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Folic acid modified chitosan quaternary ammonium salt-taxol polymer medicine, as well as preparation method and application thereof

A technology of chitosan quaternary ammonium salt and paclitaxel, which is applied in the field of medicine, can solve the problems of inability to self-assemble and form, the inability to use the EPR effect to prevent tumors, and small molecular weight, so as to facilitate intestinal absorption, enhance small intestinal permeability, The effect of reducing toxicity

Inactive Publication Date: 2013-05-08
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Low-molecular-weight chitosan-paclitaxel polymer drugs have a small molecular weight and cannot self-assemble into nanoparticles, so they cannot use the EPR effect to improve anti-tumor efficacy

Method used

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  • Folic acid modified chitosan quaternary ammonium salt-taxol polymer medicine, as well as preparation method and application thereof
  • Folic acid modified chitosan quaternary ammonium salt-taxol polymer medicine, as well as preparation method and application thereof
  • Folic acid modified chitosan quaternary ammonium salt-taxol polymer medicine, as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Preparation of Succinyl Paclitaxel

[0041] Weigh 3 mg of succinic anhydride, add 4 mL of dichloromethane, stir; add 30 mg of PTX, stir; add 10 μL of anhydrous pyridine, the reaction system becomes clear, stir for 24 h; 50 °C vacuum distillation, add 10 mL of water , Stir for 15 min, centrifuge to collect the precipitate; add 30 mL of water to wash the precipitate, centrifuge to collect the precipitate, and vacuum dry.

Embodiment 2

[0042] Example 2 Preparation of Succinyl Paclitaxel

[0043] Weigh 6 mg of succinic anhydride, add 4 mL of dichloromethane, stir; add 30 mg of PTX, stir; add 20 μL of anhydrous pyridine, the reaction system becomes clear, stir for 40 h; 50 °C vacuum distillation, add 10 mL of water , Stir for 15 min, centrifuge to collect the precipitate; add 30 mL of water to wash the precipitate, centrifuge to collect the precipitate, and vacuum dry.

Embodiment 3

[0044] Example 3 Preparation of Succinyl Paclitaxel

[0045] Weigh 10 mg of succinic anhydride, add 4 mL of dichloromethane, stir; add 30 mg of PTX, stir; add 30 μL of anhydrous pyridine, the reaction system becomes clear, stir for 55 h; 50 °C vacuum distillation, add 10 mL of water , Stir for 15 min, centrifuge to collect the precipitate; add 30 mL of water to wash the precipitate, centrifuge to collect the precipitate, and vacuum dry.

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Abstract

The invention belongs to the technical field of medicines and specifically provides a folic acid modified chitosan quaternary ammonium salt-taxol polymer medicine, as well as a preparation method and an application of the polymer medicine. The polymer medicine provided by the invention is formed by connecting taxol to chitosan quaternary ammonium salt in the form of covalent linkage by succinyl ester and connecting tumor target ligand folic acid. The preparation method comprises the following steps of: connecting succinic anhydride open loop with taxol to synthesize succinyl taxol, modifying chitosan by quaternization to obtain chitosan quaternary ammonium salt; and under the action of a catalyst, connecting succinyl taxol to chitosan quaternary ammonium salt in the form of covalent linkage, and introducing target ligand folic acid. The polymer medicine can be assembled automatically in water to form nanoparticles, wherein hydrophobic medicine is used as the inner core and chitosan quaternary ammonium salt is used as a hydrophilic shell. The polymer medicine is simple in preparation method, excellent in repeatability and security, and can enhance the targeting and tumor inhibiting effect of taxol by two administration routes consisting of oral taking and intravenous injection.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a folic acid-modified chitosan quaternary ammonium salt-paclitaxel polymer medicine and a preparation method and application thereof. Background technique [0002] Due to poor water solubility, non-specific distribution in the body, and large toxic and side effects, anti-tumor chemicals cannot fully exert their therapeutic effects. As a first-line chemotherapy drug, paclitaxel can promote the assembly of microtubules and prevent the depolymerization of tubulin, thereby effectively inhibiting the rapid division and proliferation of cancer cells. However, paclitaxel is difficult to dissolve in water. The clinical paclitaxel injection uses polyoxyethylene castor oil / ethanol (1:1, v / v) as a solvent, which can cause allergic reactions and cardiovascular toxicity after intravenous injection. The use of a drug delivery system can overcome the above-mentioned shortcomings. The po...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/337A61P35/00
Inventor 印春华贺睿
Owner FUDAN UNIV
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