Preparation method of epidoxorubicin lipidosome and application of epidoxorubicin lipidosome in resisting tumors

A technology of epirubicin fat and epirubicin, which is applied in the field of medicine to achieve significant effects, reduce toxicity, and improve drug efficacy

Inactive Publication Date: 2014-02-05
JIANGXI HERBFINE HI TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] There are still some deficiencies in the above two patents in terms of givi

Method used

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  • Preparation method of epidoxorubicin lipidosome and application of epidoxorubicin lipidosome in resisting tumors
  • Preparation method of epidoxorubicin lipidosome and application of epidoxorubicin lipidosome in resisting tumors
  • Preparation method of epidoxorubicin lipidosome and application of epidoxorubicin lipidosome in resisting tumors

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Experimental program
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Embodiment 1

[0031] Hydrogenated soybean lecithin (HSPC) and N-(carbonyl-methoxypolyethylene glycol-2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE-mPEG2000) in a molar ratio of 90 :10 dispersed in 300mM pH4 citric acid buffer solution at 70°C. After 1000 bar high-pressure homogenization, blank liposomes with a phospholipid concentration of 100 mg / ml and an average particle size of 50-300 nm were obtained. Add 2.0ml of epirubicin (5.0mg / ml) in trehalose (1g / ml) aqueous solution and 1.5ml of 0.4mM sodium carbonate solution into 2.0ml of blank liposomes, and incubate at 60°C for 30min. Then drug-loaded liposomes and blank liposomes were stored at -20°C. Liposomes without addition of cryoprotectant mPEG and trehalose were prepared by the same method. After storage at -20°C, the change in particle size was detected, and the results are shown in Table 1. The results showed that the particle size of the blank and drug-loaded liposomes added with the cryoprotectant did not change s...

Embodiment 2

[0035] Prepare epirubicin liposomes according to the method of Example 1, store the sample at -20°C for 6 months, and measure the content and particle size of the sample at the initial moment, 1 month, 3 months, and 6 months respectively , encapsulation efficiency, burst release percentage and pH value, the results are shown in Table 2. The results showed that the properties of the liposomes did not change significantly within 6 months, which proved that the storage method was reasonable and feasible.

[0036] Table 2 Effect of freezing / thawing process on liposome properties

[0037] time Content (epirubicin) (mg / ml) Particle size (nm) Encapsulation rate (%) Burst release percentage (%) pH value initial 2.01 101 99.9 8 7.88 1 month 1.99 103 99.8 7 7.91 3 months 1.97 104 99.7 8 7.87 6 months 1.98 107 99.8 9 7.92

Embodiment 3

[0039] 1.1 Inhibitory effect on transplanted tumors in animals

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Abstract

The invention belongs to the technical field of medicines, and relates to a preparation method of epidoxorubicin lipidosome and application of the epidoxorubicin lipidosome in resisting tumors. The epidoxorubicin lipidosome is prepared from epidoxorubicin, at least one phospholipid, as well as at least one surfactant, cryoprotectant or cholesterol. Pharmacodynamic tests prove that the epidoxorubicin lipidosome has a remarkable anti-tumor effect, and can be used for treating diseases including but not limited to liver cancer, lung cancer and gastric cancer.

Description

technical field [0001] The technology relates to the preparation of an epirubicin liposome and its antitumor application, belonging to the technical field of medicine. Background technique [0002] Epirubicin (Epirubicin, EPI) is an anthracycline anti-tumor antibiotic synthesized by Italian scholar Arcamone in 1975 through a semi-synthetic pathway. The mechanism of action is to directly intercalate between DNA base pairs, interfere with the transcription process, and prevent mRNA Therefore, it has effects on all stages of the cell cycle. It is a non-specific drug for the cell cycle and mainly acts on the nucleus. At present, epirubicin is mainly used clinically for various solid tumors such as acute leukemia and malignant lymphoma, breast cancer, ovarian cancer, bladder cancer, testicular cancer, gastric cancer, and liver cancer. There are many adverse reactions of epirubicin. In addition to the possible general adverse reactions of antineoplastic drugs (including myelosupp...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/704A61P35/00
Inventor 李俊李翔罗晓健陈兰英范玫玫何秀菊杨世林刘微
Owner JIANGXI HERBFINE HI TECH
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