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Target and fluorescence dual-functional slightly-soluble antitumor medicament nano structural lipid carrier

A technology of nanostructured lipids and antitumor drugs, which can be used in antitumor drugs, liposome delivery, drug combination, etc. System phagocytosis and other problems, to achieve the effect of prolonging the circulation time in the body, high chemical stability, and improving bioavailability

Inactive Publication Date: 2011-08-31
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with other lipid drug-loading systems, solid lipid nanoparticles have many advantages such as good biocompatibility, ability to regulate the release of drugs, and good physical and chemical stability, but there are still some defects: the method used in the preparation process Solid lipids will form a lattice structure with tightly arranged molecules, which limits the drug-loading capacity of solid lipid nanoparticles; during storage of solid lipid nanoparticles loaded with drugs, their solid lipids will also become more compact due to the formation of solid lipids. The crystal lattice "crowds out" the drug, thus causing the leakage of the drug
[0009] However, some of the currently prepared nanostructured lipid carriers have large particle sizes and are easily swallowed by the RES system. Some carriers have low targeting specificity for tumors and have high toxicity to normal tissues.

Method used

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  • Target and fluorescence dual-functional slightly-soluble antitumor medicament nano structural lipid carrier
  • Target and fluorescence dual-functional slightly-soluble antitumor medicament nano structural lipid carrier
  • Target and fluorescence dual-functional slightly-soluble antitumor medicament nano structural lipid carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Preparation of nanostructured lipid carrier targeting paclitaxel:

[0043] 10mg of stearic acid was dissolved in 30mL of N,N-dimethylformamide and stirred to dissolve. 10 mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and 5 mg of N-hydroxysuccinimide were added, followed by stirring for 1 hour. Then add 100 mg of glucosamine, stir for 4 hours, and dialyze to obtain target-modified stearic acid.

[0044] Take 34mg of target-modified stearic acid and 34mg of glyceryl monostearate and melt them in a water bath at 70°C, add 12mg of oleic acid, stir and mix well, then add 5mg of paclitaxel, stir for 30min, add 30mL of 1.5% Tween 20 Ionized water, high-speed stirring, ultrasonication, and centrifugation in an ice bath were used to obtain the nanostructured lipid carrier targeting paclitaxel.

[0045] Lipid carrier particle size distribution see figure 1 , the surface potential see figure 2 .

Embodiment 2

[0047] Preparation of targeted camptothecin nanostructured lipid carrier:

[0048] 10mg of stearic acid was dissolved in 30mL of N,N-dimethylformamide and stirred to dissolve. 10 mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and 5 mg of N-hydroxysuccinimide were added, followed by stirring for 1 hour. Then add 100 mg of glucosamine, stir for 4 hours, and dialyze to obtain target-modified stearic acid.

[0049] Take 34mg of target-modified stearic acid and 34mg of glyceryl monostearate and melt in a water bath at 70°C, add 12mg of oleic acid, stir and mix well, then add 5mg of camptothecin, stir for 30min, add 30mL containing 1.5% Tween 20 deionized water, high-speed stirring, ultrasonication, and centrifugation in an ice bath to obtain the targeted camptothecin nanostructured lipid carrier.

Embodiment 3

[0051] Preparation of targeted fluorescent bifunctional paclitaxel nanostructured lipid carrier:

[0052] 10mg of stearic acid was dissolved in 30mL of N,N-dimethylformamide and stirred to dissolve. 10 mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and 5 mg of N-hydroxysuccinimide were added, followed by stirring for 1 hour. Then add 100 mg of glucosamine, stir for 4 hours, and dialyze to obtain target-modified stearic acid.

[0053] Take 34mg of target-modified stearic acid and 34mg of glyceryl monostearate and melt in a water bath at 70°C, add 12mg of oleic acid, stir and mix well, then add 5mg of fluorescent dye and 5mg of paclitaxel, stir for 30min, add 30mL containing 1.5% Deionized water at a temperature of 20°C, high-speed stirring, ultrasonication, and centrifugation in an ice bath were used to obtain targeted fluorescent bifunctional paclitaxel nanostructured lipid carriers.

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Abstract

The invention relates to the field of medicinal preparations, in particular to a target and fluorescence dual-functional slightly-soluble antitumor medicament nano structural lipid carrier. In the slightly-soluble antitumor medicament nano structural lipid carrier, a lipid carrier of which the inside carries medicaments is formed by solid lipid, liquid lipid, surfactants and slightly-soluble antitumor medicaments; and the surface of the lipid carrier is chemically modified and is in covalent connection with a ligand with a tumor target. The slightly-soluble antitumor medicament nano structural lipid carrier can prolong the in-vivo circulation time of the slightly-soluble antitumor medicaments and improve the bioavailability of the slightly-soluble antitumor medicaments and can be used fortopical diagnosis of tumors by fluorescence imaging.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations. It specifically relates to a nanostructured lipid carrier targeted drug delivery system for insoluble antitumor drugs, including the targeted delivery of insoluble antitumor drugs by nanostructured lipid carriers and the application of fluorescence imaging in tumor location diagnosis. Background technique [0002] Tumor is a major disease that threatens human health at present. The current methods of treating tumors mainly include radiotherapy, chemotherapy, surgical therapy and gene therapy. Radiotherapy and chemotherapy are very important non-surgical treatments, but while killing tumor cells, radiotherapy and chemotherapy also cause serious damage to normal cells in the body. Especially for chemotherapy, due to the lack of targeting of the drug itself, there are major treatment problems such as low cure rate, multidrug resistance, and huge toxic and side effects. [0003] Paclitax...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/26A61K47/34A61K47/44A61K49/18A61K31/337A61K31/4745A61P35/00A61K47/54A61K47/69
Inventor 顾月清陈晶邓大伟
Owner CHINA PHARM UNIV
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