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Salidroside segmented copolymer lipid nanoparticle preparation

A technology of salidroside block and lipid nanoparticles, applied in the field of medicine, can solve the problems of low encapsulation rate and the like, and achieve the effects of high drug loading, good sustained release effect and uniform particle size distribution

Inactive Publication Date: 2012-10-03
SOUTHWEST UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Although the use of PLGA or PLGA derivative nanoparticles to entrap drugs has been reported in the literature, it has been shown in practice that such nanoparticles have a low encapsulation efficiency for water-soluble drugs.

Method used

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  • Salidroside segmented copolymer lipid nanoparticle preparation
  • Salidroside segmented copolymer lipid nanoparticle preparation
  • Salidroside segmented copolymer lipid nanoparticle preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0062] Dissolve 20 mg of PLGA, 0.25 mg of soybean lecithin and 0.25 mg of cholesterol in 2 ml of dichloromethane, and ultrasonically dissolve. Add 200 μl of the inner aqueous phase containing 2.5 mg / ml salidroside, and sonicate the probe for 2 minutes. Add 8 ml of 1% PVA solution, and ultrasonically treat the probe for 5 minutes. The organic solvent was removed by rotary evaporation at 37° C. to obtain a colloidal solution of salidroside-PLGA lipid nanoparticles. The average particle size is 138nm, and the encapsulation efficiency is 81%. Transmission electron microscope photos are attached figure 1 .

Embodiment 2

[0064] Dissolve 50 mg of PEG-PLGA, 0.5 mg of DOPC and 0.25 mg of cholesterol in 2 ml of dichloromethane, and ultrasonically dissolve. Add 200 μl of the inner aqueous phase containing 2.5 mg / ml salidroside, and sonicate the probe for 2 minutes. Then add 16ml of 1% PVA solution, and ultrasonically treat the probe for 5 minutes. The organic solvent was removed by rotary evaporation at 37°C to obtain salidroside PEG-PLGA lipid nanoparticle colloidal solution. The average particle diameter is 115nm, and the encapsulation efficiency is 89%. Transmission electron microscope photos are attached figure 2 .

Embodiment 3

[0066] Dissolve 80mg of PLGA-PEG-PLGA, 5mg of lecithin and 1mg of cholesterol in 1ml of chloroform, and ultrasonically dissolve. Add 250 μl of the inner aqueous phase containing 25 mg / ml salidroside, and sonicate the probe for 2 minutes. Add 20 ml of 1% TPGS solution, and ultrasonically treat the probe for 5 minutes. The organic solvent was removed by rotary evaporation at 37° C. to obtain salidroside-PLGA-PEG-PLGA lipid nanoparticle colloidal solution. The average particle size is 148nm, and the encapsulation efficiency is 84%. Transmission electron microscope photos are attached image 3 .

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Abstract

The invention provides a salidroside segmented copolymer lipid nanoparticle preparation for intravenous injection and a preparation method of the nanoparticle preparation, as well as application of the preparation in preparing anti-cancer medicaments. The preparation comprises salidroside, segmented copolymer, lipid and surfactant.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a salidroside block copolymer lipid nanoparticle preparation and a preparation method and application thereof. Background technique [0002] At present, tumor treatment is one of the medical problems in the world. The treatment methods mainly include comprehensive measures such as surgery, chemotherapy, radiotherapy, immunity, biology, and traditional Chinese medicine. Due to the high mortality rate and low cure rate of cancer patients, cancer treatment has become one of the most important areas in current medical research. Although tumor biotherapy has been used in clinical trials for more than 10 years, there are still major problems such as large adverse reactions and insufficient clinical efficacy. Some tumor chemotherapy drugs not only have cardiovascular system toxicity, but also can cause adverse reactions such as phlebitis, nausea and vomiting, diarrhea, mucosal necrosis, hair lo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/7032A61K47/34A61P35/00
Inventor 何黎黎宋相容
Owner SOUTHWEST UNIVERSITY FOR NATIONALITIES
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