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Cis-aconitic anhydride bond adriamycin/human serum albumin (CAD/HSA) composition and preparation method and application thereof

A technology of aconitic anhydride-bonded doxorubicin and human serum albumin, which is applied in the field of pharmaceutical preparations and preparations of doxorubicin-coupled albumin, which can solve cell and tissue damage, toxic side effects, chemotherapy drugs lack of tumor cells or Issues such as tissue selectivity or targeting can achieve the effects of increasing accumulation, reducing heart and kidney toxicity, and improving safety

Pending Publication Date: 2022-06-03
LANZHOU UNIVERSITY
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0002] One of the main problems faced in cancer chemotherapy is that chemotherapy drugs lack selectivity or targeting to tumor cells or tissues, so the drugs are easy to cause damage to normal cells and tissues
Doxorubicin belongs to anthracycline antibiotics and is one of the most effective cytotoxic drugs. It can be used as a chemotherapeutic drug for various cancers, but it can also cause severe toxicity to other normal cells and tissues, especially the heart, nerves, and bone marrow. side effects, so doxorubicin needs to be dealt with accordingly, and it is particularly important to design an efficient drug-targeted delivery system

Method used

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  • Cis-aconitic anhydride bond adriamycin/human serum albumin (CAD/HSA) composition and preparation method and application thereof
  • Cis-aconitic anhydride bond adriamycin/human serum albumin (CAD/HSA) composition and preparation method and application thereof
  • Cis-aconitic anhydride bond adriamycin/human serum albumin (CAD/HSA) composition and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation process and characterization of CAD / HSA

[0028] (1) Preparation of cis-aconitic anhydride-bonded doxorubicin / human serum albumin (CAD / HSA) composition, the molar ratio of the cis-aconitic anhydride-bonded doxorubicin / human serum albumin (CAD / HSA) The ratio is 20:10:1.

[0029] Take 7mg cis-aconitic anhydride doxorubicin (CAD), 8mg 1-ethyl-(3-dimethylaminopropyl) carbodiimide salt (EDCI), 6mg N-hydroxysuccinimide (NHS) Dissolve in 3mL pH7.4 phosphate buffer and stir for 4 hours in the dark; then dissolve 66.7mg of human serum albumin (HSA) in 2mL pH7.4 phosphate buffer, add human serum to the reaction solution albumin (HSA) solution, stirred at room temperature for 24 hours, and finally centrifuged at 4000 rpm for 5 min to take the supernatant, dialyzed with a 25kD dialysis bag for 24 hours, and separated free cis-aconitic anhydride-bonded doxorubicin (CAD) with a SepHadex 25 column. The purified product was freeze-dried to obtain cis-aconitic an...

Embodiment 2

[0034] Example 2 Determination of DOX coupling ratio in CAD / HSA

[0035] Determination of DOX content by trypsin hydrolysis method: Weigh 5 mg CAD / HSA, add 1 mL of 250 μg / mL bovine trypsin, put it in a water bath at 37 °C for 5 hours, centrifuge at 10,000 rpm / min, and take the supernatant after 2 minutes. , and then use an ultraviolet spectrophotometer to measure the absorbance value at 490nm, and substitute it into the 490nm DOX ultraviolet standard curve to calculate the content.

[0036] Table 1 Content of DOX in 5 batches of CAD / HSA

[0037]

[0038] In order to determine the coupling ratio of DOX, a regression curve was used to determine the DOX content in the samples after hydrolysis. The regression curve of DOX Y=0.01835X(μg / mL)+0.01558(R 2 =0.9992).

[0039] Five batches of CAD / HSA samples were measured, and the calculated molar ratio was DOX:HSA=2-3:1 (n=5). It shows that HSA and DOX can be coupled within a certain range.

Embodiment 3

[0040] Example 3 In vitro acid-sensitive drug release experiment of CAD / HSA

[0041]Weigh 5mg CAD / HSA respectively, dissolve with 1mL buffer solution of pH 3.5, 5.0, 7.4, 9.0 in turn and put it into a 25KDa dialysis bag, add the dialysis bag in turn to a beaker containing a 50mL system of corresponding pH, and place it in the dialysis bag. In a constant temperature shaker at 37°C and 70rpm / min, take 1mL of the external buffer of each dialysis bag at 1, 2, 4, 8, 12, and 24 hours respectively, take three times in parallel, and then make up the corresponding pH buffer to 50mL, The F value of the samples at each time point was measured at 493 nm with a spectrofluorometer, and substituted into the DOX spectrofluorometer standard curve (Y=138.6X+21.45, R 2 =0.9961), calculate the content of DOX at each time point, and draw the in vitro release curve of CAD / HSA to study the sensitive response of CAD / HSA to different pH.

[0042] from image 3 It can be seen that CAD / HSA releases mo...

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Abstract

The invention relates to a folic acid / cis-aconitic anhydride bond adriamycin / human serum albumin (FA / CAD / HSA) composition as well as a preparation method and application thereof. The composition is a targeted drug delivery system formed by chemically coupling cis-aconitic anhydride bond doxorubicin and human serum albumin, has a pH-sensitive drug release function and a certain tumor targeting property, can reduce the toxicity of doxorubicin while killing tumor cells, and is beneficial to clinical application.

Description

technical field [0001] The invention belongs to the technical field of targeted drugs, and in particular relates to a drug preparation of doxorubicin-coupled albumin and a preparation method and application thereof. Background technique [0002] A major problem faced in cancer chemotherapy is the lack of selectivity or targeting of chemotherapy drugs to tumor cells or tissues, which makes them prone to damage normal cells and tissues. Doxorubicin belongs to the class of anthracyclines and is one of the most effective cytotoxic drugs. It can be used as a chemotherapeutic drug for many cancers, but it can also cause severe toxicity to other normal cells and tissues, especially the heart, nerves, and bone marrow. Therefore, it is necessary to deal with doxorubicin accordingly, and it is particularly important to design an efficient drug targeted delivery system. [0003] Although there are related patents that disclose the combination of doxorubicin and albumin, but there are ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/64A61K31/704A61K9/08A61K9/19A61P35/00A61P35/02
CPCA61K47/643A61K31/704A61K9/0019A61K9/08A61K9/19A61P35/00A61P35/02
Inventor 李红玉王加涛余兰邹玥乔志伟李洋
Owner LANZHOU UNIVERSITY
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