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Triptolide-multiarm polyethylene glycol-hydroxycamptothecine binder nanoparticle and preparation method thereof

A multi-arm polyethylene glycol, triptolide technology, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of pH sensitivity of lactone ring, reduced anticancer activity, large toxic and side effects, etc. Environmentally friendly, easy to operate, and the effect of improving the curative effect

Inactive Publication Date: 2018-10-16
BEIJING FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Hydroxycamptothecin (10-Hydroxy camptothecin, HCPT) is a camptothecin anticancer drug widely used clinically in my country at present. It has a broad-spectrum anticancer effect, but the main problem in clinical application is its short half-life. , the lactone ring is sensitive to pH, the anti-cancer activity decreases after ring opening and it is extremely difficult to dissolve in water. In order to improve the solubility, HCPT is mostly applied in the form of ring-opening sodium salt injection and powder injection, which has low curative effect and large toxic and side effects

Method used

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  • Triptolide-multiarm polyethylene glycol-hydroxycamptothecine binder nanoparticle and preparation method thereof
  • Triptolide-multiarm polyethylene glycol-hydroxycamptothecine binder nanoparticle and preparation method thereof
  • Triptolide-multiarm polyethylene glycol-hydroxycamptothecine binder nanoparticle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0025] (1) Preparation of multi-arm polyethylene glycol-triptolide prodrug:

[0026] Take 100mg of eight-armed polyethylene glycol (MW40K) in a 50mL dry three-neck flask, add 15mL of tetrahydrofuran and magnetically stir for 20min to fully dissolve it, then add 5.8mg of EDC and 6.1mg of DMAP; then add 5.4mg of TP, at 35°C Magnetically stirred for 48 hours; after the reaction was completed, 15ml of ether was added to the reaction solution, and a large amount of white flocculent precipitate appeared, and then centrifuged at a speed of 4000rpm for 15 minutes to collect the lower layer of solid precipitate, and then continued to wash the precipitate with ether repeatedly three times, centrifuged Obtain a white solid, dissolve the obtained white solid in 10mL deionized water, transfer the solution to a 1000D dialysis bag, and dialyze in phosphate buffer for eight hours, accompanied by magnetic stirring to increase the dialysis speed; after the dialysis, the above solution Freeze-dr...

Embodiment 2

[0032] (1) Preparation of multi-arm polyethylene glycol-triptolide prodrug:

[0033] Take 100mg of eight-armed polyethylene glycol (MW20K) in a 50mL dry three-neck flask, add 15mL of tetrahydrofuran and magnetically stir for 20min to fully dissolve it, then add 6.9mg of EDC and 7.3mg of DMAP; then add 11.4mg of TP, at 35°C Magnetically stirred for 48 hours; after the reaction was completed, 15ml of ether was added to the reaction solution, and a large amount of white flocculent precipitate appeared, and then centrifuged at a speed of 4000rpm for 15 minutes to collect the lower layer of solid precipitate, and then continued to wash the precipitate with ether repeatedly three times, centrifuged Obtain a white solid, dissolve the obtained white solid in 10mL deionized water, transfer the solution to a 1000D dialysis bag, and dialyze in phosphate buffer for eight hours, accompanied by magnetic stirring to increase the dialysis speed; after the dialysis, the above solution Freeze-d...

Embodiment 3

[0038] (1) Preparation of multi-arm polyethylene glycol-triptolide prodrug:

[0039] Take 100mg of four-armed polyethylene glycol (MW20K) in a 50mL dry three-neck flask, add 15mL of tetrahydrofuran and magnetically stir for 20min to fully dissolve it, then add 2.7mg of EDC and 1.3mg of DMAP; then add 3.0mg of TP, at 35°C Magnetically stirred for 48 hours; after the reaction was completed, 15ml of ether was added to the reaction solution, and a large amount of white flocculent precipitate appeared, and then centrifuged at a speed of 4000rpm for 15 minutes to collect the lower layer of solid precipitate, and then continued to wash the precipitate with ether repeatedly three times, centrifuged Obtain a white solid, dissolve the obtained white solid in 10mL deionized water, transfer the solution to a 1000D dialysis bag, and dialyze in phosphate buffer for eight hours, accompanied by magnetic stirring to increase the dialysis speed; after the dialysis, the above solution Freeze-dry...

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Abstract

The invention discloses a triptolide-multiarm polyethylene glycol-hydroxycamptothecine binder nanoparticle and a preparation method thereof. The triptolide-multiarm polyethylene glycol-hydroxycamptothecine binder nanoparticle is characterized in that a triptolide-multiarm polyethylene glycol-hydroxycamptothecine binder is formed by connecting triptolide, multiarm polyethylene glycol and hydroxycamptothecine via ester bonds, the multiarm polyethylene glycol is used as a hydrophilic segment, the triptolide and hydroxycamptothecine are used as hydrophobic segments, and the triptolide-multiarm polyethylene glycol-hydroxycamptothecine binder is assembled by self in a water solution so as to form the nanoparticle.

Description

technical field [0001] The invention relates to a triptolide-multi-arm polyethylene glycol-hydroxycamptothecin conjugate nanoparticle and a preparation method thereof, belonging to the technical field of medicine and nanomedicine. Background technique [0002] Triptolide (Triptolide, TP), also known as triptolide and triptolide alcohol, is an epoxy diterpene lactone compound extracted from the traditional Chinese medicine Triptolide, and is one of the main active ingredients of Triptolide. Immunomodulation, anti-oxidation, anti-inflammation, anti-rheumatoid, anti-senile dementia, anti-tumor and other biological activities can inhibit the growth of various tumors and induce apoptosis. In recent years, the research on triptolide has gradually deepened. When exploring its powerful pharmacological activity, serious adverse reactions have also been found, such as serious adverse reactions to the body's digestive system, circulatory system, urinary system, reproductive system and ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/60A61K31/585A61K31/4745A61P35/00C08G65/331C08G65/333
CPCA61K47/6935A61K31/4745A61K31/585A61P35/00C08G65/331C08G65/33396A61K2300/00
Inventor 肖萌曹永丽郑督刘彦雪雷建都
Owner BEIJING FORESTRY UNIVERSITY
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