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Traceable boric acid nano-drug compound, preparation method and use thereof

A nano-drug and compound technology, applied in the fields of material science and biomedicine, can solve the problems of ineffective nano-delivery carrier, slow metabolism, low drug-loading rate, etc., and achieve remarkable cancer treatment efficiency, high biological safety, and biological Effect of Compatibility Guarantee

Active Publication Date: 2018-08-21
EAST CHINA NORMAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, most of today's nano-delivery vehicles have no therapeutic effect on their own
Due to the low drug loading rate of some carriers, refractory degradation, slow metabolism, difficult excretion and other factors, severe toxicity and inflammatory reactions in the kidneys and other organs will occur

Method used

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  • Traceable boric acid nano-drug compound, preparation method and use thereof
  • Traceable boric acid nano-drug compound, preparation method and use thereof
  • Traceable boric acid nano-drug compound, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 This example involves the size comparison of BTZ / TA and BTZ / TA / Iron composites and the morphology of BTZ / TA / Iron

[0039] The boric acid nano-drug bortezomib (BTZ) and natural polyphenol tannic acid (TA) were mixed in DMSO at room temperature (mass ratio 1:0.88), and then added with iron ions (Fe 3+ ) in an aqueous solution and stirred for 10 s to form a complex. The complexes were placed in aqueous solution and phosphate buffer solution respectively, and the size and shape of the complexes were observed by dynamic light scattering and transmission electron microscopy.

[0040] Experimental results:

[0041] Such as figure 1 A and B in the figure show the sizes of BTZ / TA and BTZ / TA / Iron complexes in aqueous solution and phosphate buffer, respectively. figure 2 Shown is the electron microscope morphology of the BTZ / TA / Iron complex in phosphate buffer. The results show that compared with BTZ / TA, the BTZ / TA / Iron complex with iron ions can exist stably in phos...

Embodiment 2

[0042] Example 2 This example relates to the stability of the BTZ / TA / Iron complex in different physiological environment solutions.

[0043] The prepared BTZ / TA / Iron complexes were placed in phosphate buffer, 10% fetal bovine serum and cell culture medium, and their stability over time under different physiological conditions was observed by dynamic light scattering.

[0044] Experimental results:

[0045] Such as image 3 Shown are the size changes of the BTZ / TA / Iron complex over time in phosphate buffered saline, 10% fetal calf serum, and cell culture The complexes can exist stably in different physiological environments.

Embodiment 3

[0046] Example 3 This example relates to the release rules of the bortezomib component and the tannic acid component of the BTZ / TA / Iron complex at different pH values.

[0047] The dialyzed BTZ / TA / Iron complex was packaged in a dialysis bag (molecular weight cut-off of 3500), placed in phosphate buffer solution with different pH, and the content of each monomer in the phosphate buffer solution was regularly detected by high performance liquid chromatography (The elution ratio of bortezomib, methanol:water=7:3; the elution ratio of tannic acid, 4% acetic acid:methanol=1:1), and then draw its release curve.

[0048] Experimental results:

[0049] Such as Figure 4 Shown in A and B in the BTZ / TA / Iron complex are the release rules of bortezomib monomer and tannic acid monomer at different pH values. The results show that when the pH value is 7.4, bortezomib and tannin There is basically no release of acid, and when the pH is close to the tumor microenvironment (pH=6.5) and the i...

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Abstract

The invention provides a traceable boric acid nano-drug compound and a preparation method thereof. The traceable boric acid nano-drug compound comprises natural polyphenol, a boric acid drug and ironions. The preparation method includes: in an organic solution, firstly mixing the boric acid drug with natural polyphenol, and then mixing the obtained product with iron ions to obtain the boric acidanticancer nano-drug compound containing the boric acid drug, natural polyphenol and iron ions. The traceable boric acid nano-drug compound can be used for tumor tracing and the like. The invention also puts forward application of the nano-drug compound in preparation of drugs for prevention and / or treatment of tumors and inflammatory diseases. The nano-drug compound also has tracing ability, canensure that anti-cancer drugs only take effect at tumor sites so as to reduce side effects, and has better biocompatibility and better therapeutic efficiency. The traceable boric acid nano-drug compound provided by the invention has the characteristics of simple and safe synthesis, efficient and safe delivery of boric acid drugs, and has excellent medical value.

Description

technical field [0001] The invention belongs to the fields of material science and biomedicine, and relates to a boric acid nano drug compound, a preparation method and application thereof. Background technique [0002] Natural polyphenols are a class of polyphenolic compounds widely present in plants, including phenolic acids and flavonoids, which can be eaten and drunk directly. There are several phenolic hydroxyl groups in the molecular structure of this polyphenolic compound. A number of in vivo and in vitro experiments have proved that this polyphenolic compound has significant functions of scavenging free radicals in the body, anti-oxidation, anti-ultraviolet rays, anti-obesity, prevention of cardiovascular diseases, anti- Inflammation, prevention and treatment of cancer, often used in health care products or additives in cosmetics. [0003] Bortezomib (BTZ), as a new type of proteasome inhibitor, has been used in the treatment of multiple myeloma. It improves the de...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/69A61K38/05A61K31/7024A61K31/353A61P35/00A61P29/00A61K49/00A61K49/06
CPCA61K31/353A61K31/69A61K31/7024A61K38/05A61K45/06A61K49/0019A61K49/06A61P29/00A61P35/00A61K2300/00
Inventor 程义云桑华君王长平李乙文
Owner EAST CHINA NORMAL UNIV
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