Biocompatible boric acid nano-drug compound as well as preparation method and application thereof

A nano-drug, biocompatible technology, applied in the fields of material science and biomedicine, can solve the problems of ineffective nano-delivery carrier, slow metabolism, low drug-carrying rate, etc., achieve remarkable cancer treatment efficiency, high biological safety, High biocompatibility effect

Active Publication Date: 2018-11-02
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] 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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  • Biocompatible boric acid nano-drug compound as well as preparation method and application thereof
  • Biocompatible boric acid nano-drug compound as well as preparation method and application thereof
  • Biocompatible boric acid nano-drug compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1 This example involves the size comparison of BTZ / TA / F127, BTZ / TA / PVA and BTZ / TA / PVP and the morphology of BTZ / TA / PVP.

[0055] Bortezomib (BTZ) and tannic acid (TA) were mixed in dimethyl sulfoxide solution at room temperature (mass ratio 1:1.443), and then added dropwise to polyvinyl alcohol (PVA) and polyoxyethylene The aqueous solution of oxypropylene ether block copolymer (F127) was stirred for 10s to form BTZ / TA / F127 and BTZ / TA / PVA complexes. Then the BTZ / TA / F127 and BTZ / TA / PVA complexes were placed in phosphate buffer, and the particle size of the complexes was detected by dynamic light scattering.

[0056] Bortezomib (BTZ), tannic acid (TA) and polyvinylpyrrolidone (PVP) were mixed in dimethyl sulfoxide solution at room temperature (mass ratio 1:1.475:1.75), then added dropwise to water and stirred for 10 s to form BTZ / TA / PVP complex, the BTZ / TA / PVP complex was placed in aqueous solution and phosphate buffer solution respectively, and the size and shap...

Embodiment 2

[0060] Example 2 This example relates to the stability of the BTZ / TA / PVP complex in different physiological environment solutions over time.

[0061] The BTZ / TA / PVP complex prepared in Example 1 was respectively placed in water, phosphate buffer and 10% fetal bovine serum, and its stability over time under different physiological conditions was observed by dynamic light scattering.

[0062] Experimental results:

[0063] Such as Figure 4 Shown, the size change of BTZ / TA / PVP complex over time in water, phosphate buffer and 10% fetal calf serum, the results show that, over time, within 48 hours, BTZ / TA / PVP The complexes can exist stably in the different physiological environments mentioned above.

Embodiment 3

[0064] Example 3 This example relates to the release pattern of the bortezomib component in the BTZ / TA / PVP complex at different pH values.

[0065] The BTZ / TA / PVP complex prepared in Example 1 was dialyzed, and then the dialyzed BTZ / TA / PVP complex was packaged in a dialysis bag (molecular weight cut-off was 3500), and then placed in phosphoric acid with different pH In the buffer solution, the content of bortezomib in the phosphate buffer solution was regularly detected by high performance liquid chromatography (the elution ratio of bortezomib, methanol:water=7:3), and then its release curve was drawn.

[0066] Experimental results:

[0067] Such as Figure 5 Shown, under different pH, the release law of bortezomib monomer in BTZ / TA / PVP complex, the result shows, when pH is 7.4, bortezomib basically does not release; As pH approaches tumor microenvironment (pH = 6.5) and endosomes (pH = 5.0), the release of bortezomib components was greatly increased, indicating that the BTZ...

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Abstract

The invention provides a biocompatible boric acid nano-drug compound and preparation method thereof, wherein the composition comprises natural polyphenols, boric acid drugs and high molecular compounds. In an organic solvent, boric acid drugs are firstly mixed with natural polyphenols to obtain a compound containing boric acid drugs and natural polyphenols, and then the previously obtained compound is mixed with the high-molecular compound to obtain a boric acid anticancer nano-drug compound containing boric acid drugs, natural polyphenols and high-molecular compounds, the nano-drug compound has excellent tumor cell inhibition potency and biocompatibility, the preparation method provided by the invention is simple and safe, the prepared boric acid nano-drug compound can efficiently and safely carry out boric acid drug delivery, and has excellent medical value.

Description

technical field [0001] The invention belongs to the fields of material science and biomedicine, and relates to a biocompatible boric acid nano-medicine compound and 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/32A61K47/10A61K47/55A61K31/69A61K31/7024A61P35/00A61P29/00
CPCA61K9/5138A61K9/5146A61K31/69A61K31/7024A61K47/55A61P29/00A61P35/00A61K2300/00
Inventor 程义云桑华君
Owner EAST CHINA NORMAL UNIV
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