A kind of carboxymethyl chitosan-rhein conjugate modified by TPGS and its synthesis process and application

A carboxymethyl chitosan and conjugate technology, which is applied to TPGS-modified carboxymethyl chitosan-rhein conjugate and its synthesis process and application fields, can solve the problems of poor absorption, drug resistance, The problem of low drug encapsulation rate, etc., achieves the effect of less toxic and side effects, promoting absorption, and inhibiting drug resistance.

Active Publication Date: 2022-04-26
FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] However, the drug carriers in the prior art face the problems of low drug encapsulation efficiency, poor absorption and drug resistance

Method used

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  • A kind of carboxymethyl chitosan-rhein conjugate modified by TPGS and its synthesis process and application
  • A kind of carboxymethyl chitosan-rhein conjugate modified by TPGS and its synthesis process and application
  • A kind of carboxymethyl chitosan-rhein conjugate modified by TPGS and its synthesis process and application

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Experimental program
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Embodiment 1

[0055] The synthesis of embodiment 1TPGS-CR conjugate

[0056] 1. Synthesis of TPGS-SA intermediate

[0057] Weigh TPGS, succinic anhydride (SA) and 4-dimethylaminopyridine (DMAP), place in a vial, add triethylamine (TEA) dropwise, and the feeding amount is based on the molar ratio TPGS:SA:DMAP:TEA=1 :2:1:1, add appropriate amount of pyridine to dissolve. After magnetic stirring at room temperature for 24 h, pyridine was removed by rotary evaporation. The rotary evaporation residue was dissolved with an appropriate amount of dichloromethane, left to stand, centrifuged at 4000r / min for 10min, and the upper layer was evaporated to dryness to obtain a light yellow gel. The jelly was dissolved in an appropriate amount of water, stirred overnight by magnetic force, dialyzed for 72 hours, centrifuged to remove the precipitate, and the supernatant was freeze-dried to obtain a light yellow loose crude TPGS-SA.

[0058] 2. Synthesis of TPGS-CR conjugate

[0059] Weigh CMCS into a r...

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Abstract

The present invention provides a TPGS-modified carboxymethyl chitosan-rhein conjugate as shown in formula I, wherein A and B are independently selected from rhein or TPGS; n=436-512. The invention also provides the synthesis process of the conjugate and the application of the conjugate in the preparation of drug-loaded micelles. The TPGS modified carboxymethyl chitosan-rhein conjugate prepared by the present invention can self-assemble into micelles in water; the micelles have a very high drug loading capacity for paclitaxel, and the particle size is small; significantly promote paclitaxel in the stomach Intestinal absorption; the drug-loaded micelles have significant anti-tumor effects, can inhibit the drug-resistant effects of tumors, and have less toxic and side effects.

Description

technical field [0001] The invention relates to a TPGS modified carboxymethyl chitosan-rhein conjugate and its synthesis process and application. Background technique [0002] Polymeric micelles (PMs) are assembled by amphiphilic polymers and are thermodynamically stable systems that spontaneously form when the polymer concentration exceeds the critical micelle concentration. Polymer micelles have a typical shell-core structure and nano-scale particle size. They are characterized by stable properties, strong solubilization ability, good biocompatibility, and dilution resistance, making them more widely used in water-insoluble drugs (especially delivery of anticancer drugs). [0003] Paclitaxel (PTX) has significant curative effect on various cancers with its unique mechanism of inhibiting microtubule depolymerization. It has been approved by the USFDA for the treatment of non-small cell lung cancer, ovarian cancer, breast cancer, etc. However, the poor water solubility, p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/08A61K9/107A61K47/36A61K31/337A61P35/00
CPCC08B37/003A61K9/1075A61K47/36A61K31/337A61P35/00
Inventor 王晓颖邱梁桢欧阳惠枝王夏英
Owner FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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