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Silica body loaded with 10-hydroxycamptothecin and its preparation method

A technology of hydroxycamptothecin and siliceous body, which is applied in the fields of medicinal chemistry and therapeutics, can solve the problems of drug loading not exceeding 2%, low siliceous body encapsulation rate, etc. Effect

Active Publication Date: 2016-07-13
NORTHEAST FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Silicone body is a new type of silicon-containing liposome vesicles, which can be used to load drugs, but the encapsulation efficiency of silicon body obtained by traditional preparation methods is low (less than 70%), and the drug loading capacity is not more than 2%.

Method used

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  • Silica body loaded with 10-hydroxycamptothecin and its preparation method
  • Silica body loaded with 10-hydroxycamptothecin and its preparation method
  • Silica body loaded with 10-hydroxycamptothecin and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 Synthesis of Silicon-containing Lipid Molecules

[0028] Add 2.3 grams of 1,3-oleic acid glyceride into dry dichloromethane, and after fully dissolving, continue to add 1 gram of aminopropyltriethoxysilane and 5 grams of 1-(3-dimethylaminopropyl base)-3-ethylcarbodiimide hydrochloride, and the reaction system was stirred at 25°C for 4 hours. The reaction product was rotary evaporated under vacuum conditions to obtain a crude product, which was purified by column chromatography and then obtained by rotary evaporation to obtain silicon-containing lipid molecules with a yield of 50%.

[0029] 1 HNMR (400MHz, CDCl 3 ,TMS,ppm):δ0.59(2H,t),0.85(6H,t),1.21(9H,t),1.22-1.26(54H,m),1.489-1.64(6H,m),2.59(2H ,t),3.19-3.30(2H,m),3.49-3.53(2H,t),3.63-3.66(4H,t),3.68-3.86(6H,m),3.95-4.10(4H,t)6.40(1H ,s).

Embodiment 2

[0030] Embodiment 2 Synthesis of Silicon-containing Lipid Molecules

[0031] Add 3.4 grams of 1,3-oleic acid glyceride into dry dichloromethane, and after fully dissolving, continue to add 0.8 grams of aminopropyltriethoxysilane and 6.2 grams of 1-(3-dimethylaminopropyl base)-3-ethylcarbodiimide hydrochloride, and the reaction system was stirred at 27.5°C for 3.8 hours. The reaction product was rotary evaporated under vacuum to obtain a crude product, which was purified by column chromatography and then obtained by rotary evaporation to obtain silicon-containing lipid molecules with a yield of 55%.

[0032] 1 HNMR (400MHz, CDCl 3 ,TMS,ppm):δ0.59(2H,t),0.85(6H,t),1.21(9H,t),1.22-1.26(54H,m),1.489-1.64(6H,m),2.59(2H ,t),3.19-3.30(2H,m),3.49-3.53(2H,t),3.63-3.66(4H,t),3.68-3.86(6H,m),3.95-4.10(4H,t)6.40(1H ,s).

Embodiment 3

[0033] The synthesis of embodiment 3 silicon-containing lipid molecules

[0034] Add 1.5 grams of 1,3-oleic acid glyceride to dry dichloromethane. After fully dissolving, continue to add 0.78 grams of aminopropyltriethoxysilane and 4.4 grams of 1-(3-dimethylaminopropyl base)-3-ethylcarbodiimide hydrochloride, and the reaction system was stirred at 23°C for 6 hours. The reaction product was rotary evaporated under vacuum to obtain a crude product, which was purified by column chromatography and then obtained by rotary evaporation to obtain silicon-containing lipid molecules with a yield of 58.5%.

[0035] 1 HNMR (400MHz, CDCl 3 ,TMS,ppm):δ0.59(2H,t),0.85(6H,t),1.21(9H,t),1.22-1.26(54H,m),1.489-1.64(6H,m),2.59(2H ,t),3.19-3.30(2H,m),3.49-3.53(2H,t),3.63-3.66(4H,t),3.68-3.86(6H,m),3.95-4.10(4H,t)6.40(1H ,s).

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Abstract

Disclosed are a 10-hydroxycamptothecin-loaded silica body and a preparation method therefor. The method comprises the following steps: dissolving 10-hydroxycamptothecin in an acidic dichloromethane solution with the pH value of 2 to 4; adding siliceous lipid molecules into the acidic dichloromethane solution of the 10-hydroxycamptothecin under the ice water bath conditions by 3 to 10 batches, stirring for 10 to 120 minutes while continuing maintaining the ice water bath conditions, and removing the solvent in the reaction mixed solution; adding an ethanol / water solution into the solvent-removed solution, treating in a water bath at 50°C to 80°C for 10 to 240 minutes, and carrying out ultrasonic treatment on the solution for 1 to 20 minutes; and centrifugating the mixed solution subjected to the ultrasonic treatment, taking the supernate, and carrying out freeze-drying on the supernate to obtain the 10-hydroxycamptothecin-loaded silica body. By using the silica body, the encapsulation efficiency of the 10-hydroxycamptothecin is at least 75%, and the drug loading rate is at least 3%.

Description

technical field [0001] The invention relates to the fields of medicinal chemistry and therapeutics, in particular to a silicon body loaded with 10-hydroxycamptothecin and a preparation method thereof. Background technique [0002] Camptothecin (CPT) is an alkaloid extracted from the unique plant Camptothecus in my country. In the early in vitro activity screening, camptothecin showed strong anti-tumor activity and had obvious inhibitory effect on a variety of solid tumors and leukemia. However, camptothecin has poor water solubility and strong toxicity, which limits its use in tumor therapy. on the application. In 1985, Hsiang Y.H. found that camptothecin exerted cytotoxic activity by inhibiting topoisomerase Ⅰ, which aroused people's attention again. [0003] 10-Hydroxycamptothecin is a natural derivative of camptothecin. It is an anti-tumor drug widely used clinically in my country. The molecular structure of 10-Hydroxycamptothecin is as follows. [0004] [0005] Th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F7/08A61K47/24
CPCA61K47/24C07F7/08
Inventor 阎秀峰王洋张明珠丁为民于涛
Owner NORTHEAST FORESTRY UNIVERSITY
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