have certain targeting.

Description

technical field [0001] The invention relates to a preparation method and application of a drug-loaded silicon dioxide nanometer material for sustained and controlled release. Background technique [0002] After more than half a century of continuous development and improvement, chemotherapy has become one of the important means of comprehensive treatment of malignant tumors. However, the curative effect of chemotherapy has always been at a low level. The reason is that the amount of chemotherapy drugs is large, which has serious toxic and side effects on both cancerous and normal tissues. For example, doxorubicin has a broad anti-tumor spectrum and good curative effect, but the drug is highly toxic. In addition to bone marrow suppression and gastrointestinal side effects, long-term use can also cause dose-dependent irreversible cardiomyopathy, causing severe cardiotoxicity and liver damage are clinically largely limited [1] ; Temozolomide, as a new type of oral chemotherap...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/04A61K47/34A61K47/36
Inventor 张阳德刘勤龚连生康丽群汪建荣
Owner 中华人民共和国卫生部肝胆肠外科研究中心
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