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Injectable amphiphilic block copolymer nano drug-loaded micelle

A technology of amphiphilic block and drug-loaded micelles, which is applied in antipyretics, anti-infectives, drug combinations, etc., and can solve the problem of difficult stability and uniform dispersion of microspheres, large molecular weight of side chain polylactic acid, and difficulty in the use of injection preparations And other problems, to achieve the effect of wide range of applicable drugs, uniform particle size, good physical and chemical stability

Pending Publication Date: 2022-03-15
苏州优诺康医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the goal of this patent is not to use the drug-loaded microspheres as a direct injectable preparation, and its side chain polylactic acid has a relatively large molecular weight, a high degree of polymerization, and a molecular weight of 1,0000-1,8000. Such a high molecular weight is difficult Delivery and release of drugs through the cell membrane or blood-brain barrier, and large agglomeration is prone to occur in the water phase, the resulting microspheres are not easy to disperse stably and evenly in the water phase, and it is difficult to be used clinically as an injection preparation

Method used

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  • Injectable amphiphilic block copolymer nano drug-loaded micelle
  • Injectable amphiphilic block copolymer nano drug-loaded micelle
  • Injectable amphiphilic block copolymer nano drug-loaded micelle

Examples

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Effect test

Embodiment 1

[0049] In this embodiment, the amphiphilic block copolymer PAA-C60-PLA is prepared, such as figure 1 , its structural formula is as follows:

[0050]

[0051] (1) Add 10 mg of silver sulfate and deionized water into a reaction kettle equipped with a reflux condenser, a stirrer, and a thermometer, start stirring, and heat the water bath to 70°C, and slowly add 100 g of acrylic acid and 20 g of hydrogen peroxide dropwise , dripping time 4h, reacting at the same time by dripping 10mol / L sodium hydroxide solution, control system pH = 5-6, after the end of the reaction, keep warm for 4h to get a light yellow viscous liquid, precipitate and filter and wash with deionized water , then add 200ml of water and heat to 70-80°C to dissolve, then add anhydrous ethanol to precipitate, cool and refine, and freeze-dry for 24 hours to obtain low molecular weight polyacrylic acid with an average molecular weight of 700-1200 and m=10-15. Yield 80-90%.

[0052] (2) Add a magnetic stir bar to...

Embodiment 2

[0057] Embodiment 2: Preparation of blank micelles and drug-loaded micelles with the amphiphilic block copolymer prepared in Example 1

[0058] (1) Preparation of blank micelles

[0059] Accurately weigh 50 mg of the amphiphilic block copolymer PAA-C60-PLA prepared in Example 1, dissolve it in 10 ml of methanol, shake until completely dissolved, add the methanol solution into a 50 ml rotary evaporator, evaporate the methanol to dryness, and form a thin film , and then add 5ml of pure water, fully hydrated by ultrasonic vibration, and a blank micellar solution can be obtained at 0.45 μm. The particle size distribution of the blank micelles is as follows Figure 4 As shown, the average particle diameter is 199.9nm, and the distribution index (PDI) is 0.280.

[0060] (2) Determination of critical micelle concentration CMC of blank micelles

[0061] Determination of Critical Micelle Concentration Blank micelles without drug were prepared. Prepare 5×104mol / L pyrene solution wit...

Embodiment 3

[0070] Micellar drug release experiment: Take 0.5ml of the drug-loaded micelles prepared in Example 2(4), add them into a 2KDa dialysis bag, put the dialysis bag into a 50ml centrifuge tube, and add 5ml of dialysis medium, the difference between the inner and outer volumes is more than 10 times Manufacturing sink conditions, shaking at 100rpm at 37°C. The dialysis media were divided into three groups: 1. pH7.4 phosphate buffer (PBS) + 10% fetal bovine serum; 2. pH6.8PBS; 3. pH5.5PBS. Each medium contained 1mol / L sodium salicylate. Among them, pH7.4 phosphate buffer solution (PBS)+10% fetal bovine serum simulates the blood environment, pH6.8PBS simulates the slightly acidic environment outside tumor cells, and the pH5.5PBS group simulates the conditions in the lysosome.

[0071] The dialysis medium was collected at 0.5h, 1h, 2h, 4h, 6h, 9h, 12h, 24h, 36h, and 48h, and the dialysis medium was replaced. 200 μl of the collected dialysis medium was added into the injection bottle...

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Abstract

The invention relates to an injectable amphiphilic block copolymer nano drug-loaded micelle, and relates to the field of drug carriers, hydrophobic fullerene, hydrophilic group agglomerated lactic acid and polyacrylic acid are chemically chimeric to prepare a micelle material with a pH response characteristic. The material is simple in preparation process, high in micelle hydrophilicity and good in drug loading capacity for insoluble hydrophobic drugs, and is a good carrier for preparing injection dosage forms. The drug-loaded micelle prepared from the material has good pH response under the action of lesion cell microenvironment and lysosome, and can release drugs more easily; in addition, animal experiments show that the vorinostat micelle prepared from the material has the pharmacodynamic effect of remarkably reducing peripheral bladder cancer cells on bladder cancer model mice compared with a traditional emulsion.

Description

technical field [0001] The invention belongs to the field of preparation of drug micelle preparations, in particular to a novel amphiphilic block copolymer drug-loaded micelle and a preparation method thereof. Background technique [0002] Block copolymer micelles are a new drug nanocarrier developed rapidly in recent years. In aqueous solution, the hydrophobic block in the amphiphilic block copolymer constitutes the core, and the hydrophilic block constitutes the shell, forming a block copolymer micelle with a spherical core-shell structure. Block copolymer micelles have the following advantages as drug carriers: (1) The critical micelle concentration (CMC) is low, with a high degree of thermodynamic and kinetic stability, and it is not easily destroyed even below the CMC, and has high resistance to dilution Ability; (2) Self-assemble in aqueous solution to form micelles, the inner core can be loaded with hydrophobic drugs, and the hydrophilic surface makes it difficult to...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/58A61K47/59A61K47/34A61K41/00A61K31/167A61K45/00A61P35/00A61P29/00A61P31/00C08G63/08C08G63/664C08G63/78C08G63/85
CPCA61K9/1075A61K47/58A61K47/593A61K47/34A61K41/0057A61K31/167A61K45/00A61P35/00A61P29/00A61P31/00C08G63/08C08G63/664C08G63/78C08G63/85A61K2300/00
Inventor 蔡世珍王立峰
Owner 苏州优诺康医药科技有限公司
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