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Folic acid-adriamycin immunological preparation for treating cancer through dual targets and preparation method thereof

A technology of doxorubicin and folic acid, which is applied in the preparation methods of peptides, chemical instruments and methods, and medical preparations of inactive ingredients, etc., can solve the problems of no cancer cells and long cycle.

Active Publication Date: 2014-06-18
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this therapy does not have the advantage of chemotherapy to directly kill cancer cells, and the period of efficacy is longer

Method used

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  • Folic acid-adriamycin immunological preparation for treating cancer through dual targets and preparation method thereof
  • Folic acid-adriamycin immunological preparation for treating cancer through dual targets and preparation method thereof
  • Folic acid-adriamycin immunological preparation for treating cancer through dual targets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1 Preparation of doxorubicin-bovine serum albumin conjugate shown in formula I

[0056] Take 100mg of bovine serum albumin (BSA) in a 100mL round bottom flask, add 3mL of 0.1M phosphate buffered saline (PBS) to dissolve to obtain BSA solution; weigh another 78mg of doxorubicin (ADM) and add 1mL of DMF to dissolve, To obtain the ADM solution, add the ADM solution to the above-mentioned BSA solution, and slowly drop in 75 μL of 20-fold diluted 25% glutaraldehyde solution while stirring. After reacting in the dark for 5 hours at room temperature, the reaction solution was centrifuged at 6000 rpm and -4°C for 10 minutes. , transfer the supernatant to a dialysis bag (molecular weight cut-off 8000-12000), dialyze in 0.01M PBS dialysis medium for 7 days, and refresh the dialysis medium 3 times a day. Then, the liquid in the dialysis bag was centrifuged at 6000 rpm at -4°C for 10 min, and the supernatant was taken and freeze-dried to obtain an orange-red solid powder, w...

Embodiment 2

[0059] Example 2 Investigation of the Immunogenicity of Adriamycin-Bovine Serum Albumin Conjugates as Shown in Formula I

[0060] Healthy New Zealand rabbits (commonly used animals for the preparation of polyclonal antibodies) were used to prepare polyclonal antibodies, and the immunogenicity of ADM-BSA provided in Example 1 was investigated. A total of 5 immunizations were performed (the first immunization and 4 booster immunizations). The first immunization operation is: weigh 1-4 mg of ADM-BSA provided in Example 1 and dissolve it in 0.5-4 mL of normal saline, add 0.5-3 mL of Freund's complete adjuvant to make a mixture, and inject the mixed solution subcutaneously at multiple points on the back of the rabbit. Solution 0.5-2mL / rat; booster immunization procedure: the second immunization was performed 1-5 weeks after the first immunization, with Freund's incomplete adjuvant, and the rest were the same as the first immunization. The next immunization is carried out every 2-5 ...

Embodiment 3

[0064] Example 3 Investigation of the Immunogenicity of Adriamycin-Bovine Serum Albumin Conjugates as Shown in Formula I

[0065] Prepare polyclonal antibody with healthy Balb / c mice (the next step of dual targeting research experimental model animals), investigate the immunogenicity of ADM-BSA provided in Example 1 to healthy Balb / c mice, and immunize 3 times (first immunization and 2 booster immunizations). The first immunization operation is: weigh 1-2 mg of ADM-BSA provided in Example 1, dissolve it in 0.5-2 mL of normal saline, add 0.5-3 mL of Freund's complete adjuvant to make a mixture, and inject it subcutaneously at multiple points on the back of the mouse Mixed liquid 0.05-1mL / mouse; three booster immunizations (due to the longevity of mice and the need for later treatment, 2 immunizations less than rabbits, but it will affect the activity of the antibody obtained), the specific operation is: perform the second immunization 1 to 3 weeks after the first immunization. ...

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Abstract

The invention relates to the field of pharmaceutical preparations and in particular relates to a pharmaceutical composition as well as application and a preparation method thereof. The pharmaceutical composition provided by the invention can be used for synergistically treating a tumor (a cancer) through dual actions of immunological therapy and active targeted drug therapy with remarkable curative effects. An adriamycin-bovine serum albumin conjugate as shown in a formula 1 is prepared from adriamycin and bovine serum albumin. The formula 1 is as shown in the specification.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition and its application and preparation method. Background technique [0002] Cancer, also known as malignant tumor (Malignant neoplasm), is a disease caused by the abnormal mechanism of controlling cell growth and proliferation. In addition to growing out of control, cancer cells can also locally invade the surrounding normal tissues and even transfer to other parts of the body through the circulatory system or lymphatic system in the body, which can destroy the structure and function of tissues and organs, cause necrosis, bleeding and infection, and eventually the patient suffers from organ failure. And die. Common cancers include blood cancer (leukemia), bone cancer, lymphoma (including lymphocytoma), colon cancer, liver cancer, stomach cancer, pelvic cancer (including uterine cancer, cervical cancer), lung cancer (including mediastinal canc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/765C07K1/107A61K39/00A61K31/704A61K47/48A61P35/00
CPCA61K39/00A61K39/385A61K47/545A61K47/643C07K14/765C07K19/00
Inventor 杨红吴秀凤邓安平龚珠萍梅丽芸黄晨蓉明志君刘扬
Owner SUZHOU UNIV
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