Composite micro-sphere co-carrying adriamycin nanoparticles and ginsenoside rh2 and preparation method thereof

A technology of doxorubicin hydrochloride and ginsenosides, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, microcapsules, etc., can solve the problem of unsatisfactory clinical test results and affect the pharmacokinetics of anticancer drugs It can improve the anti-tumor effect, reduce the toxic and side effects, and achieve the effect of high encapsulation efficiency.

Active Publication Date: 2018-09-21
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, most of the currently used p-glycoprotein inhibitors have strong toxicity, and some inhibitors will also affect the pharmacokinetics and distribution of anticancer drugs, and the results of clinical trials are not satisfactory.

Method used

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  • Composite micro-sphere co-carrying adriamycin nanoparticles and ginsenoside rh2 and preparation method thereof
  • Composite micro-sphere co-carrying adriamycin nanoparticles and ginsenoside rh2 and preparation method thereof
  • Composite micro-sphere co-carrying adriamycin nanoparticles and ginsenoside rh2 and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] This example provides a composite microsphere co-loaded with doxorubicin hydrochloride nanoparticles and ginsenoside rh2. The preparation method is as follows:

[0053] (1) Precisely weigh a certain amount of doxorubicin hydrochloride, and prepare a doxorubicin hydrochloride solution with a concentration of 0.4 mg / ml with ultrapure water, and set aside. Accurately weigh a certain quality of sodium alginate (MW=75KDa) and chitosan (MW=50KDa), and prepare 3mg / ml sodium alginate solution and chitosan solution with ultrapure water, respectively, and adjust the pH to 6.00 and 5.50, filtered through a 0.22 μm filter membrane for later use. Place 10ml of 3mg / ml sodium alginate solution on a stirrer with a stirring speed of 500rpm, add 10ml of 0.4mg / ml doxorubicin hydrochloride solution, then slowly add 20ml of 3mg / ml chitosan solution dropwise to form doxorubicin hydrochloride Mycin polyelectrolyte nanoparticle suspension. The nanoparticle suspension was centrifuged at 15000...

Embodiment 2

[0062] This example provides a composite microsphere co-loaded with doxorubicin hydrochloride nanoparticles and ginsenoside rh2. The preparation method is as follows:

[0063] (1) Precisely weigh a certain amount of doxorubicin hydrochloride, and prepare a doxorubicin hydrochloride solution with a concentration of 0.4 mg / ml with ultrapure water, and set aside. Accurately weigh a certain quality of sodium alginate (MW=75KDa) and chitosan (MW=50KDa), and prepare 3mg / ml sodium alginate solution and chitosan solution with ultrapure water, respectively, and adjust the pH to 6.00 and 5.50, filtered through a 0.22 μm filter membrane for later use. Place 10ml of 3mg / ml sodium alginate solution on a stirrer with a stirring speed of 500rpm, add 10ml of 0.4mg / ml doxorubicin hydrochloride solution, then slowly add 20ml of 3mg / ml chitosan solution dropwise to form doxorubicin hydrochloride Mycin polyelectrolyte nanoparticle suspension. The nanoparticle suspension is centrifuged at 15000r...

Embodiment 3

[0070] This example provides a composite microsphere co-loaded with doxorubicin hydrochloride nanoparticles and ginsenoside rh2. The preparation method is as follows:

[0071] (1) Precisely weigh a certain amount of doxorubicin hydrochloride, and prepare a doxorubicin hydrochloride solution with a concentration of 0.4 mg / ml with ultrapure water, and set aside. Accurately weigh a certain quality of sodium alginate (MW=75KDa) and chitosan (MW=50KDa), and prepare 3mg / ml sodium alginate solution and chitosan solution with ultrapure water, respectively, and adjust the pH to 6.00 and 5.50, filtered through a 0.22 μm filter membrane for later use. Place 10ml of 3mg / ml sodium alginate solution on a stirrer with a stirring speed of 500rpm, add 10ml of 0.4mg / ml doxorubicin hydrochloride solution, then slowly add 20ml of 3mg / ml chitosan solution dropwise to form doxorubicin hydrochloride Mycin polyelectrolyte nanoparticle suspension. The nanoparticle suspension is centrifuged at 15000r...

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Abstract

The invention relates to a composite microsphere for co-loading adriamycin nanoparticles and ginsenoside rh2 and a preparation method thereof, wherein the preparation method comprises the following steps: (1) preparing adriamycin hydrochloride and a nanoparticle carrier material into doxorubicin polyelectrolyte nanoparticles; (2) dispersing the adriamycin polyelectrolyte nanoparticles in water toform a nano-particle suspension, and dispersing the nano-particle suspension in an organic solution containingginsenoside rh2 and a high-molecular polymer to prepare S / W1 / O colostrum; (3) adding the S / W1 / O colostrum into an aqueous solution containing an emulsifier to prepare S / W1 / O / W2 complex milk; (4) solidifying the S / W1 / O / W2 complex emulsion into microspheres, collecting the microspheres, washing and drying. The microsphere prepared by the method can achieve the sequential release, slow release of doxorubicin hydrochloride and ginsenoside rh2,and has the advantages of low burst release rate and high encapsulation rate.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a composite microsphere co-loading doxorubicin hydrochloride nanoparticles and ginsenoside rh2 and a preparation method thereof. Background technique [0002] Breast cancer is one of the common malignant tumors in women, and 500,000 women die of breast cancer every year in the world. Chemotherapy occupies a very important position in the systemic treatment of breast cancer, but the multidrug resistance to chemotherapy in breast cancer patients is still the main cause of clinical treatment failure and poor prognosis. There are many reasons for multidrug resistance, among which, the overexpression of p-glycoprotein is currently recognized as the main cause of multidrug resistance. Doxorubicin hydrochloride is a broad-spectrum and powerful chemotherapy drug that kills cells by binding to the DNA of cancer cells. It is also one of the most commonly used chemotherapy drugs ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/113A61K47/36A61K31/704A61P35/00
CPCA61K9/113A61K9/5161A61K31/704A61P35/00A61K2300/00
Inventor 吴传斌杨莉朱春娥龙婕妤李静潘昕孙铭昊
Owner SUN YAT SEN UNIV
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