A small particle size dendrobetin nanomedicine targeting tumor cells with high expression of αvβ3 integrin receptor

Abstract

The invention discloses a nanometer drug of dendrobetin with a small particle size targeting αvβ3 integrin receptor highly expressed tumor cells and a preparation method thereof. The mass ratio of the raw material drug to the carrier is 1:10-1:100, and the carrier includes an amphiphilic polymer and a targeting compound, wherein the molar ratio of the amphiphilic polymer to the targeting compound is 1:100-1: 1. The carrier is a micelle carrier, the surface of which is modified with a high-affinity ligand of the αvβ3 integrin receptor overexpressed on the surface of tumor cells. The invention realizes that the drug can actively target specific tumor cells and can make the drug fast and effective Being taken up by cells, the drug can exert anti-tumor effect to a greater extent, and reduce the distribution of the drug in the whole body and the resulting toxic and side effects.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a small-sized dendrocetin nanomedicine targeting tumor cells with high expression of αvβ3 integrin receptors. Background technique [0002] Malignant tumors have always plagued human health. According to the latest statistics from the World Health Organization in 2018, there were about 18.08 million new cancer patients in the world in 2018. At present, there is no chemical or natural drug to cure cancer. The vast majority of chemotherapy Drugs are not selective, and these drugs can kill tumor cells as well as normal cells, so they will have serious side effects, such as paclitaxel can inhibit bone marrow, and doxorubicin can cause serious cardiotoxicity ,wait. Therefore, the development of anticancer drug preparations with less systemic toxicity and targeted effects is of great significance for tumor treatment. [0003] In the field of anti-tumor, some drug-...

AI Technical Summary

Problems solved by technology

[0005] Liposomes or nanoparticles that can target αvβ3 integrin receptors reported in the current literature have problems such as insufficient targeting function after the carrier is modified by targeting peptide due to their large particle size or heavy weight, that is, the so-called pony ( The small horse is the targeting peptide) and pulls the cart (the cart is the liposome or nanoparticle), specifically, after the targeted liposome or nanoparticle reaches the tumor site passively through the EPR effect, due to its relatively small mass or volume Due to the large size, the surface-modified targeting peptides cannot allow drugs to enter tumor cells through receptor-mediated endocytosis, thus to a large extent unable to realize the real targeting peptide-mediated drug entry behavior, resulting in Unsatisfactory anti-tumor effect

[0006] At present, the literature reports that most of the drugs targeting αvβ3 integrin receptors are drug liposomes or nanoparticles, and their preparation methods are generally thin film hydration method or anti-solvent method. The liposomes or nanoparticles prepared by these methods, due to the material Due to the nature and preparation method, the average particle size is generally 50nm-500nm, and these drug delivery carriers show insufficient penetration ability to the tumor after they passively reach the tumor site through the EPR effect

[0007] In addition, many of the carrier materials used in drug-loaded liposomes or nanoparticles that can target αvβ3 integrin receptors reported so far have not undergone effective safety evaluations, and generally speaking, they do not have the possibility of being marketed

Images