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Porphyrin-terminated nano-scale fluorescent polyrotaxane as well as preparation method and application thereof

A nano-scale, polyrotaxane technology, applied in preparations for in vivo experiments, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of poor biocompatibility of materials and lack of drugs. Tracing function, complex preparation process and other problems, to achieve the effect of simple and easy to operate preparation method, enhanced tumor treatment effect, and good biocompatibility

Inactive Publication Date: 2020-05-15
HENAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, most of the currently researched nano-drug carriers have defects such as complicated preparation process, high cost, poor biocompatibility of the materials used, and no trace function for drugs.

Method used

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  • Porphyrin-terminated nano-scale fluorescent polyrotaxane as well as preparation method and application thereof
  • Porphyrin-terminated nano-scale fluorescent polyrotaxane as well as preparation method and application thereof
  • Porphyrin-terminated nano-scale fluorescent polyrotaxane as well as preparation method and application thereof

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Embodiment 1

[0027] A method for preparing a porphyrin-terminated nanoscale fluorescent polyrotaxane, specifically:

[0028] Add pseudorotaxane (3.0471g, 0.1 mmol), porphyrin (629.24 mg, 1.0 mmol), PyBOP (520 mg, 1.0 mmol), DMAP (122.17 g, 0.1 mmol) into a 50 mL round bottom in turn, and then Add 20 mL of anhydrous DMF, and place it in a shaker at 4 °C to react overnight (12 h). After the reaction, add 20 mL of methanol, and a purple solid precipitates out. The purple solid was collected by centrifugation, and then washed successively with methanol, dichloromethane and distilled water. The obtained purple solid was ultrasonically dispersed in 10 mL of DMSO, and allowed to stand still to fully disassemble the residual pseudorotaxanes, and then 80 mL of deionized In water, a pale pink precipitate was obtained, which was collected by centrifugation, washed with methanol and water respectively, and freeze-dried to obtain a pale pink solid product porphyrin-capped nano-scale fluorescent polyrot...

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Abstract

The invention relates to a preparation method of porphyrin-terminated nano-scale fluorescent polyrotaxane. The preparation method comprises the following steps: mixing pseudorotaxane, porphyrin, PyBOP, DMAP and a solvent (anhydrous DMF), putting the mixture into a shaking table, reacting at 2-8 DEG C for 12-24 hours, adding methanol after the reaction is finished to separate out a solid, washing the solid, dispersing the solid into DMSO, adding deionized water, separating out a light pink precipitate, washing, and freeze-drying to obtain the product. The invention also provides an antitumor drug prepared by using the nano-scale fluorescent polyrotaxane as a drug carrier. Experiments show that the nano-scale fluorescent polyrotaxane can trace drugs, improve the enrichment of the drugs at tumor sites and reduce the toxic and side effects of the drugs on organisms, thereby improving the treatment effect of the drugs on tumors.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a porphyrin-terminated nanoscale fluorescent polyrotaxane, a preparation method and application thereof. Background technique [0002] The detection of tumors and the enrichment of drugs in tumor sites are the key to cancer treatment. Therefore, it is imperative to prepare fluorescent nano-drug loading system with tracer function. At present, the clinically used anti-tumor drugs have no targeting and cannot be traced, and there are serious side effects during the treatment of tumors. Nanomaterials have become a research hotspot due to their advantages of enhanced penetration and retention in tumors. However, most of the currently researched nano-drug carriers have defects such as complicated preparation process, high cost, poor biocompatibility of the materials used, and no drug-tracing function. [0003] Based on the above disadvantages, the present a...

Claims

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Application Information

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IPC IPC(8): C08B37/16A61K33/243A61K47/69A61K49/00A61P35/00
CPCA61K49/0036A61K47/6951A61P35/00A61K33/243C08B37/0015
Inventor 于树玲袁金涛石家华张艺
Owner HENAN UNIVERSITY
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