Amino-modified mesoporous silica with dual drug-loading effects

Abstract

The invention relates to the technical field of nano materials and specifically relates to amino-modified silica with dual drug-loading effects. According to the technical scheme, firstly, mesoporous silica nanoparticles are prepared by a template method; secondly, surface amino modification is carried out onto the mesoporous silica nanoparticles by 3-aminopropyltriethoxy silane; thirdly, ursolic acid is chemically coupled to the spherical mesoporous silica nanoparticles by amido bonds; and fourthly, the coupled nanoparticles are dispersed in DMF (dimethyl formamide) solution; a proper amount of ursolic acid is added, mixed and stirred; and finally vacuum drying is carried out to obtain the amino-modified silica with dual drug-loading effects. The mesoporous nano material with dual drug-loading effects prepared by the mesoporous silica disclosed by the invention is high in loading rate, can achieve controlled release effect for the loading drug ursolic acid, so that drug effect lasts for a long period time, and therefore, bioavailability of the ursolic acid is greatly improved.

Description

technical field [0001] The invention relates to the fields of pharmacy and biological nanomaterials, in particular to a spherical mesoporous silica nanoparticle with controllable particle size that can improve the bioavailability of ursolic acid and has dual drug-loading effects of chemical coupling and physical embedding. ball. Background technique [0002] Ursolic acid (Ursolic acid, referred to as: UA) is a pentacyclic triterpenoid compound widely distributed in nature. Attention of domestic and foreign research scholars. Pharmacological studies have proved that UA has: 1) inhibition of malignant tumor cell proliferation; 2) induction of tumor cell differentiation and apoptosis; 3) resistance to various carcinogens and carcinogens; 4) anti-tumor angiogenesis; 5) It has various anti-cancer activities such as enhancing immune function. At the same time, UA has a good liver-protecting effect, so it can break through the bottleneck of conventional chemotherapy drugs that g...

AI Technical Summary

Problems solved by technology

Although UA is being paid more and more attention by researchers in the fields of pharmacy and medicine because of its "high efficiency and low toxicity" characteristics and diversified anticancer and tumor suppressor mechanisms, it is not widely used as an anticancer drug in clinical development at home and abroad. very limited

The main factor is that due to the extremely poor water solubility of UA, its bioavailability in vivo is low (less than 1%), which greatly reduces the effect of ursolic acid in practical applications

Patent CN 102652735A discloses a porous silica nanoparticle loaded with insoluble drugs. The carrier material only adopts the method of physical embedding for drug loading. However, it wraps the insoluble drugs in the organic micelles in the silica pores, and because the organic micelles also occupy a certain pore volume, the loading capacity of the insoluble drugs in the pores is low, and the surface No chemical modification is coupled to the drug, the above together lead to a small drug loading, and its pharmacodynamic effect is not particularly significant

Patent CN 103357024A discloses the preparation of a nano-DNA complex formed by electrostatic adsorption by mixing plasmids and aminated silica nanoparticles, but this patent also only loads drugs by surface electrostatic adsorption, and the drug loading capacity It is smaller than the two methods of chemical coupling and physical embedding, and the stability is poor, and the slow-release effect is not obvious

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