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A kind of multilevel pH response mesoporous silica composite nanoparticle and its application

A technology of mesoporous silica and composite nanoparticles, applied in the field of nanomaterials, can solve the problems of inability to achieve therapeutic effect, low cell uptake rate, low therapeutic level of drug concentration, etc.

Active Publication Date: 2020-06-19
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, most drug carriers face the problem of low cell uptake rate, resulting in the drug concentration entering the cells being lower than the therapeutic level, and the expected therapeutic effect cannot be achieved.

Method used

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  • A kind of multilevel pH response mesoporous silica composite nanoparticle and its application
  • A kind of multilevel pH response mesoporous silica composite nanoparticle and its application
  • A kind of multilevel pH response mesoporous silica composite nanoparticle and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Example 1: Preparation of multi-stage pH-responsive mesoporous silica composite nanoparticles, the dosage ratio of each component is calculated according to the mass volume mole fraction, g / mL / mmol:

[0079] (1) Preparation of mesoporous silica containing surfactant: Weigh CTAB (0.2 parts by mass) and add 96 parts by volume of water, heat to 80°C, add sodium hydroxide solution (2M, 0.7 parts by volume), and stir for 30min , so that the templating agent forms micelles. Then TEOS (1.0 parts by volume) was added dropwise, and reacted at 80° C. for 2 h. After the reaction was completed, it was cooled to room temperature, centrifuged at 10,000 rpm, washed with water several times, and vacuum-dried at 30°C for 24 hours to obtain a white powder (MSN@CTAB).

[0080] The parts by weight of the reactants in the step (1) are as follows: 0.20 parts of CTAB; 0.06 parts of sodium hydroxide; 0.96 parts of TEOS; 98.78 parts of water;

[0081] (2) Preparation of surface aminated mesop...

Embodiment 2

[0122] Example 2: Preparation of loaded doxorubicin nanoparticles

[0123] MSN-PA (0.1 parts by mass) and doxorubicin hydrochloride (Dox) (0.02 parts by mass) were dispersed in 10 parts by volume of PBS (pH7.4) buffer solution, and stirred at room temperature for 24 hours in the dark. Add 2 drops of acetic acid dropwise, add catalyst system EDC (0.02 parts by mass) and NHS (0.01 parts by mass) and stir for 2 h. Polymer MOP-NHNH 2 (0.18 parts by mass, 0.03 parts by mole) were dissolved in 1 part by volume of THF solution. The polymer solution was slowly added dropwise into the mixed solution using a syringe, and stirred at room temperature for 24 h. After the reaction was completed, it was centrifuged at 5600 rpm, washed with PBS buffer solution (pH 7.4) until the supernatant was almost colorless, and freeze-dried to obtain drug-loaded particles (MSN-hyd-MOP@Dox). The drug loading is 12wt%, and the encapsulation efficiency is 87%.

Embodiment 3

[0124] Embodiment 3: release experiment

[0125] Determination of release performance: Accurately weigh 25 mg of doxorubicin nanoparticles and disperse them in 40 mL of pH 7.4 phosphate buffer solution, pH 6.5 phosphate buffer solution and pH 5.0 acetate buffer solution, and then place them in air at a temperature of 37.2 °C and a rotation speed of 150 rpm. in the shaker. Take a sample at a certain time interval, take out 4 parts by volume of the suspension each time, centrifuge, pour out the supernatant, transfer the precipitate to the original suspension, and add 4 parts by volume of fresh buffer. Measure the absorbance of the supernatant taken out at 480nm with an ultraviolet spectrophotometer, calculate the concentration of doxorubicin in the release liquid at different times, repeat each experiment three times, get the average value and draw the release curve, the results are shown in Figure 8 .

[0126] Depend on Figure 8 It can be seen that the drug-loaded particle...

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Abstract

The invention belongs to the technical field of nanometer materials, and discloses a multi-stage pH-responsive mesoporous silica composite nanometer particle and an application thereof. The mesoporoussilica is taken as the core of the composite nanometer particle, the acylhydrazone bond is used as a connecting bond, functionalized polymer is used as shell, the functionalize polymerd is prepared from a hydrophobic group-agglomerated polylactide, and the formula is shown in the description, wherein m=30 to 130 and n=23 to 68. The multi-stage pH-responsive mesoporous silica composite nanoparticles of the invention can be used as a carrier for controllable release and exhibit excellent pH-controlled release performance: using adriamycin as a guest molecule, the loading amount of the nanoparticles can reach 12 wt%, and the encapsulation efficiency can reach 87%; At pH 7.4 and pH 6.5, the cumulative releases were only 7% and 14% in 24h, but at pH 5.0, the cumulative releases increased to 43% in 24h.

Description

technical field [0001] The invention belongs to the technical field of nanometer materials, and in particular relates to a multilevel pH response mesoporous silicon dioxide composite nanoparticle and an application thereof. Background technique [0002] Mesoporous materials have great prospects in catalysts, industrial separations, fuel cells, and biomedicine. Mesoporous silica nanoparticles are currently the most widely used ordered mesoporous materials. The reason why mesoporous silica has attracted the attention of many researchers is mainly because of its simple synthesis method, adjustable shape, controllable particle size, uniform pore size and adjustable size, and the pores can provide space for loading guest molecules; secondly, The properties of the finished product are stable and uniform. Compared with the nano-carrier based on bio-organic materials, the physical and chemical properties are more stable, and it is not easily affected by external factors; moreover, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/04A61K31/704A61P35/00
CPCA61K9/5115A61K9/5146A61K31/704A61P35/00
Inventor 章莉娟袁晓哲彭诗元
Owner SOUTH CHINA UNIV OF TECH
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