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A dual-sensitive targeting nanoparticle preparation loaded with chemotherapy drugs and its preparation method

A technology for targeting nanoparticles and chemotherapeutic drugs, which can be used in drug combinations, pharmaceutical formulations, and medical preparations with inactive ingredients, etc. It can solve the problems of weak particle penetration, strong particle penetration, and easy damage to tissues and organs. , to achieve the effect of cheap raw materials, good biocompatibility and biodegradability, and improved solubility

Inactive Publication Date: 2021-05-11
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the inventors of the present disclosure have studied and found that when the particle size of the nano-preparation is large, the particle penetration ability is weak and the blood half-life is long, making the therapeutic effect poor; and when the particle size of the nano-preparation is small, the particle penetration ability is strong, Easy to damage normal tissues and organs

Method used

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  • A dual-sensitive targeting nanoparticle preparation loaded with chemotherapy drugs and its preparation method
  • A dual-sensitive targeting nanoparticle preparation loaded with chemotherapy drugs and its preparation method
  • A dual-sensitive targeting nanoparticle preparation loaded with chemotherapy drugs and its preparation method

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Embodiment 1

[0074] The synthesis of embodiment 1 paclitaxel-dithiodipropionic acid conjugate (PTX-SS-COOH)

[0075] Synthetic route such as figure 1 shown. Weigh paclitaxel (PTX, 0.020g, 0.023mmol), dithiodipropionic anhydride (DTDPA, 0.044g, 0.023mmol) and DMAP (0.014g, 0.11mmol) respectively (the mol ratio of PTX, DTDPA and DMAP is 1: 1:5), placed in a 25mL round bottom flask, added 2mL of pyridine, and reacted at 35°C for 24h under the protection of nitrogen. The reaction solution was rotary evaporated at 80°C to remove most of the pyridine, and dilute hydrochloric acid was added to remove pyridine that had not been evaporated to dryness. The washing solution was extracted with dichloromethane. This was repeated three times, and unreacted DTDPA was removed with a 0.22 μm filter membrane. The dichloromethane was evaporated to dryness, and dried overnight in a vacuum oven. The H NMR spectrum of PTX-SS-COOH is as follows figure 2 As shown, the product has the characteristic absorptio...

Embodiment 2

[0076] The synthesis of embodiment 2 thiolated gelatin (Gel-SH)

[0077]Weigh p-mercaptobenzoic acid (0.008g, 0.05mmol) and EDC (0.010g, 0.05mmol) in a 25mL round bottom flask (the molar ratio of p-mercaptobenzoic acid to EDC is 1:1), add 400 μL absolute ethanol, Sonicate to dissolve. Add 800 μL of sodium hydroxide solution (0.1 M) and 800 μL of deionized water, sonicate to make the solution uniform, and activate at room temperature for 1 h under the protection of nitrogen. NHS (0.012 g, 0.10 mmol) was added to the reaction solution (the molar ratio of NHS to EDC was 2:1), and the activation was continued for 1 h at room temperature under nitrogen protection. Weigh 0.1g type A gelatin, add 10mL deionized water to swell and dissolve, slowly drop the above activation solution into the gelatin solution under ultrasonic conditions, and react under nitrogen protection at 40°C for 4h. The reaction solution was put into a dialysis bag (MWCO=8000-14000), dialyzed with DMSO for 24 ho...

Embodiment 3

[0079] Synthesis of embodiment 3 amphiphilic polymer (Gel-SS-PTX)

[0080] Weigh Gel-SH (0.008g), swell and dissolve with deionized water. Another weighed PTX-SS-COOH (0.008g) and EDC (0.003g) were placed in a 25mL round bottom flask, PTX-SS-COOH:EDC=1:2 (mol / mol), dissolved in acetonitrile, room temperature and Under the protection of nitrogen, react for 1h. Then NHS (0.004g) was added, activated at room temperature under nitrogen protection for 1h. The reaction solution was slowly dropped into the Gel-SH aqueous solution, and the ratio of water-acetonitrile was adjusted to make the reaction solution clear (the volume ratio of acetonitrile to water was 1:1), and the reaction was carried out under nitrogen protection at 40°C for 24h. The reaction solution was transferred to a dialysis bag (MWCO=8000-14000), and dialyzed in DMSO and water for 24 hours each.

[0081] For the NMR spectrum of Gel-SS-PTX see Figure 4 . product of 1 In the H-NMR spectrum, there are not only t...

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Abstract

The present disclosure provides a dual-sensitive targeting nanoparticle preparation loaded with chemotherapy drugs and a preparation method thereof. The nanoparticle preparation includes an amphiphilic polymer, the amphiphilic polymer includes gelatin, at least one molecule of a chemotherapy drug, each The molecules of the chemotherapeutic drug are chemically bonded to the gelatin through a first chemical group, and the main chain of the first chemical group contains a disulfide bond. Among them, the disulfide bond is redox sensitive and can be broken to release the drug when the concentration of glutathione around the tumor tissue is high. At the same time, gelatin, as the substrate of the MMP-2 enzyme, can be degraded into small particles by the overexpressed MMP-2 enzyme around the tumor tissue, increasing the penetration in the tumor tissue, thereby achieving dual-sensitive drug release.

Description

technical field [0001] The disclosure relates to the field of pharmaceutical preparations, in particular to a dual-sensitive targeting nanoparticle preparation loaded with chemotherapy drugs and a preparation method. Background technique [0002] The statements herein merely provide background information related to the present disclosure and may not necessarily constitute prior art. [0003] As a chronic disease with a high mortality rate, cancer poses a great threat to human health. Chemotherapy is the main means of treating cancer. Its high toxicity and strong side effects are one of the main obstacles in the treatment process. While limiting the dosage of drugs, it may cause toxic side effects on normal tissues and organs. Therefore, as a method to improve drug distribution and reduce toxicity in vivo, nano-targeting technology has received extensive attention and research in the past decade. Encapsulating chemotherapy drugs in nanoparticles can not only control the re...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K31/337A61K47/64A61P35/00
CPCA61K9/5169A61K31/337A61K47/6435A61P35/00
Inventor 李凌冰朱艺馨杨敏周可
Owner SHANDONG UNIV
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