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Self-assembled nano-system of unsaturated fatty acid-anti-tumor drug conjugates as well as preparation method and application thereof

A technology for unsaturated fatty acids and anti-tumor drugs, which can be used in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., and can solve problems such as toxic side effects, low drug loading, and drug leakage.

Inactive Publication Date: 2016-06-01
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the drug loading of the carrier-dependent nano-delivery system is generally low, and the drug in the carrier will leak and cause unexpected toxic side effects in the form of carrier-loaded drug

Method used

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  • Self-assembled nano-system of unsaturated fatty acid-anti-tumor drug conjugates as well as preparation method and application thereof
  • Self-assembled nano-system of unsaturated fatty acid-anti-tumor drug conjugates as well as preparation method and application thereof
  • Self-assembled nano-system of unsaturated fatty acid-anti-tumor drug conjugates as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] Embodiment 1: the synthesis of oleic acid-paclitaxel conjugate

[0103] Under nitrogen protection, paclitaxel (85mg, 0.1mmol) was dissolved in an appropriate amount of anhydrous dichloromethane, dimethylaminopyridine (14.4mg, 0.1mmol) and dicyclohexylcarbodiimide (24.6mg, 0.2mmol) were added ), and then added oleic acid (28mg, 0.1mmol) under stirring conditions, and continued to stir and react at room temperature for 12 hours. Remove the precipitate by filtration, dry the filtrate under reduced pressure and vacuum, dissolve it with a small amount of solvent and separate it by thin-layer analysis. The oleic acid-paclitaxel conjugate was obtained (63% yield).

[0104]

Embodiment 2

[0105] Example 2: Synthesis of α-linolenic acid-paclitaxel conjugates

[0106] Under nitrogen protection, paclitaxel (85mg, 0.1mmol) was dissolved in an appropriate amount of anhydrous dichloromethane, dimethylaminopyridine (14.4mg, 0.1mmol) and dicyclohexylcarbodiimide (24.6mg, 0.2mmol) were added ), and then added oleic acid (28mg, 0.1mmol) under stirring conditions, and continued to stir and react at room temperature for 12 hours. Remove the precipitate by filtration, dry the filtrate under reduced pressure and vacuum, dissolve it with a small amount of solvent and separate it by thin-layer analysis. The α-linolenic acid-paclitaxel conjugate was obtained (68% yield).

[0107]

Embodiment 3

[0108] Embodiment 3: the synthesis of DHA-SN38 conjugate

[0109] Under nitrogen protection, 7-ethyl-10-hydroxycamptothecin (40mg, 0.1mmol) was dissolved in an appropriate amount of anhydrous N,N-dimethylformamide, and dimethylaminopyridine (14.4mg, 0.1mmol ) and dicyclohexylcarbodiimide (24.6mg, 0.2mmol), then added conjugated linoleic acid (33mg, 0.1mmol) under stirring conditions, and continued stirring at room temperature for 12 hours. Remove the precipitate by filtration, dry the filtrate under reduced pressure and vacuum, dissolve it with a small amount of solvent and separate it by thin-layer analysis. The DHA-SN38 conjugate was obtained (63% yield).

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Abstract

The invention relates to a self-assembled nano-system of unsaturated fatty acid-anti-tumor drug conjugates as well as a preparation method and application thereof. (1) Unsaturated fatty acid-anti-tumor drug conjugates can be self-assembled in water to form spherical nano-particles with uniform particle sizes and good stability; and (2) in a preparation process, an amphiphilic polymer material such as DSPE-PEG can be optionally added, so that the particle sizes of the self-assembled nano-particles can be further reduced, and the stability of the self-assembled nano-particles can be further enhanced. The self-assembled nano-system of unsaturated fatty acid-anti-tumor drug conjugates, provided by the invention, is simple in preparation method and easy in industrial production and has the advantages of high drug loading capacity, strong stability, good safety and the like; and growth inhibition tests of tumor cells in vitro prove that the self-assembled nano-system has favorable anti-tumor effects on multiple tumor cells.

Description

technical field [0001] The invention relates to the technical field of nano drug preparations, in particular to a self-assembled nano system of an unsaturated fatty acid-antitumor drug conjugate, a preparation method and application thereof. Background technique [0002] Chemotherapy drugs are one of the commonly used means of clinical anti-tumor treatment, but due to the toxic solvent contained in the preparation may cause obvious adverse reactions (such as polyoxyethylene castor oil added in Taxol may cause allergic reactions and neurotoxicity, etc.), and free The non-selectivity of the drug distribution in the whole body and the non-selectivity of cell killing may cause serious toxic side effects (such as cardiotoxicity caused by adriamycin, etc.), which greatly restricts its application and development. [0003] The nano-delivery system has the advantages of sustained release, passive targeting, improved bioavailability, prolonged circulation time in vivo, improved pharm...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K9/51A61P35/00A61K31/337A61K31/4745A61K31/704A61K31/475A61K33/24A61K31/7068
CPCA61K9/5146A61K31/337A61K31/4745A61K31/475A61K31/704A61K31/7068A61K33/24
Inventor 张烜钟婷
Owner PEKING UNIV
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