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PAMAM-TPGS as well as preparation method and application thereof

A technology of reaction solution and vitamins, which is applied in pharmaceutical formulations, medical preparations with inactive ingredients, powder delivery, etc., to achieve the effects of reducing strong cell toxicity, not easy to settle and precipitation, and good biocompatibility

Active Publication Date: 2022-03-18
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still some difficulties in the clinical application of drug carriers based on dendrimers. For example, dendrimers are quickly cleared by the monocyte phagocytic system (MPS) in vivo due to their surface electron-positive and easy formation of protein coronas on the surface.

Method used

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  • PAMAM-TPGS as well as preparation method and application thereof
  • PAMAM-TPGS as well as preparation method and application thereof
  • PAMAM-TPGS as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] The synthesis of embodiment 1 TPGS-COOH

[0071] Dissolve TPGS (0.3mmol, 459mg), SA (0.6mmol, 60mg), DIPEA (0.9mmol, 160μl), DMAP (0.06mmol, 7.2mg) in 15mL 1,4-dioxane, and fill with nitrogen protection, Reaction at room temperature for 24h. The solvent was removed by rotary evaporation, dissolved in 10ml of cold dichloromethane (0°C) solvent, added dropwise to 250ml of ice ether (-20°C), the precipitate was precipitated, and the precipitate was collected by centrifugation, dried in a vacuum drying oven to constant weight, and prepared TPGS-COOH was obtained, 32 mg of the product was obtained, and the final yield was 6.5%.

Embodiment 2

[0072] The synthesis of embodiment 2TPGS-COOH

[0073] Dissolve TPGS (0.3mmol, 459mg), SA (0.6mmol, 60mg), DIPEA (0.9mmol, 160μl), DMAP (0.06mmol, 7.2mg) in 15mL 1,4-dioxane, fill with nitrogen protection, room temperature Under reaction 24h. Remove the solvent by rotary evaporation, dissolve with 10ml of cold dichloromethane solvent, add dropwise to 250ml of glacial ether, precipitate out, filter under reduced pressure, take the precipitate and dry it to constant weight in a vacuum drying oven to obtain TPGS-COOH, collect 25 mg of the product was obtained, and the final yield was 5.1%. The synthesis of embodiment 3TPGS-COOH

Embodiment 3

[0074] Dissolve TPGS (0.3mmol, 459mg), SA (0.6mmol, 60mg), DIPEA (0.9mmol, 160μl), DMAP (0.06mmol, 7.2mg) in 15mL 1,4-dioxane, fill with nitrogen protection, room temperature Under reaction 24h. Remove the solvent by rotary evaporation, dissolve with 10ml of cold dichloromethane (0°C), add citric acid aqueous solution (PH=5-6), extract three times, then wash three times with distilled water, collect the organic phase, remove the organic solvent by rotary evaporation, Dry in a vacuum oven to constant weight to obtain TPGS-COOH, and obtain 453 mg of the product, with a final yield of 92.63%.

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Abstract

The invention provides a dendritic polymer-vitamin E succinate polyethylene glycol 1000 (PAMAM-TPGS), a preparation method thereof and an application of the dendritic polymer-vitamin E succinate polyethylene glycol 1000 (PAMAM-TPGS) as a drug carrier in preparation of a drug preparation. The dendritic polymer-vitamin E succinate polyethylene glycol 1000 nanoparticles prepared by a micro-channel method, a film dispersion method and an emulsion solvent evaporation method respectively have the characteristics of easiness in industrialization, high drug loading capacity and stable system, can obviously improve the solubility of a model drug in water and realize controllable release, have obvious pharmacological activity, and can be used for preparing a drug carrier for the drug. The device is suitable for various administration modes such as intravenous injection.

Description

(1) Technical field [0001] The invention relates to the technical field of pharmaceutical polymer carrier preparation and pharmaceutical preparations, in particular to a precursor material based on dendritic polymer-vitamin E succinate polyethylene glycol 1000 (PAMAM-TPGS) and its preparation method and its use as a pharmaceutical carrier Application in the preparation of pharmaceutical preparations. (2) Background technology [0002] Cancer is an urgent problem to be solved in the field of international medicine today. Chemotherapy is one of the three mainstream methods of cancer treatment. However, most clinical anticancer drugs are lipophilic compounds, which have poor water solubility, easy metabolism in the body, and low specific selectivity to cancer cells. Long-term, multiple or large doses are required. administered for therapeutic purposes. It often shows serious side effects, allergic reactions and drug resistance of tumor cells, which seriously affects the effec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00A61K31/12A61K47/60A61K47/69A61P35/00
CPCC08G81/00A61K47/60A61K47/6935A61K31/12A61P35/00
Inventor 郭钫元焦云龙杨根生
Owner ZHEJIANG UNIV OF TECH
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