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Antitumor drug and preparation method thereof

An anti-tumor drug and drug technology, applied in the field of drugs, can solve the problems of poor efficiency, small toxic and side effects, and high-efficiency nanovesicles, and achieve the effects of efficient loading, avoiding losses and toxic side effects, and promoting cell proliferation.

Active Publication Date: 2018-09-18
SUZHOU UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, especially in the physiological environment, it is negatively charged, which leads to poor efficiency of its entry into cells.
[0006] However, in the existing polymer vesicle technology, there is still a lack of high-efficiency nanovesicles that are stable in vivo circulation, specifically target tumors, release drugs quickly in cells, and have low toxic and side effects, especially the lack of high-efficiency loading, very Biocompatible polymersomes with good protection

Method used

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  • Antitumor drug and preparation method thereof
  • Antitumor drug and preparation method thereof
  • Antitumor drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Example 1 Synthetic polymer PEG5k-P(DTC4.6k-TMC13.5k)-SP

[0079] The synthesis is divided into two steps. First, ring-opening polymerization is used to prepare PEG5k-P (DTC4.6k-TMC13.5k) diblock copolymer. The specific operation is as follows. Under nitrogen environment, MeO-PEG-OH ( M n = 5.0 kg / mol, 0.20 g, 40 μmol), TMC (0.6 g, 5.9 mmol) and DTC (0.192g, 1.0 mmol) were dissolved in dichloromethane (DCM, 6.8 mL), and the ring-opening polymerization catalyst was added rapidly, Such as zinc bis(bistrimethylsilyl)amine (7.7 mg, 20 μmol). The airtight reactor was sealed and placed under magnetic stirring in an oil bath at 40 °C for 24 hours. After terminating the reaction with glacial acetic acid, precipitate twice in glacial ether, filter with suction, and dry under vacuum at room temperature to obtain the product. Yield: 90.3%. 1 H NMR (400 MHz, DTCl 3 ): PEG: δ 3.38,3.65; TMC: δ 4.24, 2.05; DTC: δ 4.32, 3.02. According to NMR calculation, the molecular weight of...

Embodiment 2

[0083] Example 2 Synthesis of block copolymer Mal-PEG6k-P (DTC4.8k-TMC15.2k)-SP

[0084] The synthesis of Mal-PEG6k-P (DTC4.8k-TMC15.2k)-SP is similar to that of Example 1, and is also divided into two steps, except that the initiator MeO-PEG-OH in the first step is replaced by Malay Imide-functionalized Mal-PEG6k-OH, ring-opening polymerization of TMC and DTC to obtain Mal-PEG6k-P (DTC4.8k-TMC15.2k), then its terminal hydroxyl was activated with NPC, and then reacted with the primary amine of spermine be made of. The specific operation is similar to the first embodiment. Yield: 90.2%. 1H NMR (400 MHz, DTCl3): PEG: δ3.38, 3.65; TMC: δ 4.24, 2.05; DTC: δ 4.32, 3.02, and the characteristic peaks of Mal and spermine. The number-average molecular weight of the polymer was calculated as 6.0-(4.8-15.2)-0.2 kg / mol through the integral ratio of the characteristic peak area.

Embodiment 3

[0085] Example 3 Synthesis of Targeted Diblock Polymer DP8-PEG6.5k-P(DTC6k-TMC15k)

[0086] The synthesis of DP8-PEG6.5k-P(DTC6k-TMC15k) is similar to that of Example 1, which is also divided into two steps. In the first step, the initiator MeO-PEG-OH in the first step of Example 1 is replaced by NHS-PEG6.5k-OH functionalized with N-hydroxysuccinimide, and ring-opening polymerization of TMC and DTC is carried out to obtain NHS-PEG6 .5k-P(DTC6k-TMC15k), that is, add 0.15 g ( 0.781 mmol) DTC, 0.43 g of TMC, 0.2 g ( 0.0154 mmol) NHS-PEG6.5k-OH and 5 ml DCM was dissolved, and then 5.9 mg (0.0154 mmol) of a ring-opening polymerization catalyst such as bis(bistrimethylsilyl)amine zinc was added, and the subsequent treatment was the same as in Example 1. NMR calculated NHS-PEG6.5k-P (DTC6k-TMC15k) by integral area. In the second step, the polypeptide DMAPTVLP (DP8) is added according to the molar ratio of its amino group to NHS-PEG6.5k-P (DTC6k-TMC15k) 3:1, amidation reaction at 30...

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Abstract

The invention discloses an antitumor drug and a preparation method thereof. The antitumor drug is based on block polymer PEG-P (TMC-DTC)-SP or PEG-P (LA-DTC)-SP tumor targeting and has reduction-sensitive reversible crosslinking and intracellular-soluble crosslinking biodegradable polymeric vesicles with positively-charged internal membranes, and micromolecular drugs, which can be used for protecting biological macromolecules such as protein, DNA and siRNA and have negatively-charged physiological environments, can be efficiently loaded and can be conveyed into in-vivo tumor cells to induce the apoptosis of the tumor cells. The system has a variety of unique advantages, including simplicity and control in preparation, outstanding biocompatibility, excellent drug controlled release, superhigh in-vivo cycle stability, superior cancer cell targeted performance, remarkable cancer cell apoptosis capability and the like. Therefore, the antitumor drug advantageously becomes a nano-system platform integrating the advantages of simplicity, stability, multifunction and the like and is used for efficiently and actively conveying nucleic acid to in-situ tumors in a targeted manner.

Description

[0001] The invention belongs to the reversible cross-linked biodegradable polymer vesicles with a positive inner membrane and its preparation method and application in the preparation of anti-tumor drugs. The application date is July 15, 2016, and the application number is 201610558116.6 The divisional application of an invention application belongs to the product technology part. technical field [0002] The invention belongs to the technical field of medicines, and specifically relates to a reversible cross-linked biodegradable polymer vesicle with a positive inner membrane, a preparation method thereof, and an application in the delivery of biological medicines and negatively charged small molecule medicines in a physiological environment. It specifically relates to an antitumor drug based on a reversibly cross-linked biodegradable polymer vesicle with a positive inner membrane and a preparation method thereof. Background technique [0003] Cancer is a major killer that...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/34A61K45/00A61P35/00C08G81/00
CPCA61K9/1273A61K45/00A61P35/00C08G81/00A61K9/127A61K47/34
Inventor 孟凤华方媛杨炜静邹艳钟志远
Owner SUZHOU UNIV
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