Preparation and application of glucan-protoporphyrin prodrug nano-micelle

A nano-micelle and protoporphyrin technology, which is applied in the field of preparation of dextran-protoporphyrin prodrug nano-micelle, can solve the problems of poor water solubility and instability of photosensitizers

Active Publication Date: 2021-09-14
SOUTHWEST UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem solved by the present invention provides a method for preparing a small molecule prodrug co-delivered by a

Method used

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  • Preparation and application of glucan-protoporphyrin prodrug nano-micelle
  • Preparation and application of glucan-protoporphyrin prodrug nano-micelle
  • Preparation and application of glucan-protoporphyrin prodrug nano-micelle

Examples

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Embodiment 1

[0031] Example 1 Preparation of a dextran-protoporphyrin prodrug

[0032] A kind of general synthetic schematic diagram of dextran-protoporphyrin prodrug is as figure 1 As shown, it mainly includes the following steps:

[0033] (1) The entire reaction process is carried out in an argon environment, and argon is used as a protective gas to prevent the presence of oxygen or hydrogen from affecting the reaction; at the same time, due to the presence of the photosensitizer protoporphyrin during the entire preparation process, it should be protected from light ; Protoporphyrin (PpIX) (57 mg, 0.1 mmol) was dissolved in 5 mL of anhydrous dichloromethane DCM to obtain a protoporphyrin solution, followed by addition of N-(3-dimethylaminopropyl)-N '-Ethylcarbodiimide hydrochloride EDC (75mg, 0.4mmol) and N-hydroxysuccinimide NHS (46mg, 0.4mmol) were stirred continuously to dissolve them. After dissolution, continue to stir in an ice bath for 30min, and then add hydrazine (1.2 mmol), r...

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Abstract

The invention discloses preparation and application of a glucan-protoporphyrin prodrug nano-micelle. The preparation method comprises the following steps of: (1) preparing aminated protoporphyrin (PpIX-NH2); (2) preparing aldehyde glucan (DEX-CHO); and (3) preparing DEX-CHO-PpIX-NH2 and DEX-PpIX micelles thereof. The prepared micelle has the advantages of stable particle size, uniform dispersion, high drug loading capacity, low toxic and side effects, high biological safety, high drug controlled release and the like, and the problem of poor water solubility of protoporphyrin is fundamentally solved. Due to modification of the protoporphyrin by the glucan, the toxic and side effects of a photosensitizer on normal cells are greatly reduced. Meanwhile, the small-molecule prodrug is controllably released in cancer cells, so that the protoporphyrin is effectively enriched at the tumor site, the cancer cells are killed through laser irradiation, accurate diagnosis and treatment are realized, and a novel strategy and systematic theoretical support are provided for development of a small-molecule phototherapy prodrug delivery system.

Description

technical field [0001] The invention relates to the fields of macromolecule chemical medicine and some biology, in particular to a preparation method and application of a dextran-protoporphyrin prodrug nano-micelle. Background technique [0002] Cancer is one of the major public health problems worldwide and has become a major killer threatening the health of our people. The World Health Organization's International Agency for Research on Cancer (IARC) recently released the latest global cancer burden data for 2020. According to statistics, in 2020, there will be about 19.29 million new cases of cancer and about 9.96 million deaths in the world. Among them, about 4.57 million new cancer cases will be reported in China, accounting for 23.7% of the world's total, and the number of deaths will be about 3 million, accounting for about 3 million of the global cancer deaths. about 30% of the population. Therefore, it is a general trend to find a new method and new strategy to im...

Claims

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Application Information

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IPC IPC(8): A61K47/61A61K41/00A61P35/00A61K49/00A61K49/22
CPCA61K47/61A61K41/0071A61P35/00A61K49/0054A61K49/0036A61K49/221A61K49/0002
Inventor 许志刚叶孟婕贾蝶康跃军
Owner SOUTHWEST UNIVERSITY
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