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Preparation method and application in preparation of photodynamic therapy medicines of fat-soluble photosensitizer loaded on inorganic salt carrier

A technology of inorganic salts and photosensitizers, applied in the field of photosensitizers, can solve the problems of poor water solubility and inconvenience to be made into pharmaceuticals, and achieve the effects of high water solubility, promotion of effective transmission, and easy operation.

Inactive Publication Date: 2010-10-06
NANJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to overcome the shortcomings of fat-soluble photosensitizers that are not convenient to make medicines due to their poor water solubility, and at the same time introduce inorganic salt nanoparticles into the application research of photosensitizers according to the principle of photosensitive drug sensitization in the clinical treatment process of photodynamic therapy , prepared a water-soluble inorganic salt carrier loaded with a fat-soluble photosensitizer with clinical application prospects, and applied this achievement in the field of photodynamic therapy, that is, this application will provide a water-soluble inorganic salt carrier of a fat-soluble photosensitizer and Preparation method of surface-modified inorganic salt carrier and its application in preparation of photodynamic therapy intravenous injection

Method used

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  • Preparation method and application in preparation of photodynamic therapy medicines of fat-soluble photosensitizer loaded on inorganic salt carrier
  • Preparation method and application in preparation of photodynamic therapy medicines of fat-soluble photosensitizer loaded on inorganic salt carrier
  • Preparation method and application in preparation of photodynamic therapy medicines of fat-soluble photosensitizer loaded on inorganic salt carrier

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Embodiment 1

[0046] Preparation of water-soluble hypocretin calcium phosphate nanoparticles under single system conditions, the reaction system and conditions are as follows:

[0047] In the experimental system, 20 mL of double distilled water, a certain amount of DMSO solution (15 mM), calcium chloride solution, and disodium hydrogen phosphate solution were added in sequence, and the magnetic stirrer was used for 20 hours. After the reaction was completed, small molecular substances in the system were dialyzed to remove Water-soluble hypocretin calcium phosphate nanoparticles.

Embodiment 2

[0049] Water-soluble hypocretin calcium phosphate nanoparticles were prepared by reverse microemulsion system. The reaction system and conditions were as follows:

[0050] Weigh 2.223g AOT and dissolve in 50ml cyclohexane, mix well and take 25ml, add 50μl calcium chloride solution, 400μl distilled water and a certain amount of HA in DMSO solution (15mM), stir for 72 hours to get liquid A.

[0051] Take another 25ml AOT / cyclohexane mixed solution, add 50μl disodium hydrogen phosphate solution, 350μl distilled water and a certain amount of HA in DMSO solution (15mM), and stir for 48 hours to obtain liquid B.

[0052] After liquid A and liquid B are clear and transparent, drop liquid B into solution A at a rate of 5ml per hour and stir continuously for 6 hours, then centrifuge at a speed of 16000rpm for 0.5h, wash the obtained particles with ethanol three times, and then add 10ml After dissolving in distilled water, it was sonicated for 2 hours, and after sonication, it was allow...

Embodiment 3

[0054] Composite AOT-modified calcium phosphate nanoparticles wrapped with hypocretin A were prepared in the normal phase microemulsion system. The reaction system and conditions were as follows:

[0055] After adding 20 mL of twice distilled water, 0.8 mL of n-butanol, a certain amount of HA in DMSO (15 mM), 0.44 g of AOT, and calcium chloride solution to the system, the magnetic stirrer was used for 2 hours until the liquid A became transparent.

[0056] After adding 20 mL of twice distilled water, 0.8 mL of n-butanol, a certain amount of HA in DMSO (15 mM), 0.44 g of AOT, and disodium hydrogen phosphate solution to the system, the magnetic stirrer was used for 2 hours to reach a transparent liquid B.

[0057] Drop liquid B into solution A at a rate of 5ml per hour and stir continuously for 36 hours, use a 12-14kD dialysis bag for 72 hours and centrifuge at a speed of 2000rpm for 10 minutes, and use ethanol for 3 times to obtain particles, and then add distilled water to diss...

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Abstract

The invention relates to a preparation method and application in the preparation of photodynamic therapy medicines of a fat-soluble photosensitizer loaded on inorganic salt carrier or modified surface inorganic salt carrier. The preparation method comprises the following steps: in or without the presence of surfactant, firstly adding distilled water, DMSO solution of fat-soluble photosensitizer, chloride solution and phosphate solution, performing magnetic stirring, and obtaining calcium phosphate nanoparticles with the grain size less than 100nm of fat-soluble photosensitizer after the reaction, wherein the molar ratio of chloride solution to phosphate solution is 1:10-10:1. The preparation method of the invention is simple, is easy to operate and has high stability and low cost; the diameter of the prepared nanoparticles is about 70nm, thus facilitating the preparation and storage of the product; the nanoparticles have high water-solubility and good dispersity, and can be used to promote the effective transmission of the fat-soluble photosensitizer in blood and eliminate the toxic or side effects of the fat-soluble photosensitizer which is used alone; and the nanoparticles have low toxicity in the dark and high phototoxicity.

Description

technical field [0001] The invention belongs to the technical field of photosensitizers with photodynamic activity, and relates to a method for preparing a novel fat-soluble photosensitizer loaded on an inorganic salt carrier or a surface-modified inorganic salt carrier, and the fat-soluble photosensitizer prepared by the method is used in the preparation Applications in photodynamic therapy medicine. Background technique [0002] Photodynamic therapy (Photodynamic Therapy, PDT for short) is also called photoradiation therapy (Photoradiation Therapy, PRT) or photochemotherapy (Photochemotherapy, PCT). PDT is a new type of medical technology based on photodynamic response. Since it entered clinical research in the 1970s, PDT has become an effective treatment method for malignant tumors, superficial microvascular diseases, skin diseases and eye diseases. At present, remarkable achievements have been made. PDT not only has a therapeutic effect on malignant tumors on the body s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K47/48A61K31/122A61K31/409A61P17/00A61P27/02A61P15/00A61P35/00A61P31/12A61K47/52
Inventor 周家宏周林冯玉英魏少华沈健
Owner NANJING NORMAL UNIVERSITY
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