Preparation method of hypocrellin-transferrin targeted drug delivery system and application of hypocrellin-transferrin targeted drug delivery system in photodynamic therapy

A technology of Bamboo Rhododendron A and transferrin, applied in the field of photosensitizers, can solve the problems of affecting the conformation and activity of transferrin, affecting the drug release process, disintegration of the drug delivery system, etc., and achieves good dispersibility and water solubility. The effect of high, stable dispersion properties

Inactive Publication Date: 2016-06-01
NANJING NORMAL UNIVERSITY
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Problems solved by technology

[0007] The construction of the traditional transferrin-drug delivery system (Tf-Drug) is mainly through two ways, one is to form a Schiff base between the drug and the protein through a coupling reaction to form a stable drug delivery system, but This chemical reaction process will affect the conformation and activity of transferrin to a certain extent; moreover, the stable chemical bond may affect the release process of the drug in the later stage
Another method is to connect the prote

Method used

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  • Preparation method of hypocrellin-transferrin targeted drug delivery system and application of hypocrellin-transferrin targeted drug delivery system in photodynamic therapy
  • Preparation method of hypocrellin-transferrin targeted drug delivery system and application of hypocrellin-transferrin targeted drug delivery system in photodynamic therapy
  • Preparation method of hypocrellin-transferrin targeted drug delivery system and application of hypocrellin-transferrin targeted drug delivery system in photodynamic therapy

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[0026] Example 1

[0027] A preparation method of a rhododendron A targeted drug delivery system, using all-iron transferrin to prepare a rhododendron A-transferrin chelate, the method is as follows:

[0028] In a physiological buffer solution, use urea and β-mercaptoethanol to inactivate all-ferritransferrin to make its three-dimensional structure loose and expose the Fe ion coordination site, then add excess rhododendron A (according to HA and Tf according to 2 : 1 ratio), shake at a constant temperature for 24h at 4°C, remove unbound HA, urea, and β-mercaptoethanol by dialysis to reduce the three-dimensional structure of whole iron transferrin, and obtain Bamboo Rhododendron A-transferrin targeted drug delivery system, the samples were freeze-dried to obtain freeze-dried powder, which was dissolved in purified water before use.

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Abstract

The invention discloses a preparation method of a hypocrellin-transferrin targeted drug delivery system and an application of the hypocrellin-transferrin targeted drug delivery system in photodynamic therapy. The method comprises the following steps: with holo-transferrin as a carrier, inactivating the holo-transferrin by urea and beta-mercaptoethanol, and making a three-dimensional structure loose to expose Fe-ion coordination sites; adding excessive hypocrellin, coordinating with Fe coordination sites, eliminating uncombined HA and urea through dialysis, and restoring the three-dimensional structure of holo-transferrin with beta-mercaptoethanol, thereby obtaining the hypocrellin-transferrin targeted drug delivery system. The method is simple in preparation and good in application prospect; the hypocrellin-transferrin targeted drug delivery system can be prepared into freeze-dried powder for storage, and the freeze-dried powder is prepared into a preparation suitable for intravenous injection after being dissolved. Due to the tumor targeting action of holo-transferrin in the system, the photosensitive anti-tumor activity of hypocrellin can be significantly strengthened by the targeted drug delivery system.

Description

technical field [0001] The invention belongs to the technical field of photosensitizers with photodynamic activity, and relates to a method for chelating and coupling a photosensitizer of hypocrellin A with a targeting molecule through a metal bond, and the hypocrellin A- Application of transferrin-targeted drug delivery system in photodynamic therapy. Background technique [0002] Photodynamic therapy (PDT) is a new type of clinical tumor therapy developed in recent years. It has attracted widespread attention due to its unique advantages such as broad anti-tumor spectrum, no serious side effects, minimally invasive and economical convenience. Especially for those patients with advanced cancer and who are not suitable for traditional treatment techniques due to age, physical fitness and other reasons, photodynamic therapy is still an ideal treatment method. Photodynamic therapy mainly uses a light source of appropriate wavelength to excite photosensitizers to generate reac...

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Application Information

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IPC IPC(8): A61K41/00A61K31/122A61K47/48A61P35/00
CPCA61K41/0057A61K31/122
Inventor 周林周家宏魏少华陈鑫武琦宋子怡
Owner NANJING NORMAL UNIVERSITY
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