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pH redox dual sensitive PAMAM (Polyamidoamine) targeted nano drug delivery carrier and preparation method thereof

A nano drug delivery carrier and sensitive technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of reducing drug release and reducing the anti-tumor effect of drugs, and achieve reduction Effects of uptake, reduction of cytotoxicity and hemolytic toxicity, and prolongation of residence time

Inactive Publication Date: 2017-02-15
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the PEG-modified carrier may reduce the release of the drug to a certain extent, and have a certain impact on the acid sensitivity and proton sponge effect of PAMAM itself, which will reduce the anti-tumor effect of the drug

Method used

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  • pH redox dual sensitive PAMAM (Polyamidoamine) targeted nano drug delivery carrier and preparation method thereof
  • pH redox dual sensitive PAMAM (Polyamidoamine) targeted nano drug delivery carrier and preparation method thereof
  • pH redox dual sensitive PAMAM (Polyamidoamine) targeted nano drug delivery carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Accurately weigh Fmoc-His(trt)-OH, 1-hydroxy-benzo-triazole (HOBt), benzotriazole-N,N,N,N-tetramethyluronium hexafluorophosphate (HBTU ), N,N-diisopropylethylamine (DIPEA) and PAMAM were dissolved in anhydrous dimethylformamide (DMF) according to the reaction molar ratio of 64:64:64:64:1, under nitrogen protection, at room temperature and protected from light React for 12 hours; precipitate the reaction product with cold ether, wash, centrifuge, then redissolve in piperidine / DMF (v / v, 30 / 70) solution, and continue the reaction for 6 hours; precipitate the product again with cold ether, then dissolve in trifluoroacetic acid / Triisopropylsilane / H 2 In O solution, reacted for 12 hours; finally precipitated with cold ether, redissolved in DMF, dialyzed in deionized water for 24 hours, and freeze-dried to obtain the final product PAMAM-His.

[0034] The synthesized product PAMAM-His and SPDP were neutralized by adding methanol solution at a molar ratio of 1:32, adding triet...

Embodiment 1、2、3

[0055] Example 1, 2, 3, free DOX to the IC of MCF-7 and HEPG2 cells 50 The value is as follows

[0056]

[0057] From the above table, image 3 and Figure 4 It can be seen that each complex has a certain anti-tumor effect on MCF-7 and HEPG2 cells. The cytotoxicity of the different complexes to both cells showed a dependence increase with the increase of DOX concentration. At the same dosage, the Tf-PSSPH / DOX drug-loaded complex exhibited the strongest cytotoxicity, indicating that Tf linking can significantly enhance the cytotoxicity of the complex. For MCF-7 cells, the IC50 of the Tf-PSSPH / DOX drug-loaded complex was 0.297 μg / mL, and its cytotoxicity was that of the PPH / DOX drug-loaded complex (1.873 μg / mL) and the PSSPH / DOX drug-loaded complex (1.114μg / mL) 6.31 and 3.75 times; for HepG2 cells, the IC50 of Tf-PSSPH / DOX drug-loaded complex is 0.243μg / mL, and its cytotoxicity is respectively that of PSSPH / DOX drug-loaded complex (0.743μg / mL) and 3.06 and 1.85 times of...

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Abstract

The invention discloses a pH redox dual sensitive PAMAM (Polyamidoamine) targeted nano drug delivery carrier. A general formula is T-PEG[n]-SS-PAMAM-(His)[m], wherein T is a tumor targeting ligand, the PAMAM is a cationic polyamidoamine-dendritic macromolecule, PEG is polyethylene glycol, -SS- is a bridge bond disulfide bond, His is histidine, n is 20 to 1000, and m is 1 to 4096. The invention also provides a preparation method of the pH redox dual sensitive PAMAM targeted nano drug delivery carrier. By modification of the His, the acid sensitivity of the carrier can be improved, a proton sponge effect of the PAMAM is enhanced, and a drug is enabled to quickly escape from acidic lysosome.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and more specifically relates to a PAMAM targeted nanometer drug delivery carrier sensitive to pH redox and a preparation method thereof. Background technique [0002] Malignant tumors have become frequently-occurring and common diseases that seriously threaten human health. In China, 2.2 million people die of cancer every year. The International Agency for Research on Cancer predicts that by 2030, the number of cancer patients in China will reach 5 million per year, accounting for more than 20% of the global increase. Therefore, it is of great significance to the prevention and treatment of cancer. At present, there are various methods for the treatment of cancer, including surgery, chemotherapy, radiotherapy, immunotherapy, gene therapy, and traditional Chinese medicine therapy. Among them, chemotherapy is one of the main means of treating tumors, but due to the lack of selectivity of che...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/34A61K31/704A61P35/00C08G83/00
CPCA61K9/5146A61K31/704A61K47/34C08G83/004
Inventor 程丽芳陈大为宿露
Owner SUZHOU UNIV
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