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SP peptide-modified platinum drug loaded on dendritic molecules and preparation method and applications thereof

A platinum-based drug and dendritic technology, which is applied in the field of dendrimer-loaded platinum-based drugs and its preparation, can solve the problems of preparation leakage, neurotoxicity, and difficulty in accumulation, and achieve the advantages of ensuring stability, enhancing curative effect and reducing side effects. Effect

Inactive Publication Date: 2019-05-07
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The National Comprehensive Cancer Network of the United States recommends that platinum drugs be used as one of the adjuvant chemotherapy regimens in clinical practice. However, platinum drugs cannot cross the blood-brain barrier, and because platinum drugs pass through the cell membrane through free diffusion, it is difficult Accumulation occurs at the tumor site, so the direct use of platinum-based drugs in the chemotherapy of glioma is prone to severe neurotoxicity
[0004] In response to the above problems, some scholars have tried to load platinum-based drugs on the carrier through physical action in order to achieve the purpose of delivery, but the product is unstable and easy to cause leakage of the preparation in the blood circulation; some scholars have used the method of oxidation of platinum-based drugs to achieve the purpose of delivery. The drug is made into a prodrug, but there is still a risk of the prodrug being metabolized before being reduced to the original drug in the body

Method used

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  • SP peptide-modified platinum drug loaded on dendritic molecules and preparation method and applications thereof
  • SP peptide-modified platinum drug loaded on dendritic molecules and preparation method and applications thereof
  • SP peptide-modified platinum drug loaded on dendritic molecules and preparation method and applications thereof

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Embodiment 1

[0048] Such as figure 1 In the synthesis step shown in A, add (1,2-diaminocyclohexane)platinum dichloride and silver nitrate at a molar ratio of 1:1 in deionized water, and stir for 24 hours at 25 degrees in the dark , The silver chloride was removed by centrifugation and filtration to obtain (1,2-diaminocyclohexane)-chloronitroplatinum aqueous solution, and then 0.2 molar amount of S-2-(4-benzyl isothiocyanate)- Diethylenetriaminepentaacetic acid was stirred at 25 degrees for 24 hours to obtain the chelated product of DTPA and platinum drugs. Difunctionalized NHS-PEG3500-N with a molar ratio of 1:10 3 Dissolve poly-L-lysine dendrimers in phosphate buffer at pH 8.0, stir for 24 hours at 25 degrees, then remove unreacted raw materials by ultrafiltration and change the buffer to phosphate buffer at pH 7.0 liquid. In 4-hydroxyethylpiperazine ethanesulfonic acid buffer with a pH of 8.2, add a 1:20 molar ratio of poly-L-lysine-polyethylene glycol conjugate and DTPA chelate with pla...

Embodiment 2

[0050] Dissolve 5 mg of platinum drug-loaded dendrimer nanoparticles in 2 ml of deionized water, vortex for 5 minutes, use dynamic light scattering to measure the particle size and Z potential in the solution. The measured particle size and potential are 19.65± 4.65nm and 3.5±0.9mV

Embodiment 3

[0052] Dissolve 5 mg of platinum drug-loaded dendrimer nanoparticles in 2 ml of deionized water, vortex for 5 minutes to make them evenly distributed, and drop them on a carbon-coated copper mesh. After drying under infrared light, observe with a transmission electron microscope Nanoparticles ( figure 1 E). The nanoparticles are regular in shape and have good dispersion, indicating that no larger particle size aggregates are formed between the nanoparticles. The particle size measurement result of the transmission electron microscope is close to the result of dynamic light scattering.

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Abstract

The invention belongs to the technical field of biology, and relates to an SP peptide-modified platinum drug loaded on dendritic molecules and a preparation method and applications thereof. Accordingto the invention, a common metal chelating agent DTPA is utilized to a load platinum drug on dendritic macromolecule poly L-lysine to form nanoparticles, meanwhile, SP peptide modifies the drug to serve as a targeting functional group, and the nanoparticles can be mediated to cross a blood-brain barrier and targeting brain glioma tissues, so that the platinum drug is subjected to effective targeted delivery. The SP peptide-modified platinum drug loaded on dendritic molecules can be used for preparing a novel preparation for treating brain glioma, and can enhance the curative effect and reduceside effects.

Description

Technical field [0001] The present invention belongs to the field of biotechnology, and relates to a SP peptide modified dendrimer loaded with platinum drugs, and a preparation method and application thereof. Background technique [0002] The prior art discloses that glioma is the most common tumor of the central nervous system, accounting for about 40%. Glioma has the characteristics of multiple, sporadic, infiltrating, etc., and the five-year survival rate is less than 5%. The conventional treatment of glioma is surgical resection supplemented by radiotherapy and chemotherapy. Due to its own invasive growth characteristics, surgery is difficult to complete, making chemotherapy an indispensable treatment. However, due to the existence of the blood-brain barrier, it is difficult for most chemotherapy drugs to enter the brain and accumulate in the tumor. [0003] At present, platinum drugs are the most frequently used anti-tumor drugs in clinical practice. Platinum drugs have th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/62A61K47/60A61K9/14A61K31/282A61P35/00
Inventor 孙涛蒋晨陈钦俊
Owner FUDAN UNIV