A kind of intelligent polycation nanocarrier, its preparation method and application

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: 2015-11-18
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • A kind of intelligent polycation nanocarrier, its preparation method and application
  • A kind of intelligent polycation nanocarrier, its preparation method and application
  • A kind of intelligent polycation nanocarrier, its preparation method and application

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preparation example Construction

[0055] Correspondingly, the embodiment of the present invention provides a method for preparing a smart polycation nanocarrier, which includes the following steps:

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

[0057] S02. Formation of smart polycationic nanocarrier: dissolvin...

Embodiment 1

[0090] Example 1 Synthesis of TP-PEG-b-PLL-b-PLC-HPPr triblock polymer

[0091] S111. The polymerization tube is evacuated and filled with nitrogen for protection, and 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, press Lys(BOC)-NCA monomer and HOOC-PEG-NH 2 The molar ratio of Cys(Trt)-NCA monomer and HOOC-PEG-NH was added to Lys(BOC)-NCA monomer at a ratio of 20:1, and reacted at a constant temperature for 24 hours under the protection of nitrogen. 2 Cys(Trt)-NCA monomer was added at a molar ratio of 10:1, and the reaction was continued at a constant temperature under the protection of nitrogen for 24 hours. After the reaction, 10 times of ether was added to precipitate, filtered and dried to obtain PEG-b-PLL(BOC) -b-PLC (Trt) triblock polymer.

[0092] S112. Dissolve the product PEG-b-PLL(Boc)-b-PLC(Trt) obtained above in DMF again, add 3 times the molar amount of succinimide phenylpropionate, a...

Embodiment 2

[0095] Example 2 Synthesis of TP-PEG-b-PLL-b-PLC-HPPr triblock polymer

[0096] S211. The polymerization tube is evacuated and filled with nitrogen for protection, and 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, press Lys(BOC)-NCA monomer and HOOC-PEG-NH 2 Add Lys(BOC)-NCA monomer at a molar ratio of 40:1, react at a constant temperature under nitrogen protection for 36 hours, and then press Cys(Trt)-NCA monomer and HOOC-PEG-NH 2 Cys(Trt)-NCA monomer was added at a molar ratio of 20:1, and the reaction was continued for 72 hours under the protection of nitrogen. After the reaction, 30 times of ether was added for precipitation, filtration and drying to obtain PEG-b-PLL(BOC) -b-PLC (Trt) triblock polymer.

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

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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 particularly relates to a smart polycation nano carrier, a preparation method and application thereof. Background technique [0002] Nanocarrier refers to a carrier system with nanometer scale that can load target substances such as drugs, genes, and proteins. The amphiphilic block polymer nanomicelle carrier has both hydrophilic and hydrophobic segments. When it reaches the critical micelle concentration in water, the hydrophilic and hydrophobic segments of the polymer will undergo microphase separation , It spontaneously forms a "core-shell" nanomicelle with a hydrophobic segment inside and a hydrophilic segment outside. This polymer micelle has a lower critical micelle concentration and a larger solubilization space. The stable inner core can contain hydrophobic drug molecules in its hydrophobic inner core through chemical, physical and coordination methods. When the polymer contains both cationic ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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