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Intelligent polycation nano-carrier, and preparation method and application thereof

A technology of nanocarriers and polycations, which is applied in the field of nanomedicine, can solve the problem of inability to have active targeted delivery of pH response and reduction responsiveness at the same time, anti-tumor nanocarriers that cannot simultaneously load multiple loads, and anti-tumor nanocarriers that cannot simultaneously Load and other issues, achieve good market prospects, avoid immune system clearance, and the method is simple and controllable

Active Publication Date: 2014-04-30
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to provide an intelligent polycation nanocarrier, which aims to solve the problem that the existing anti-tumor nanocarriers cannot simultaneously load multiple loads, have poor stability, cannot be completely degraded or metabolized, and cannot have active targeted delivery pH response at the same time. and reduction responsiveness, as well as the problem that its particle size cannot be adjusted
[0009] Another object of the present invention is to provide an intelligent polycation nanocarrier composition, which aims to solve the problem that the existing anti-tumor nanocarriers cannot simultaneously load multiple loads, and the nanocarrier composition has poor stability and cannot be completely degraded or metabolized, It cannot have the functions of active targeted delivery of pH response and reduction responsiveness at the same time, and its particle size cannot be adjusted

Method used

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  • Intelligent polycation nano-carrier, and preparation method and application thereof
  • Intelligent polycation nano-carrier, and preparation method and application thereof
  • Intelligent polycation nano-carrier, and preparation method and application thereof

Examples

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preparation example Construction

[0055] Correspondingly, an embodiment of the present invention provides a method for preparing an intelligent polycation nanocarrier, comprising the following steps:

[0056] S01. Synthesis of TP-PEG-b-PLL-b-PLC-capping agent tri-block polymer: by HOOC-PEG-NH 2 As an initiator, the amino acid NCA ring-opening polymerization reaction is gradually initiated to synthesize PEG-b-PLL(Boc)-b-PLC(Trt); succinimide phenylpropionate is used as an end-capping agent to block the end of PLC(Trt) The amino group obtains PEG-b-PLL(Boc)-b-PLC(Trt)-capping agent; after activating the carboxyl group at the PEG end of the polymer, it combines with the polypeptide TP that can mediate active targeted delivery to obtain TP-PEG-b-PLL( Boc)-b-PLC(Trt)-blocking agent; TP is obtained after removing TP-PEG-b-PLL(Boc)-b-PLC(Trt)-blocking agent side chain protecting group Boc group and Trt group - PEG-b-PLL-b-PLC-capper triblock polymer;

[0057] S02. Formation of intelligent polycation nanocarriers: d...

Embodiment 1

[0090] The synthesis of embodiment 1TP-PEG-b-PLL-b-PLC-HPPr triblock polymer

[0091] S111. Vacuum the polymerization tube and fill it with nitrogen to protect, and put 1g of HOOC-PEG-NH with a number average molecular weight of 500KD 2 Dissolve it with 20mL DMF and add it to the polymerization tube, mix Lys(BOC)-NCA monomer with HOOC-PEG-NH 2 Lys(BOC)-NCA monomer was added at a molar ratio of 20:1, reacted at a constant temperature for 24 hours under nitrogen protection, and then Cys(Trt)-NCA monomer and HOOC-PEG-NH 2 Add Cys(Trt)-NCA monomer at a molar ratio of 10:1, and continue to react at a constant temperature for 24 hours under nitrogen protection. After the reaction, add 10 times of diethyl ether to precipitate, filter, and dry to obtain PEG-b-PLL (BOC) - b-PLC(Trt) triblock polymer.

[0092] S112. Dissolve the above product PEG-b-PLL(Boc)-b-PLC(Trt) in DMF again, add 3 times molar amount of succinimide phenylpropionate, and react at room temperature (25°C) for 24 A...

Embodiment 2

[0095] The synthesis of embodiment 2TP-PEG-b-PLL-b-PLC-HPPr triblock polymer

[0096] S211. Vacuumize the polymerization tube and fill it with nitrogen protection, and put 0.5g of HOOC-PEG-NH with a number average molecular weight of 2000KD 2 Dissolve it with 30mL DMF and add it to the polymerization tube, mix Lys(BOC)-NCA monomer with HOOC-PEG-NH 2 Lys(BOC)-NCA monomer was added at a molar ratio of 40:1, reacted at a constant temperature under nitrogen protection for 36 hours, and then Cys(Trt)-NCA monomer and HOOC-PEG-NH 2 Add Cys(Trt)-NCA monomer at a molar ratio of 20:1, and continue to react at a constant temperature for 72 hours under nitrogen protection. After the reaction, add 30 times of ether to precipitate, filter, and dry to obtain PEG-b-PLL (BOC) - b-PLC(Trt) triblock polymer.

[0097] S212. Dissolve the above product PEG-b-PLL(Boc)-b-PLC(Trt) in DMF again, add 5 times molar amount of succinimide phenylpropionate, and react at room temperature (25° C.) for 24 H...

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Abstract

The invention is applicable to the field of nanometer medical science and provides an intelligent polycation nano-carrier capable of mediating active targeting delivery and restoring sensitivity at the same time and a preparation method and application thereof. The intelligent polycation nano-carrier comprises a TP-PEG-b-PLL-b-PLC-end-capping reagent triblock polymer and is divided into four layers from exterior to interior, wherein the outmost layer is polypeptide TP capable of mediating active targeting delivery, the second layer is PEC exerting a protection effect, the third layer is a positive charge layer formed by PLL, and the innermost layer is a PLC hydrophobic core formed by cross-linking of disulfide bonds. The polycation nano-carrier can carry a plurality of loads at the same time, is completely degradable and has active targeting delivery and responsiveness restoring functions and the like; and the particle size and the potential of the carrier are controllable.

Description

technical field [0001] The invention belongs to the field of nanomedicine, and in particular relates to an intelligent polycation nanocarrier, its preparation method and its application. Background technique [0002] Nanocarriers refer to nanoscale carrier systems that can load target substances such as drugs, genes, and proteins. The amphiphilic block polymer nanomicelle carrier has both a hydrophilic segment and a hydrophobic segment. When it reaches the critical micelle concentration in water, the hydrophilic segment and the hydrophobic segment of the polymer will undergo microphase separation. , spontaneously formed nano-micelles with a "core-shell" structure with hydrophobic segments inside and hydrophilic segments outside. This polymer micelle has a lower critical micelle concentration and a larger solubilization space. The stable inner core can encapsulate hydrophobic drug molecules in its hydrophobic inner core through chemical, physical and coordination methods, an...

Claims

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Application Information

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IPC IPC(8): C08G69/10C08G69/48C08G65/48A61K47/34A61K47/42
Inventor 蔡林涛易虎强谢高峰刘朋马轶凡
Owner SHENZHEN INST OF ADVANCED TECH
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