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Multibiologically active modified lignin self-assembled drug-loaded nanomicelles and preparation method thereof

A biologically active and drug-loaded nanotechnology, which is applied in the direction of pharmaceutical formulations, organic active ingredients, and medical preparations of non-effective ingredients, can solve problems that have not been related to research, and achieve rich raw material sources, simple processes, and low cost. Effect

Active Publication Date: 2022-07-22
CENTRAL SOUTH UNIVERSITY OF FORESTRY AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current research only stays on lignin as a carrier, and there is no relevant research on the application of lignin and active organisms in the field of drug delivery.

Method used

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  • Multibiologically active modified lignin self-assembled drug-loaded nanomicelles and preparation method thereof
  • Multibiologically active modified lignin self-assembled drug-loaded nanomicelles and preparation method thereof
  • Multibiologically active modified lignin self-assembled drug-loaded nanomicelles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] A method for preparing multi-biologically active modified lignin self-assembled drug-loaded nanomicelles specifically includes the following steps:

[0037] Step 1, 2.00g of lignin, 0.49g (5.0mmol-CO 2 ) of maleic anhydride and 25 mg (0.2 mmol) of 4-dimethylaminopyridine (DMAP) were added to 30 mL of N,N-dimethylformamide (DMF) and reacted for 4 h under stirring in a constant temperature water bath at 50 °C. After the reaction, 300 mL of pure water was added to make it precipitate, filtered, washed three times with pure water, three times with absolute ethanol, and vacuum-dried at 50 °C to obtain acylated lignin acyl, namely maleylated lignin (MAL);

[0038]Step 2. Dissolve 2.0 g of MAL, 0.15 g (0.50 mmol) of ellagic acid (EA) and 3 mg (0.025 mmol) of 4-dimethylaminopyridine (DMAP) in 10 mL of DMF, and add it to a 100 mL round bottom flask After stirring for 5 min, 10 mL of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride dissolved in 114 mg (0.6 mmol) was s...

Embodiment 2-8

[0046] The parameter comparison table of embodiment 1 and embodiment 2-8 is shown in Table 1:

[0047] Among them: alkali lignin, enzymatic hydrolyzed lignin, sulfate lignin and kraft lignin are respectively represented by A1-A4; maleic anhydride, phthalic anhydride and succinic anhydride are represented by B1-B3 respectively; ellagic acid, white Veratrol and curcumin are represented by C1-C3, respectively.

[0048] The parameter comparison table of table 1 embodiment 1-8

[0049]

[0050] The process steps and other process parameters of the above-mentioned embodiments 2-8 are the same as those of the embodiment 1.

[0051] The drug loading rate data of Examples 1-8 are shown in Table 2.

[0052] Table 2 Example 1-8 product package drug loading rate table of ibuprofen (the initial charge of IBU is 50%)

[0053] serial number Example 1 Example 2 Example 3 Example 4 Example 5 Example 6 Example 7 Example 8 Drug loading rate (%) 17.55 15.637...

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Abstract

The invention provides a multi-biologically active modified lignin self-assembled drug-loaded nano-micelle, which is prepared from acylated lignin modified by an acid anhydride and then modified by a biologically active compound. Bioactive compounds have a variety of biological activities. Lignin is prepared by acylation, esterification and other reactions to prepare lignin-grafted bioactive compounds, which are then prepared into nanomicelles. The nanomicelles are good drug carriers and also have lignin and Various biological activities of biologically active compounds; the biologically active compounds of the present invention are linked together with lignin through chemical bonds, and the amphiphilic nature of lignin is used to self-assemble into nano-micelles, which can greatly improve the utilization rate of biologically active compounds; The introduction of a hydrophobic unit of a biologically active compound on the base can greatly improve the drug-carrying capacity of the nanomicelles for hydrophobic drugs. The invention also provides a preparation method of the above-mentioned multi-biologically active modified lignin self-assembled drug-loading nano-micelles, which has the advantages of simplified process and good drug-loading capacity of the micelles.

Description

technical field [0001] The invention relates to the technical field of lignin modification and utilization, in particular to a multi-biologically active modified lignin self-assembled drug-loaded nanomicelle and a preparation method thereof. Background technique [0002] Lignin is an amorphous polymer composed of phenylpropane units connected by carbon-carbon bonds and ether bonds. It is the second largest biomass resource in the plant kingdom after cellulose. As a typical biomass material, lignin is one of the few renewable resources among aromatic compounds. Lignin is the second largest resource of biomass material in the plant kingdom after cellulose, with an annual global output of about 50 million tons. [0003] Since there are active groups such as aromatic groups, phenolic hydroxyl groups, alcoholic hydroxyl groups, carbon-based conjugated double bonds in the molecular structure of lignin, it can be oxidized, reduced, hydrolyzed, alcoholysis, acidolysis, photolysis, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/34A61K47/22A61K47/10A61K31/192A61K31/337A61K31/704
CPCA61K9/1075A61K47/34A61K47/22A61K47/10A61K31/192A61K31/337A61K31/704
Inventor 罗卫华承良浩聂少飞罗淳译吴志平熊福全
Owner CENTRAL SOUTH UNIVERSITY OF FORESTRY AND TECHNOLOGY
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