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Amphiphilic targeting nanomaterial as well as nano preparation and application thereof

A nanomaterial and nanoformulation technology, applied in the field of new nano-targeted drug formulations, can solve problems such as toxic reactions, and achieve the effects of good stability, uniform particle size and high encapsulation efficiency.

Inactive Publication Date: 2016-07-20
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the non-targeted distribution of such drugs can lead to severe toxic reactions in the body, which has become a major bottleneck in cancer treatment today, and even makes patients more afraid of the side effects of chemotherapy drugs than the tumor itself

Method used

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  • Amphiphilic targeting nanomaterial as well as nano preparation and application thereof
  • Amphiphilic targeting nanomaterial as well as nano preparation and application thereof
  • Amphiphilic targeting nanomaterial as well as nano preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Preparation of targeted functional materials

[0033] (a) Take 2.1g polyethylene glycol stearate (PEG-SA, wherein PEG is 40 ethylene glycol molecules) and 3.0g benzyloxycarbonyl-lysine (Cbz-Lys) and dissolve in dichloromethane , adding 1 g of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) and 0.6 g of 1-4-N, N-lutidine (DMAP), in N 2 Stir magnetically in a water bath at 30°C for 24 hours under protection. After the reaction, wash and dry. After purification, the product (I) is obtained.

[0034] (b) Dissolve the product (I) in tetrahydrofuran, in palladium carbon (Pd / C) and H 2 Under the influence of magnetic stirring in a 30°C water bath for 6h. Filtrate, collect the filtrate, and rotate to evaporate to obtain the product (II). The synthetic route is shown in the following formula:

[0035]

[0036] Determination by NMR 1 H-NMR hydrogen spectrum to determine the structure of the functional polymer material in embodiment 1, the solvent selec...

Embodiment 2

[0038] Preparation of drug-loaded targeted nano-formulations (DTX-LPS-Lips)

[0039] Weigh 120mg of soybean lecithin, 30mg of cholesterol, 3mg of docetaxel, and 12mg of the targeted functional material prepared in Example 1, dissolve them in 10mL of dichloromethane into a 100mL eggplant-shaped bottle, shake evenly, and evaporate at 37°C for 30min to remove Organic solvents. Nitrogen flow (N 2 ) Blow the eggplant-shaped bottle to remove the residual organic solvent, add 3mL of pH7.4PBS, stir at 37°C for 1h to hydrate. Filter through a 0.22 μm filter membrane to remove unencapsulated drug, and obtain the product. The encapsulation efficiency of the drug-loaded targeting nano-preparation is over 94%.

[0040] The prepared drug-loaded targeted nano-preparation was measured by dynamic light scattering and scanning electron microscopy for its particle size and shape. The results are as follows: image 3 . The particle size of the lysine-modified active targeting nano-preparatio...

Embodiment 3

[0042] In vitro release of drug-loaded targeted nanoformulations

[0043]The in vitro drug release characteristics of the drug-loaded targeting nano-preparation prepared in Example 2 and the commercially available docetaxel agent (DTX-Sol) were investigated by dialysis. Pipette 500 μL of 1 mg / mL drug-loaded targeted nano-preparation or DTX-Sol into the dialysis bag, clamp both ends of the dialysis bag, place them in 30 mL of PBS release medium containing 0.5% Tween80 at pH 7.4, and place in a constant temperature shaker at 37 °C 100r / min for in vitro release test. Take 0.5 mL of samples at 0.5, 1, 2, 4, 8, 12, and 24 hours respectively, and supplement 0.5 mL of fresh release medium at the same time. The samples are filtered through a 0.45 μm microporous membrane, and 20 μL is taken for HPLC determination.

[0044] Figure 4 The results showed that the drug-loaded targeted nano-preparation had sustained-release characteristics under the condition of pH7.4PBS, which indicated ...

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Abstract

The invention relates to an amphiphilic targeting functional material based on high expression of tumor amino acid transporter ATB<0, +> and an application of nano preparation modified by the same in targeting therapy of tumor. In the amphiphilic targeting functional material, stearic acid (SA) serves as a hydrophobic end while amino acid (AA) serves as a target end, and the middle connection bridge is polyethylene glycol (PEG). The nano preparation modified by the amphiphilic targeting functional material can remarkably improve the tumor targeting ability of an active drug. The characteristics of the invention are that the targeting functional material is easy to prepare, and the nano preparation modified by the targeting functional material can actively target the amino acid transporter ATB<0, +> with high expression of tumor, has high biocompatibility and can remarkably improve the drug therapeutic effect.

Description

technical field [0001] The invention relates to an amphiphilic targeting nanomaterial and its nano-preparation and application, in particular to a novel amphiphilic targeting functional material and its modified nano-preparation with tumor-targeting properties, belonging to a novel nano-targeting drug Preparation field research. Background technique [0002] Chemotherapy remains an important treatment modality in the treatment of cancer. However, the non-targeted distribution of such drugs can lead to severe toxic reactions in the body, which has become a major bottleneck in cancer treatment today, and even makes patients more afraid of the side effects of chemotherapy drugs than the tumor itself. Therefore, developing an effective drug delivery system to deliver chemotherapy drugs to the target site, reduce the toxicity of non-target sites, improve clinical efficacy, and improve the quality of life of patients is one of the main strategies to solve this problem. [0003] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48A61K9/127A61K31/337A61K47/34A61P35/00
CPCC08G65/48A61K9/127A61K31/337A61K47/34
Inventor 孙进罗秋华何仲贵王永军孙英华刘晓红
Owner SHENYANG PHARMA UNIVERSITY
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