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

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...

AI Technical Summary

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 protein to the drug through the simple interaction force between the drug and the protein, such as electrostatic force, hydrophobic bond, hydrogen bond, etc. This method has a simple reaction system and has little effect on the protein conformation and activity, but because The strength of the above three forces is not high, so the drug delivery system obtained by this method often falls off from the protein during the drug delivery process, causing the drug delivery system to disintegrate.

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