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Preparation method of in-vivo self-assembled targeting drug carrier

A nano-drug carrier and self-assembly technology, which is applied in the direction of drug combinations, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of easy aggregation, slow drug release, difficult delivery and absorption, etc.

Inactive Publication Date: 2018-08-10
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These drug-loading systems have certain defects, such as the former drug release rate is too slow, and the latter is too fast
And it belongs to colloid or particle system in vitro, which is easy to agglomerate, has poor physical stability, and is not easy to be transported and absorbed

Method used

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  • Preparation method of in-vivo self-assembled targeting drug carrier
  • Preparation method of in-vivo self-assembled targeting drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0006] (1) Preparation of 6-O-carboxymethyl chitosan grafted with α, β, γ-cyclodextrin

[0007] Dissolve 2.00g of 6-O-carboxymethyl chitosan in 100mL of distilled water, add 0.20g of 6-amino-α-cyclodextrin, 0.20g of 6-amino-β-cyclodextrin, 0.20g of 6-amino - Gamma-cyclodextrin was added to 20mL of distilled water, stirred and dissolved at room temperature, cooled to 0°C, slowly added 5.00g of 30% EDC aqueous solution and 2.00g of NHS 10% aqueous solution, stirred and reacted at 0°C for 2h, and then reacted statically at room temperature for 72h, Then add 50 mL of absolute ethanol under stirring, a light yellow precipitate precipitates out, filter, wash with absolute ethanol and acetone three times, and dry in vacuum to obtain a white solid powder, which is set aside;

[0008] (2) Preparation of poly-L-histidine

[0009] Add 1.00g of L-histidine into 30mL of distilled water, stir to dissolve, cool down to 0°C, slowly add 3.00g of 30% EDC aqueous solution and 1.00g of 10% NHS a...

Embodiment 2

[0013] (1) Temperature sensitivity

[0014] Take the sample solution of Example 1 (3) and place it in an airtight container, change the temperature from 0-40° C., place it for different times, observe the change of the sample solution, and measure its turbidity. The maximum time is 30 days, and within the range of 0-40°C, the temperature change cannot cause the turbidity of the sample solution to change. The results are shown in Table 1.

[0015] Table 1 Turbidity of sample solution (NTU, pH=7.3)

[0016]

[0017] (2) pH value and dilution sensitivity

[0018] At different temperatures, the pH value of the sample solution was adjusted with 0.1% NaOH solution. When the pH value was 6.7, the turbidity of the sample solution began to increase significantly and gradually turned into a colloidal solution. See Table 2.

[0019] Table 2 Turbidity (NTU) of sample solution

[0020]

[0021] At 36.7°C, the sample solution was diluted with physiological saline (0.9% NaCl). As ...

Embodiment 3

[0025] (1) Particle size measurement

[0026] At 36.7°C, take 20 mL of the sample solution, dilute it 22 times with normal saline (0.9% NaCl), take the samples that have been left for different times, drop them on the copper grid with the support film, absorb the excess liquid with the filter paper, and then drip the heavy metal complexation Dye, filter paper to absorb excess liquid, dry naturally for 45min, measure particle size with scanning electron microscope. See Table 4.

[0027] Table 4 The average particle size of particles at rest for different times

[0028] standstill time, h

5

10

24

36

48

60

72

Average particle size, um

0.24

0.38

0.45

0.52

0.53

0.52

0.53

[0029] (2) Zeta potential measurement

[0030] At 36.7°C, take 20 mL of the sample solution, dilute it with physiological saline (0.9% NaCl) 5 times, 10 times, 15 times, 20 times, 22 times, 25 times and 30 times, stand still for 36 hours, and measu...

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Abstract

The invention relates to a precursor solution of active targeting nano-drug particles and a preparation method of the precursor solution. The precursor solution of active targeting nano-drug particlesis prepared from 6-O-carboxymethyl chitosan, 6-amino-alpha-cyclodextrin, 6-amino-belta-cyclodextrin, 6-amino-gamma-cyclodextrin, L-histidine and wheat germ agglutinin, has multiple drug-carrying factors, and can be assembled in organisms automatically. The preparation method includes, firstly, preparing three types of cyclodextrin grafted 6-O-carboxymethyl chitosan from raw materials of 6-amino-alpha-cyclodextrin, 6-amino-belta-cyclodextrin, 6-amino-gamma-cyclodextrin and 6-O-carboxymethyl chitosan; secondly, preparing poly L-histidine from the raw material of histidine and condensating agents, namely 1-ethyl-(3-dimethylaminopropyl) carbodiimide (EDC) and N-hydroxysuccinimide (NHS); thirdly, dissolving the three types of cyclodextrin grafted 6-O-carboxymethyl chitosan and the poly L-histidine in alkalescent water for injection, and then adding wheat germ agglutinin (WGA) to obtain the precursor solution which can be assembled into the nano particles carrying drug-carrying factors andtargeting factors in faintly acid normal saline.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a 6-O-carboxymethyl chitosan, 6-amino-α-cyclodextrin, 6-amino-β-cyclodextrin, 6-amino-γ- Cyclodextrin, L-histidine and wheat germ agglutinin are prepared as main raw materials, and have multiple drug-loading factors, which can be self-assembled in the body. The precursor solution of active targeting nano-medicine carrier particles and its preparation method. Background technique [0002] Targeted drugs can maximize the delivery of drugs to the target area, make the drug concentrated in the target area, directly act on diseased tissues, organs and cells, prolong the action time of the drug and the target site, and increase the amount of drug reaching the lesion, thereby Reduce the amount of medication, reduce the toxic and side effects of drugs, and achieve the therapeutic effect of high efficiency and low toxicity. There are two main types of active targeting drug deli...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K47/40A61K47/36A61K47/34A61K47/64A61K47/61A61P35/00C08G81/00C08G69/10
CPCA61K47/34A61K47/36A61K47/40A61K47/42A61K47/61A61K47/64A61P35/00C08G69/10C08G81/00
Inventor 麻金海张波涛孔淑玲
Owner QINGDAO UNIV
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