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A double prodrug co-assembled nano-targeted drug delivery system and its preparation method

A technology of targeted drug delivery and co-assembly, applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve problems such as large differences in physical and chemical properties, incompatibility, etc., to achieve efficient co-loading and improve synergistic anti-tumor efficacy.

Active Publication Date: 2022-02-15
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, CDDP is a lipid-water-insoluble drug, and MET is a water-soluble drug. The physical and chemical properties of the two drugs are quite different. The co-loading method of using a polymer prodrug to self-assemble and encapsulating another drug small molecule is not suitable for CDDP and MET. Coloading of MET
Therefore, the co-encapsulation and in vivo co-delivery of CDDP and MET bring challenges to its nano-combination chemotherapy.

Method used

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  • A double prodrug co-assembled nano-targeted drug delivery system and its preparation method
  • A double prodrug co-assembled nano-targeted drug delivery system and its preparation method
  • A double prodrug co-assembled nano-targeted drug delivery system and its preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0042] 1. Synthesis of hyaluronic acid-cisplatin (HA-CDDP) polymer prodrug

[0043] Dissolve 30mg of cisplatin and 33mg of silver nitrate in 5mL of distilled water, protect from light, stir magnetically in a water bath at 50°C for 3h, then react magnetically for 24h at room temperature, centrifuge the resulting reaction solution at 1000rpm for 5min, filter to remove silver chloride, and obtain cisplatin intermediate body;

[0044] Dissolve 200mg of hyaluronic acid in 4mL of distilled water and add it to the cisplatin intermediate solution obtained above, avoid light, and react with magnetic stirring at room temperature for 24 hours. CDDP polymer prodrugs. That 1 H NMR spectrum such as figure 1 shown.

[0045] 2. Synthesis of polystyrene-metformin (PMet) prodrug

[0046] Add 1.5 g of 4-styrene chloride, 10 mg of 4-cyano-4-[(dodecylsulfanylthiocarbonyl)sulfanyl]valeric acid and 1 mg of azobisisobutyronitrile into a dry reaction flask, Dissolve in 2mL of anhydrous tetrahydr...

Embodiment 2

[0052] 1. Synthesis of hyaluronic acid-cisplatin (HA-CDDP) polymer prodrug

[0053] Dissolve 40mg of cisplatin and 50mg of silver nitrate in 8mL of distilled water, protect from light, stir magnetically in a water bath at 70°C for 6h, then react magnetically for 20h at room temperature, centrifuge the resulting reaction solution at 1000rpm for 10min, filter to remove silver chloride, and obtain cisplatin intermediate body;

[0054] Dissolve 400mg of hyaluronic acid in 10mL of distilled water and add it to the cisplatin intermediate solution obtained above, keep away from light, and react with magnetic stirring at room temperature for 48h; CDDP polymer prodrugs. That 1 H NMR spectrum such as figure 1 shown.

[0055] 2. Synthesis of polystyrene-metformin (PMet) prodrug

[0056] Add 1g of 4-styrene chloride, 15mg of 4-cyano-4-[(dodecylsulfanylthiocarbonyl)sulfanyl]valeric acid and 2mg of azobisisobutyronitrile into a dry reaction flask, dissolve In 6mL of anhydrous tetrahyd...

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Abstract

The invention relates to a double-prodrug co-assembled nano-targeted drug delivery system for tumor combined chemotherapy and a preparation method thereof. The double-prodrug co-assembled nano-targeted drug delivery system is composed of hyaluronic acid with CD44 receptor targeting Acid-cisplatin (HA-CDDP) prodrug and polystyrene-metformin (PMet) prodrug with micellar self-assembly properties were co-assembled by electrostatic binding. The present invention breaks through the traditional co-delivery mode in which two drugs are physically co-encapsulated and a polymer prodrug is self-assembled to physically entrap another drug small molecule, and can achieve accurate and high-efficiency combination drugs at an optimal ratio Co-loading, tumor-targeted co-delivery and intracellular enzymatic hydrolysis synchronously release cisplatin and metformin, improving the synergistic anti-tumor efficacy of the combination of the two drugs.

Description

technical field [0001] The invention belongs to the field of polymer materials and new dosage forms of pharmaceutical preparations, and relates to a double-prodrug co-assembled nano-targeted drug delivery system for combined tumor chemotherapy and a preparation method thereof. Background technique [0002] The pathogenesis of lung cancer is very complex, and its mortality rate ranks first among malignant tumors. Cisplatin (Cisplatin, CDDP) is the first-line drug in the clinical treatment of cancer, its toxicity and drug resistance limit the use of effective therapeutic dose, which further limits the efficacy of the drug. Therefore, exploring drug combination strategies with multi-effect synergy is an effective means for CDDP clinical combined treatment of lung cancer. [0003] The hypoglycemic drug metformin (Metformin, MET) can activate the adenylate-activated protein kinase (AMPK) / inhibit the target of rapamycin (mTOR) signaling pathway, inhibit the proliferation and migr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/61A61K47/58A61K33/243A61P35/00A61K31/155
Inventor 刘艳华杨彤孙悦兰杨李莉李治芳朱溶月
Owner NINGXIA MEDICAL UNIV
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