Calcium-affinity nanoparticle with Pamidronate disodium-modified Brij78 as key component and preparation method thereof

A technology of disodium pamidronate and nanoparticles, which is applied in the field of medicine, can solve the problems of loss, lack of universality, and reduced drug activity, and achieves low environmental pollution, good high temperature stability and chemical stability, and simple steps. Effect

Inactive Publication Date: 2014-09-10
SOUTHWEST JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These modification methods are specific to nanoparticles and their surface properties, and are not universal
At the same time, the modification of nanoparticles is usually after the active drug is loaded, and the chemical reaction of the modification is likely to reduce or lose the activity of the drug.

Method used

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  • Calcium-affinity nanoparticle with Pamidronate disodium-modified Brij78 as key component and preparation method thereof
  • Calcium-affinity nanoparticle with Pamidronate disodium-modified Brij78 as key component and preparation method thereof
  • Calcium-affinity nanoparticle with Pamidronate disodium-modified Brij78 as key component and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the preparation of the Brij78 that p-toluenesulfonyl chloride modifies

[0032] Weighed Brij78 (11.5g, 10mmol) and dissolved it in dichloromethane, added triethylamine (3.03g, 30mmol), added p-toluenesulfonyl chloride (3.8g, 20mmol) in batches while stirring in an ice bath, Continue to stir overnight to make the reaction complete, remove dichloromethane by distillation under reduced pressure, redissolve the solid in ethanol, add concentrated hydrochloric acid, place the solution in a refrigerator at -20°C, let it rest overnight, and centrifuge at -10°C at 5000g for 5min to obtain Crude Brij78 modified with p-toluenesulfonyl chloride (13.22 g). Using Brij700 instead of Brij78 as the starting material, the same preparation method can be used to obtain the crude product of Brij700 modified with p-toluenesulfonyl chloride.

Embodiment 2

[0033] Embodiment 2: the Brij78 of pamidronate disodium modification of the present invention

[0034] The Brij78 (13.22 g, 10 mmol) modified by p-toluenesulfonyl chloride obtained in Example 1 was dissolved in distilled water, sodium bicarbonate (4.2 g, 50 mmol) and disodium pamidronate (3.7 g, 10 mmol) were added, The solution was refluxed overnight to make the reaction complete, the solvent was distilled off under reduced pressure, the solid was redissolved in ethanol, filtered, the filtrate was evaporated to dryness, the solid was redissolved in petroleum ether, filtered, the solid was washed with the filtrate, and then washed three times with petroleum ether to obtain this product The Brij78 (9.3g) modified by disodium pamidronate described in the invention is named Brij78-Pa.

[0035] See attached figure 1 , which is the proton nuclear magnetic resonance spectrum of Brij78-Pa provided by the present embodiment, combined with figure 1 and compare as figure 2 From the ...

Embodiment 3

[0037] Embodiment 3: the preparation of emulsion nanoparticles of the present invention

[0038] Take the surfactant Brij78-Pa (3.5mg), TPGS (1.2mg), and My808 (2mg) of the present invention into a glass bottle, heat to 55°C, add deionized water (200ul, 55°C) at 55°C, Stir vigorously at 55°C for 2 minutes to form a slurry-like mixture, add deionized water (1.8ml, 55°C) at 55°C, stir the mixture vigorously at 55°C until an oil-in-water microemulsion is formed, stop heating, Cool and stir to room temperature to form nano-microemulsion, and do the particle size and zata potential test of the prepared micro-emulsion (see image 3 ). For specific data, such as average particle size, particle size distribution and surface potential, see Figure 11 .

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Abstract

The invention relates to a calcium-affinity nanoparticle with Pamidronate disodium-modified Brij78 as a key component and a preparation method thereof. The key component is a surfactant with a calcium affinity effect and is prepared by reacting a series of Brij compounds with p-methyl benzene sulfonic chloride to prepare an intermediate and then reacting the intermediate with bisphosphonate. According to the invention, good surface activity of the series of Brij compounds is retained, and calcium affinity capability of the series of Brij compounds is improved at the same time. The preparation method has the advantages of reliable principles, simple steps, easy operation, high security of used reactants and solvents and small pollution to the environment. The Pamidronate disodium-modified Brij78 has good high temperature stability and chemical stability; and a variety of drug-loaded nanoparticles prepared from the Pamidronate disodium-modified Brij78 have calcium affinity and bone targeting performances and can be used in the technical field of medicine.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a drug-loaded biorepair material, a bone-targeting nano-medicine preparation, especially a Brij series surfactant modified with an amino-containing bisphosphonate and a preparation method thereof. Background technique [0002] Amino group-containing bisphosphonates (such as pamidronate disodium) have the following structural formula: [0003] [0004] R 1 for -CH 3 Or -OH; R is hydrogen, a monovalent metal salt or an alkyl group containing 1-4 carbons; n is 0-10. [0005] The bisphosphonates utilized in the present invention are a class of drugs used to strengthen bones. Bone is in a constant state of bone remodeling, in which new bone is produced by cells called osteoblasts and old bone is removed by cells called osteoclasts. Bisphosphonates inhibit bone removal (resorption) by osteoclasts. Bisphosphonates are used to treat bone pain from osteoporosis and diseases such as...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K9/14A61K9/127C08G65/335
Inventor 晏为力张家彬宋鹤粱刘新荣姚鹏邓同铭梁欢王倩王康
Owner SOUTHWEST JIAOTONG UNIV
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