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Anti-tumor nano medicine based on cross-linking biodegradable polymer vesica and preparation method of anti-tumor nano medicine

A technology for degrading polymers and nano-drugs, which is applied in the direction of anti-tumor drugs, drug combinations, and pharmaceutical formulations. Effects of preventing protein denaturation and solving disease problems

Active Publication Date: 2016-10-12
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the loading efficiency of existing vesicle technology for negatively charged small molecule anticancer drugs and protein drugs with high efficiency and low toxicity is low, or proteins and peptides remain in late endosomes / lysosomes for a long time (partially) Denaturation; at the same time, there are problems such as unstable circulation of vesicles, low uptake by tumor cells, and low drug concentration in cells, which lead to low drug efficacy and side effects of nano-medicines, which greatly limit the use of vesicles as such. Application of drug carrier

Method used

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  • Anti-tumor nano medicine based on cross-linking biodegradable polymer vesica and preparation method of anti-tumor nano medicine
  • Anti-tumor nano medicine based on cross-linking biodegradable polymer vesica and preparation method of anti-tumor nano medicine
  • Anti-tumor nano medicine based on cross-linking biodegradable polymer vesica and preparation method of anti-tumor nano medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Example 1 Synthesis of PEG5k-P(DTC4.4k-TMC19.8k)-bPEI1.8k block copolymer

[0073] The synthesis of PEG5k-P(DTC4.4k-TMC19.8k)-bPEI1.8k is divided into two steps, the first is ring-opening polymerization to prepare PEG5k-P(DTC4.4k-TMC19.8k) diblock copolymer, the specific operation is as follows , in a nitrogen glove box, weigh MeO-PEG-OH ( M n = 5.0 kg / mol, 0.50 g, 100 μmol), TMC (2.0 g, 19.2 mmol) and DTC (0.50 g, 2.60 mmol) were dissolved in dichloromethane (DCM, 7.0 mL), and the ring-opening polymerization catalyst such as Zinc bis(bistrimethylsilyl)amine (29 mg, 75 μmol). The airtight reactor was sealed and placed under magnetic stirring in an oil bath at 40 °C for 2 days. 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 PEG5k-P (DTC4.4k-TMC19.8k).

[0074] Next, PEG5k-P (DTC4.4k-TMC19.8k) was activated by p-nitrophenyl hydroxychloroformate NPC, ...

Embodiment 2

[0076] Example 2 Synthesis of copolymer Mal-PEG6k-P(DTC3.2k-TMC15.4k)-bPEI1.8k

[0077] Its synthesis is similar to Example 1, and it is also divided into two steps, except that the initiator MeO-PEG-OH in the first step is replaced by maleimide-functionalized Mal-PEG6k-OH, and the ring-opening polymerization of TMC and DTC to obtain Mal-PEG6k-P (DTC3.2k-TMC15.4k), and then its terminal hydroxyl was activated by NPC, and then reacted with the primary amine of bPEI1.8k. The specific operation is similar to the first embodiment. Yield: 90.2%. 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, PEI: δ 2.56-2.98, and the characteristic peak of Mal. The number-average molecular weight of the polymer was calculated as 6.0-(3.2-15.4)-1.8 kg / mol through the characteristic peak area integral ratio.

[0078]

Embodiment 3

[0079] Example 3 Synthetic polymer Azide-PEG6.5k-P(DTC4.0k-LA15.3)-lPEI0.7k

[0080] Its synthesis is similar to Example 1, and it is also divided into two steps, except that the MeO-PEG-OH in the first step is replaced by azide-functionalized Azide-PEG6.5k-OH, and Azide-PEG6 is obtained by ring-opening polymerization of LA and DTC .5k-P (DTC4.0k-LA15.3), and then its terminal hydroxyl is activated by NPC, and then reacted with the primary amine of linear PEI (lPEI0.7k). Yield: 90.2%. 1H NMR (400MHz, DTCl3): PEG: δ 3.38, 3.65; TMC: δ 4.24, 2.05; DTC: δ 4.32, 3.02, and the characteristic peaks of PEI. The number-average molecular weight of the polymer was calculated as 6.5-(4.0-15.3)-0.7 kg / mol through the characteristic peak area integral ratio.

[0081]

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Abstract

The invention discloses an anti-tumor nano medicine based on cross-linking biodegradable polymer vesicae and a preparation method of the anti-tumor nano medicine. The anti-tumor nano medicine is prepared by loading a medicine on reversible cross-linking biodegradable polymer vesicae of asymmetric membrane structures; the medicine is a protein medicine, a polypeptide drug or a small molecule medicine; the reversible cross-linking biodegradable polymer vesicae of the asymmetric membrane structures are prepared from a polymer in a manner of self-assembling and cross-linking in sequence; the molecular chain of the polymer comprises a hydrophilic chain segment, a hydrophobic chain segment and PEI molecules which are connected in sequence; the hydrophobic chain segment comprises a polycarbonate chain segment and / or polyester chain segment; the medicine can be compounded and loaded under the electrostatic interaction of PEI; a membrane is reversible cross-linking biodegradable polyester / polycarbonate which is good in compatibility; dithiolane of a side chain is similar to a human body natural antioxidant lipoic acid; a shell takes PEG as a background and can target to cancer cells; the anti-tumor nano medicine has the potential to be a nano medicine system with advantages of simplicity, stability, multifunction and the like.

Description

technical field [0001] The invention belongs to the drug carrier technology, in particular to an anti-tumor nano-medicine based on cross-linked biodegradable polymer vesicles and a preparation method thereof. Background technique [0002] Cancer is a major killer that threatens human health, and its morbidity and mortality are increasing year by year. Protein and peptide drugs have the advantages of high efficiency, strong specificity, low toxicity and side effects, and are not affected by drug resistance in anticancer. However, many protein drugs that induce apoptosis need to enter cells to play a role, and the large protein size has poor ability to enter cells, and is easily degraded by proteases in body fluids, which greatly affects its anticancer effect. In addition, some water-soluble small molecule anticancer drugs, especially negatively charged drugs in physiological environment, such as pemetrexed disodium and methotrexate disodium, are difficult to enter cells effi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/34A61K38/41A61K31/519A61P35/00C08G81/02
CPCA61K9/1273A61K31/519A61K38/415A61K47/34C08G81/027
Inventor 孟凤华杨炜静方媛邹艳钟志远
Owner SUZHOU UNIV
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