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Water-soluble hypocrellin PLGA nanoparticle and preparation method thereof

A technology of hypocrellin and PLGA, which is applied in the field of photosensitizers, can solve the problems of unstable drug decomposition or oxidation, long preparation process time, and high requirements for equipment, so as to help storage and transportation, reduce dark toxicity, and improve the quality of materials. simple effect

Inactive Publication Date: 2014-07-23
NANJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] At present, the preparation methods of PLGA nanoparticles mainly include emulsification solvent volatilization method, nanoprecipitation, solvent diffusion method, spray drying method, etc. (Journal of Controlled Release, 2001, 70:1-20). The requirements are high, the preparation process takes a long time, consumes a lot of manpower, has the disadvantages of large drug loss and serious agglomeration during the preparation, and may decompose or oxidize unstable drugs, bringing potential safety hazards

Method used

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  • Water-soluble hypocrellin PLGA nanoparticle and preparation method thereof
  • Water-soluble hypocrellin PLGA nanoparticle and preparation method thereof
  • Water-soluble hypocrellin PLGA nanoparticle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0048] Embodiment 1. The screening of hypocrellin embedding agent:

[0049] Weigh 10 mg of PVA, PLGA, and PEG and dissolve them in 50 mL of ultrapure water, and weigh an equal amount of chitosan and dissolve them in 0.1% acetic acid aqueous solution as the water phase; label them 1-1, 1-2, 1-3 and 1-4, 1mg of hypocretin was dissolved in 100mg of acetone as the organic phase; under high-speed stirring, slowly add the organic phase to the water phase; 100W ultrasonic dispersion in ice bath for 5min; -80℃ pre-freezing; freeze-drying to obtain water-soluble hypocrellin nanoparticles.

[0050] Table 1. Screening of Hypocretin Embedding Agents

[0051] label

[0052] Drug loading(%)

[0053] The results are shown in Table 1, which shows that the encapsulation efficiency and drug loading capacity of PLGA (label 1-2) are significantly higher than other materials, so PLGA is selected as the preferred material of hypocrellin embedding agent.

Embodiment 2

[0054] Embodiment 2. Selection of lyophilized excipients:

[0055] Weigh 0.5 mg of glucose, lactose, trehalose, mannitol, and sucrose and dissolve them in 50 mL of ultrapure water as the water phase, numbered 2-1, 2-2, 2-3, 2-4, and 2-5; Take 8 mg of PLGA (the ratio of lactic acid: glycolic acid is 75:25), 1 mg of hypocrellin A is dissolved in 100 mg of glycerin in a certain proportion, as the organic phase, and slowly add the organic phase to the water phase under high-speed stirring. Phase; 100W ultrasonic dispersion in ice bath for 5min; pre-freezing at -80°C; freeze-drying to obtain water-soluble hypocretin PLGA nanoparticles; photos of reconstitution effect are as follows figure 1 , the results show that the reconstitution of nanoparticles using mannitol and trehalose as excipients in water yields a uniform and transparent colloidal solution, which is significantly better than the other three materials. Mannitol and trehalose are selected as the preferred bamboo red fungu...

Embodiment 3

[0056] The selection of embodiment 3. oil phase solvent:

[0057] Weigh 0.5 mg of mannitol and dissolve it in 50 mL of ultrapure water as the water phase; weigh 8 mg of PLGA (the ratio of lactic acid: glycolic acid is 75:25), and 1 mg of hypocrellin A are dissolved in a certain proportion 100 mg of acetone, oleic acid, linoleic acid, ethanol, dichloromethane, chloroform and glycerol, numbers 3-1, 3-2, 3-3, 3-4, 3-5, 3-6 and 3-7, As the organic phase, slowly add the organic phase to the water phase under high-speed stirring; 100W ultrasonic dispersion in ice bath for 5min; Surface morphology of nanoparticles: electron microscope observation results are as follows figure 2It shows that the nanoparticles in No. 3-1, 3-2, 3-3 and 3-7 samples have the most uniform particle size distribution, no agglomeration, regular shape and round shape, so acetone, oleic acid, linoleic acid and glycerin It is the preferred solvent for hypocrellin embedding agent.

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Abstract

The invention relates to the technical field of medicines, and particularly relates to a water-soluble hypocrellin PLGAnanoparticle and a preparation method thereof. The preparation method comprises the following steps: by taking poly(lactic-co-glycolic acid) (PLGA) as a carrier, dissolving PLGA and hypocrellin into an organic solvent to prepare an oil phase, adding into freeze-drying excipient-containing water phase under high-speed stirring, and finally obtaining the hypocrellin nanoparticle by adopting an emulsification freeze-drying method. By using a biodegradable medical polymer material PLGA used in the preparation method and approved by the food and drug administration (FDA) of the United States, the toxic and side effects of a common drug-carrying material can be reduced, the water solubility of the drug can be improved, the particle size of the prepared nanoparticle ranges from 20-200nm, the drug has red shift, the absorption of the nanoparticle in a phototherapy window (600-900nm) can be increased, and the dark toxicity of the drug can be reduced. The preparation method is simple in raw materials and easy to operate.

Description

technical field [0001] The invention belongs to the technical field of photosensitizers with photodynamic activity, and relates to a water-soluble hypocretin PLGA nanoparticle and a preparation method thereof. Background technique [0002] Photodynamic therapy (PDT) is a new clinical treatment technology under research and development. Since Dousherty et al first applied PDT to clinical tumor treatment in the 1970s and achieved success. Up to now, PDT is not only one of the effective means of cancer treatment, but also widely used in the treatment of senile fundus plaque degeneration, port wine stains, Peripheral arterial disease and coronary artery disease, in addition, antiviral, photodynamic pesticides have also been successfully applied. Since its inception, many patients in the world have benefited from photodynamic therapy. [0003] Due to its better selectivity, photodynamic therapy has attracted much attention in cancer treatment, and has achieved remarkable achiev...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K47/34A61K9/19A61P35/00
Inventor 陈双林祁姗姗闫淑珍
Owner NANJING NORMAL UNIVERSITY