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Adriamycin nano-particles and preparation method thereof

A technology of doxorubicin and nanoparticles, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., to achieve good biodegradability, improve curative effect, and good stability

Active Publication Date: 2012-07-11
CHANGZHOU INST OF ENERGY STORAGE MATERIALS &DEVICES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, among the existing anticancer drugs, there are only a few such as Doxil, which are prepared by physically loading doxorubicin, and there are few studies on the way of using other carriers to physically load doxorubicin, which is far from satisfying market needs

Method used

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  • Adriamycin nano-particles and preparation method thereof
  • Adriamycin nano-particles and preparation method thereof
  • Adriamycin nano-particles and preparation method thereof

Examples

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preparation example Construction

[0061] The invention provides a method for preparing doxorubicin nanoparticles, comprising the following steps:

[0062] Doxorubicin is electrostatically compounded with a block copolymer having a structure of formula (I) or formula (II) in an aqueous medium to obtain doxorubicin nanoparticles.

[0063] According to the preparation method of doxorubicin nanoparticles of the present invention, the obtained doxorubicin nanoparticles exist in the aqueous medium in the form of micelles, and the fluid radius of the micelles is preferably 10 nm to 2000 nm, more preferably 10 nm to 2000 nm. 600nm.

[0064] Since the doxorubicin nanoparticles that exist in the form of micelles are not conducive to preservation, it is preferred to obtain the freeze-dried powder of doxorubicin nanoparticles through post-processing, and the post-processing preferably includes the following steps:

[0065] After obtaining the doxorubicin nanoparticle micelles, dialyze for 24h-72h, change the water for 6-...

Embodiment 1

[0083] The block copolymer having the structure of formula (III-a), m=45 and x=10 is denoted as mPEG 45 -b-PPLG 10 .

[0084] Add 0.2009g mPEG to the dry reaction vial 45 -b-PPLG 10 , after stirring and dissolving with 5mL N,N-dimethylformamide, after passing nitrogen for 0.5 hours, add 13.9mg benzoin dimethyl ether and 0.1636g mercaptosuccinic acid at room temperature under the condition of nitrogen protection, and react with 365nm ultraviolet light for 2h , to obtain the product; the product was dialyzed for 72 hours, the water was changed 12 times, and freeze-dried to obtain a block copolymer freeze-dried powder with a structure of formula (I-a).

[0085] The nuclear magnetic resonance test was carried out on the block copolymer, and the grafting rate was calculated to be 40.1%, and the reaction conversion rate was 68.5%.

Embodiment 2

[0087] The block copolymer having the structure of formula (III-a), m=45 and x=10 is denoted as mPEG 45 -b-PPLG 10 .

[0088] Add 0.2003g mPEG to the dry reaction vial 45 -b-PPLG 10 , after stirring and dissolving with 5mL N,N-dimethylformamide, after passing nitrogen for 0.5 hours, add 14.0mg benzoin dimethyl ether and 0.6543g mercaptosuccinic acid at room temperature under the condition of nitrogen protection, and react with 365nm ultraviolet light for 2h , to obtain the product; the product was dialyzed for 72 hours, the water was changed 12 times, and freeze-dried to obtain a block copolymer freeze-dried powder with a structure of formula (I-a).

[0089] The nuclear magnetic resonance test was carried out on the block copolymer, and the grafting rate was calculated to be 61.8%, and the reaction conversion rate was 30.2%.

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Abstract

The invention provides adriamycin nano-particles. The adriamycin nano-particles are prepared by compounding adriamycin and a block copolymer with a structure shown as a formula (I) or a formula (II) through electrostatic interaction. A preparation method for the adriamycin nano-particles comprises the following step of: electrostatically compounding the adriamycin and the block copolymer with thestructure shown as the formula (I) or the formula (II) in an aqueous medium to obtain the adriamycin nano-particles. In the aqueous medium, a poly(gamma-propargyl-L-glutamate-g-mercaptosuccinic acid)segment and a polyethylene glycol segment which are contained in the block copolymer wrap the adriamycin into cores of the nano-particles, so the adriamycin composite particles are high in stability.The nano-particles are expected to be gathered at tumor sites in blood circulation through an 'enhanced permeability and retention effect' so as to improve the targeting effect of the adriamycin on the tumor sites. Meanwhile, the electrostatic interaction between a carboxyl group of the block copolymer and an amino group of the adriamycin is easy to eliminate under the condition of low intracellular pH values, so that the intracellular release can be accelerated, and the medicinal effect can be improved.

Description

technical field [0001] The invention relates to the field of polymer medicine, in particular to doxorubicin nanoparticles and a preparation method thereof. Background technique [0002] Doxorubicin (DOX) belongs to anthracycline antibiotics, and its mechanism of action is that doxorubicin molecules are embedded in the double helix structure of DNA, changing the template properties of DNA, inhibiting nucleic acid synthesis, and playing an anti-tumor effect. Since the 1960s, doxorubicin has been widely used in clinical chemotherapy. At present, it is mainly used to treat acute leukemia, breast cancer, small cell lung cancer, gastric cancer, liver cancer, ovarian cancer, bladder cancer and other malignant tumors. Adriamycin is mostly administered in the form of intravenous infusion. After intravenous infusion, doxorubicin will be rapidly distributed throughout the body, with severe side effects, such as bone marrow suppression, hair loss, and cardiotoxicity. At the same time,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/704A61P35/00A61P35/02C08G69/48
Inventor 汤朝晖李明强宋万通吕世贤陈学思庄秀丽
Owner CHANGZHOU INST OF ENERGY STORAGE MATERIALS &DEVICES
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