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Folic acid-glucan conjugate and application thereof

A technology of glucan and conjugates, applied in the field of folic acid-glucan conjugates, can solve the problems of low synthesis efficiency, loss of drug adaptability, no reported particle anti-tumor effect, etc., to reduce toxic side effects, reduce Treatment costs, effects of good drug adaptation

Inactive Publication Date: 2014-06-18
SUZHOU YOULIN BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent 20121002970.5 discloses covalently bonded folic acid-dextran-iron oxide nanoparticles, which have an in vitro targeting effect, but it has not reported the anti-tumor effect of the particle itself (actually basically none), and the inventors found that its It is to synthesize dextran-iron oxide nanoparticles first, and then carry out folic acid conjugation, the synthesis efficiency is low, and the adaptability of excipients to drugs is lost

Method used

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  • Folic acid-glucan conjugate and application thereof
  • Folic acid-glucan conjugate and application thereof
  • Folic acid-glucan conjugate and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1: Preparation of folic acid-dextran conjugates

[0068] 1. Synthesis of Succinylated Dextran

[0069] The synthetic route is as follows:

[0070]

[0071] Get 10.0g dextran (average molecular weight 20KDa, Mw / Mn=1.3, can be purchased from Shanghai Sunshine Reagent Co., Ltd.) and dissolve in anhydrous dimethylformamide (DMF), stir for 20 minutes to form a clear solution, then add 1670 mg succinic anhydride and 200.0 mg 4-dimethylaminopyridine (DMAP), stir rapidly until all solids dissolve. Place the reaction solution at room temperature (25° C.) to react for 24 hours, then put the reaction solution into a Spectra / Por3 dialysis bag (molecular weight cut-off 3,500) and dialyze in water for 2 days. The solution in the dialysis bag was then freeze-dried to obtain white succinylated dextran. Nuclear magnetic resonance (NMR) results are as follows: 1H-NMR (d-DMSO): 2.8 (-CH 2 CH 2 -, succinylated dextran), 3.2-3.6 (dextran), 4.4-5.8 (dextran).

[0072] 2. Syn...

Embodiment 2

[0081] Example 2: Preparation and Stability Test of Freeze-dried Powder Injection of Paclitaxel Encapsulated by Folic Acid-Dextran Conjugate

[0082] Take 1000 mg of the folic acid-dextran conjugate prepared in Example 1 and dissolve it in 100 ml of 15 mM phosphate buffer (pH=7.4). After dissolving, place it on a magnetic stirrer and stir at 400 rpm. During the stirring process, 250 mg of paclitaxel was dissolved in 5 mL of ethanol, added dropwise to the stirred solution, and placed in the FS-1 type high-speed homogenizer (available from Jintan Zhongzheng Instrument Manufacturing Co., Ltd.) , Homogenize 6 times at maximum power, 1 minute each time, stop for 2 minutes, then put the homogenate into a Spectra / Por3 dialysis bag (molecular weight cut-off 3,500), and dialyze in 15mM phosphate buffer (pH=7.4) 12 hours to remove ethanol, then add 2500mg mannitol to adjust the osmotic pressure, and pass through a 0.2μm membrane filter to sterilize. After being detected by a particle s...

Embodiment 3

[0086] Example 3: Pharmacodynamic study of paclitaxel freeze-dried powder injection coated with folic acid-dextran conjugate

[0087] The tumor cytotoxicity test was carried out on the freeze-dried powder injection prepared in Example 2, and the tested cells were human non-lobular lung cancer cells. Freeze-dried powder injections of different concentrations were added to the IC50 was calculated after 72 hours of treatment in cell culture medium. The results showed that the cytotoxicity of paclitaxel encapsulated by various concentrations of folic acid-dextran conjugates was similar to that of paclitaxel of the same concentration without any treatment, and the calculated IC50 was , while the cytotoxicity of the folic acid-dextran conjugate itself is very small, IC50>0.05mg / ml, it can be seen that the cytotoxicity in vitro mainly comes from paclitaxel, and the folic acid-dextran conjugate basically does not affect paclitaxel cells The exertion of toxic effects.

[0088] The...

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Abstract

The invention discloses a folic acid-glucan conjugate and an application thereof. The method comprises the following steps: synthesizing amber acylation glucan; synthesizing amino folic acid analogues; and synthesizing the folic acid-glucan conjugate. The invention also discloses an application of the folic acid-glucan conjugate for preparing a drug composition, and the like.

Description

technical field [0001] The present invention is an invention of Chinese patent application No. 201210543504.9, and enjoys a filing date of December 14, 2012. [0002] The invention belongs to the field of pharmaceutical preparations, in particular, the invention relates to folic acid-dextran conjugates, which can improve the physicochemical properties of pharmaceutical compounds (such as paclitaxel) encapsulated with them, even It can work synergistically and can improve drug tolerance. In addition, the present invention also relates to the application of the folic acid-dextran conjugate to prepare a pharmaceutical composition and its preparation method. Background technique [0003] Most anticancer drugs currently used clinically, such as paclitaxel, Docetaxel (docetaxel), doxorubicin, etc., have poor solubility in normal saline and cannot be directly used clinically, and some auxiliary materials are required. For example, Paclitaxel was formulated with a mixture of pol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/02A61K47/36A61K31/337A61P35/00
Inventor 李军游绍进陈琼
Owner SUZHOU YOULIN BIO TECH
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