Multi-bioactivity modified lignin self-assembled drug-loaded nano-micelle and preparation method thereof
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A biologically active, 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 abundant raw material sources, low cost, and simple processes. Effect
Active Publication Date: 2020-10-09
CENTRAL SOUTH UNIVERSITY OF FORESTRY AND TECHNOLOGY
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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.
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Embodiment 1
[0036] A method for preparing multi-biologically active modified lignin self-assembled drug-loaded nano-micelles, specifically comprising the following steps:
[0037] Step 1, the lignin of 2.00g, 0.49g (5.0mmol-CO 2 ) of maleic anhydride, 25mg (0.2mmol) of 4-dimethylaminopyridine (DMAP) were added to 30mL of N,N-dimethylformamide (DMF), and reacted in a constant temperature water bath at 50°C for 4h while stirring. After the reaction, add 300mL of pure water to make it precipitate, filter, wash with pure water three times, then wash with absolute ethanol three times, and dry under vacuum at 50°C to obtain acylated lignin, that is, 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 to a 100 mL round bottom flask After stirring for 5 min, slowly add 10 mL of 114 mg (0.6 mmol) of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride dropwis...
Embodiment 2-8
[0046] The parameter comparison table of embodiment 1 and embodiment 2-8 is shown in table 1 for details:
[0047] Among them: alkali lignin, enzymatic lignin, kraft lignin and kraft lignin are represented by A1-A4 respectively; 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 above-mentioned embodiment 2-8 are the same as embodiment 1.
[0051] See Table 2 for the drug loading data of Examples 1-8.
[0052] Table 2 The drug loading rate table of embodiment 1-8 product entrapped ibuprofen (the initial charging amount 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 15.79 15....
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Abstract
The invention provides a multi-bioactivity modified lignin self-assembled drug-loaded nano-micelle. The multi-bioactivity modified lignin self-assembled drug-loaded nano-micelle is prepared by acylating lignin modified by anhydride and then modifying the acylated lignin by a bioactive compound. The bioactive compound has a variety of biological activities, lignin is subjected to acylation, esterification and other reactions to prepare the lignin grafted bioactive compound, then the lignin grafted bioactive compound is prepared into the nano-micelle, and the nano-micelle is adopted as a good drug carrier, and further has a variety of biological activities of lignin and the bioactive compound; the bioactive compound and the lignin are connected together through chemical bonds, and the nano-micelle is self-assembled by utilizing the amphipathy of the lignin, so that the utilization rate of the bioactive compound can be greatly improved; a hydrophobic unit of the bioactive compound is introduced into the lignin, so that the drug loading capacity of the nano-micelle to hydrophobic drugs can be greatly improved. The invention further provides a preparation method of the multi-bioactivitymodified lignin self-assembled drug-loaded nano-micelle, the process is simple, and the drug-loading capacity of the micelle is good.
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 nano-micelle and a preparation method thereof. Background technique [0002] Lignin is an amorphous polymer composed of phenylpropane units linked 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 in the plant world after cellulose, with an annual global output of about 50 million tons. [0003] Due to the presence of active groups such as aromatic groups, phenolic hydroxyl groups, alcoholic hydroxyl groups, and carbon-based conjugated double bonds in the molecular structure of lignin, it can undergo oxidation, reduction, hydrolysis, alcoholysis, acidolysis, photol...
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