Amino-modified mesoporous silica with dual drug-loading effects

A technology of mesoporous silica and dual drug loading, which is applied in the fields of pharmacy and bionanomaterials, can solve the problems of small drug loading, low bioavailability, and poor stability, and achieve low requirements for equipment and simple preparation process , Enhance the effect of immobilization

Inactive Publication Date: 2014-09-10
FUZHOU UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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 organi

Method used

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  • Amino-modified mesoporous silica with dual drug-loading effects
  • Amino-modified mesoporous silica with dual drug-loading effects
  • Amino-modified mesoporous silica with dual drug-loading effects

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Preparation of Mesoporous Silica

[0030] (1) Mix 0.50 mL (0.015 mol) of ethanol, 0.28 g (0.768 mmol) of cetyltrimethylammonium bromide (CTAB), 6.4 mL (0.36 mol) of ultrapure water, and add 0.19 mL of triethanolamine as an additive (0.0014 mol) to control the pH to 9.8, heat in a water bath at 60 °C, and stir at a certain speed.

[0031] (2) After the solution is mixed evenly and the temperature is constant, 0.73 mL (3.25 mmol) TEOS is added dropwise at a certain speed (1 mL / min). Stirring was continued for 2 hours to obtain a milky white suspension. Naturally cool at room temperature, centrifuge at 12000r / min for 15min to separate, wash with water and ethanol and centrifuge, then disperse in the mixed solution system of ethanol and hydrochloric acid (hydrochloric acid: ethanol volume ratio is 5:2), reflux three times, each time for 2 h . After reflux, wash with water and ethanol respectively, centrifuge and dry in vacuum to obtain mesoporous silica. Th...

Embodiment 2

[0032] Example 2 Preparation of Mesoporous Silica

[0033] Same as Example 1, the amount of additive triethanolamine added in step (1) was changed to 0.41 mL (0.0031 mol) to control the value of pH to 10.0, and other conditions remained unchanged to obtain mesoporous silica, the particle size test results are shown in Figure 4 .

Embodiment 3

[0034] Example 3 Preparation of Mesoporous Silica

[0035] Same as Example 1, change the amount of additive triethanolamine added in step (1) to 0.68 mL (0.0051 mol) to control the value of pH to 10.4, and other conditions remain unchanged, to prepare mesoporous silica, the particle size test results are shown in Figure 5 .

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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...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/04A61K31/56A61K9/16A61P35/00
Inventor 邵敬伟许煜禹小波林丽卿杨祥江舟贾力
Owner FUZHOU UNIV
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