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Preparation method of pH-responsive core-shell structure dendrimer drug carrier

A dendrimer and amine dendrimer technology, which is applied in the field of preparation of core-shell structure dendrimer drug carriers, can solve problems such as improving release efficiency, and achieves reduction of toxic and side effects, simple reaction conditions, and high drug The effect of loading rate

Inactive Publication Date: 2019-11-26
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a preparation method of a pH-responsive core-shell structure dendrimer drug carrier, which overcomes the defect that the existing technology cannot be dissociated in the tumor microenvironment to improve the release efficiency. In the present invention, the Methods Using polyamide-amine (PAMAM) dendrimers as reaction units, a pH-responsive core-shell superstructure dendrimer was constructed by host-guest self-assembly. This method is easy to operate, and the preparation process is simple. It can react under liquid, has the advantages of high drug loading rate and pH response in cancer cells, and has a good application prospect in tumor chemotherapy

Method used

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  • Preparation method of pH-responsive core-shell structure dendrimer drug carrier
  • Preparation method of pH-responsive core-shell structure dendrimer drug carrier
  • Preparation method of pH-responsive core-shell structure dendrimer drug carrier

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Embodiment 1

[0043] Weigh 1.97 mg of benzimidazole-2-acetic acid (BM-COOH) and dissolve it in 5 mL of DMSO. Weigh 32.21mg EDC and 19.34mg NHS, dissolve them in 5mL DMSO respectively, first drop the EDC solution dissolved in DMSO into the BM-COOH solution and stir at room temperature for 30min, then add the NHS solution dissolved in DMSO dropwise into the reaction solution Stir continuously for 3h, BM-COOH can be activated. Weigh 50 mg of the third-generation polyamidoamine dendrimer (PAMAM G3) and dissolve it in 10 mL of DMSO. Then the above activated BM-COOH solution was added dropwise into the vigorously stirred G3 solution, and the reaction was continued under stirring for 3 days at room temperature. After the reaction was completed, the reaction solution was transferred to a dialysis bag with a molecular weight cut-off of 1000 Da, dialyzed in PBS buffer for 1 day, and then replaced with ultrapure water for dialysis for 2 days. Finally, the powder product G3.NH was obtained by freeze-...

Embodiment 2

[0048] The dendrimers prepared in Example 1 were characterized. G5.NH 2 -CD's 1 H NMR characterization results as figure 2 As shown in A, the proton peak at chemical shift 2.25-3.4ppm represents the methylene proton peak of G5, and the proton peak at chemical shift 3.5-4.1ppm and 5.1ppm represents the proton peak in the molecular structure of β-CD, indicating that β-CD has been successfully modified on the surface of G5. By integrating the proton peak areas of G5 and β-CD, it was calculated that 8.2 β-CD molecules were surface-modified per G5. G3.NH 2 -BM's 1 HNMR characterization results such as figure 2 Shown in C, the proton peak at the chemical shift 7-8ppm represents the proton peak in the molecular structure of the benzimidazole-2-acetic acid group, and the proton peak at the chemical shift 2.2-3.4ppm represents the methylene proton peak of G3, It shows that BM-COOH has been successfully modified on the surface of G3. By integrating the proton peaks in these tw...

Embodiment 3

[0051] The materials G5.NHAc-CD / BM-G3.NHAc and G5.NHAc-CD / Ad-G3.NHAc prepared in Example 1 and Comparative Example 1 were weighed and dissolved in ultrapure water, then doxorubicin hydrochloride ( DOX·HCl) was dissolved in methanol solution, and then triethylamine was added to the DOX hydrochloride solution to completely dissolve DOX·HCl, and then the dissolved DOX was added drop by drop to the vigorously stirred shell-core structure tree In the aqueous solution of macromolecules, keep the pH of the whole system at about 7.4. The reaction was carried out at room temperature and protected from light, the bottle was opened and kept stirring for 24 hours, centrifuged at 7500r for 10 minutes, the supernatant was collected, and freeze-dried to obtain a core-shell structure dendrimer wrapped with DOX. Calculate the percentage of DOX uploaded onto the core-shell structured dendrimer from the pellet collected by centrifugation, and the drug loading amount of G5.NHAc-CD / BM-G3.NHAc and ...

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Abstract

The invention relates to a preparation method of a pH-responsive core-shell structure dendrimer drug carrier. The fifth generation dentrimer modified by beta-cyclodextrin is taken as a core, the thirdgeneration dentrimer modified by benzimidazole-2-acetic acid is taken as a shell, and a pH-responsive core-shell super structure dendrimer is constructed by the self-assembly function of a supramolecule of host and guest molecules. When the prepared pH-responsive core-shell structure dendrimer is used as an anticancer drug carrier, the advantages of low toxicity, safety, high loading rate, intelligent release in tumor microenvironment and the like are achieved, and potential application prospects are achieved in aspects of chemotherapy and the like.

Description

technical field [0001] The invention belongs to the field of preparation of pH-responsive drug carriers, in particular to a method for preparing a pH-responsive core-shell structure dendrimer drug carrier. Background technique [0002] Since the 1970s, the morbidity and mortality of malignant tumors in my country have shown an obvious upward trend, which has caused great harm to human health. Among them, chemotherapy is the most widely used way to treat cancer. However, there are many defects in the clinical application of traditional chemotherapy drugs, such as poor water solubility, low bioavailability, and greater lethality to normal tissues. If a drug delivery system is constructed, it can significantly improve the performance of the drug in all aspects . In recent years, a new type of drug carrier polyamidoamine dendrimers (PAMAM) has been constructed as an excellent drug carrier for the treatment of tumors because of its unique physical and chemical properties. [00...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K47/38A61K47/59A61K47/61A61P35/00C08G81/00C08G73/02A61K31/704
CPCA61K31/704A61K47/34A61K47/38A61K47/59A61K47/61A61P35/00C08G73/028C08G81/00
Inventor 史向阳王建洪范钰史梦晗李杜
Owner DONGHUA UNIV
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