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Novel methotrexate controlled-release targeted carbon nanohorn drug loading system

A technology of methotrexate and single-walled carbon nanohorns, which is applied in the field of medicine, can solve the problems of lack of cell selectivity, discounted clinical effect, and multiple action sites, so as to improve water solubility and biocompatibility, and enhance water solubility. Sexuality and high drug loading rate

Inactive Publication Date: 2015-12-09
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is precisely because of its many sites of action and the lack of cell selectivity that it produces some toxic side effects such as neurotoxicity, bone marrow suppression, mucosal reaction, etc., which greatly reduces the clinical effect.

Method used

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  • Novel methotrexate controlled-release targeted carbon nanohorn drug loading system
  • Novel methotrexate controlled-release targeted carbon nanohorn drug loading system
  • Novel methotrexate controlled-release targeted carbon nanohorn drug loading system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Complex MTXoxSWNHs synthesis

[0041] First, 1 mgoxSWNHs was dispersed in 1 mL DMSO, and placed in a bath sonicator for 6 h. Dissolve 5 mg MTX in 0.5 mL DMSO. The MTX solution and the oxSWNHs solution were mixed and ultrasonicated for 2 hours, and then stirred for 6 hours. The sample was centrifuged at high speed at 12000rpm for 15min, and the supernatant was removed. Add 2mL DMSO:H 2 O=1:1 solvent, high-speed centrifugation at 12000 rpm for 15 min, remove the supernatant, and repeat this operation twice. Add 2 mL of deionized water at 12000 rpm for 15 min, remove the supernatant, and precipitate MTXoxSWNHs. The loading capacity of methotrexate in the complex is 55% by thermogravimetric test.

Embodiment 2

[0043] Complex MTXoxSWNHs synthesis

[0044] First, 1 mgoxSWNHs was dispersed in 1 mL DMSO, and placed in a bath sonicator for 6 h. Dissolve 10 mg MTX in 0.5 mL DMSO. The MTX solution and the oxSWNHs solution were mixed and ultrasonicated for 2 hours, and stirred for 12 hours. The sample was centrifuged at high speed at 12000rpm for 15min, and the supernatant was removed. Add 2mL DMSO:H 2 O=1:1 solution, high-speed centrifugation at 12,000 rpm for 15 min, remove the supernatant, and repeat the operation twice. Add 2 mL of deionized water, 12000 rpm, 15 min, remove the supernatant, and precipitate MTXoxSWNHs. The loading capacity of methotrexate in the complex is 150% by thermogravimetric test.

Embodiment 3

[0046] Complex MTXoxSWNHs synthesis

[0047] First, 1 mgoxSWNHs was dispersed in 1 mL DMSO, and placed in a bath sonicator for 6 h. 15 mg MTX was dissolved in 0.5 mL DMSO. The MTX solution and oxSWNHs solution were mixed and ultrasonicated for 2h, and stirred for 18h. The sample was centrifuged at high speed at 12000rpm for 15min, and the supernatant was removed. Add 2 mL of DMSO:H to the bottom layer 2 The mixed solution of O=1:1 was centrifuged at 12000 rpm for 15 min at high speed, and the supernatant was removed. This operation was repeated twice. Add 2 mL of deionized water, 12000 rpm, 15 min, remove the supernatant, and precipitate MTXoxSWNHs. The loading capacity of methotrexate in the complex is 170% by thermogravimetric test.

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Abstract

The invention relates to a tumor targeted nano drug loading system with a controlled-release effect and a preparation method thereof, in particular to a method of adopting a nano precipitation method to enable single-wall carbon nanohorn to efficiently load first-class antitumor drug methotrexate (MTX). Polyethylene glycol is used as a solubilizer to modify the single-wall carbon nanohorn (MTX@oxSWNHs) loaded with the drug, so that water solubility and biocompatibility of MTX@oxSWNHs are improved obviously, and the drug loading system has a good controlled-release effect. Transferrin (Tf) is used as a targeting agent, so that the drug loading system has capability of targeted positioning and targeted releasing. Concentration of drug at a focus is increased, and toxic and side effect, on normal cells, of the drug is reduced greatly. The drug loading system has the advantages of being high in drug loading capacity and biocompatibility and capable of prolonging in-vivo circulating time of slightly-soluble antitumor drug, having targeting performance and being capable of improving the treatment effect of the drug.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a high-efficiency, slow-release, targeted and low-toxicity drug-carrying system constructed with novel nanomaterials as a carrier and a preparation method thereof. Background technique [0002] Tumor has replaced cardiovascular and cerebrovascular diseases as the number one killer threatening human health. There are certain defects in traditional treatment methods. For example, surgical treatment is generally only suitable for the early stage of cancer, and the trauma is relatively large and often accompanied by metastasis. Cells have relatively large side effects. At present, it is urgent to develop new targeted drugs with high efficiency and low toxicity for tumor treatment. Finding a more ideal drug-loading system, realizing more precise targeted therapy, improving drug stability in vivo, further reducing its adverse reactions and prolonging the action time are the direct...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K47/34A61K47/04A61K47/42A61P35/00
Inventor 钟文英王冉
Owner CHINA PHARM UNIV
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