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Degradable polyethyleneimine (PCFC-PEI) polymer preparation method and application in drug delivery system

A polymer and drug technology, which is applied in the directions of pharmaceutical formulations and medical preparations with inactive ingredients, can solve the problems of difficulty in loading genetic drugs, inactivation of genetic drugs, and large toxic and side effects, and achieves low cost, simple steps, and high performance. uniform effect

Inactive Publication Date: 2010-03-10
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] PEI25KD is a non-viral gene therapy vector with high transfection efficiency, but it has the disadvantages of high toxic side effects and non-degradable, so it has not entered clinical trials so far
PCFC is a degradable polymer material. The micelles made by self-assembly of PCFC can be loaded with chemotherapy drugs such as paclitaxel, curcumin, and honokiol, but it is difficult to load gene drugs.
Generally, polymers can only load DNA into the interior of nanoparticles by encapsulation, but this process requires the use of organic solvents, which usually leads to the inactivation of gene medicines

Method used

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  • Degradable polyethyleneimine (PCFC-PEI) polymer preparation method and application in drug delivery system
  • Degradable polyethyleneimine (PCFC-PEI) polymer preparation method and application in drug delivery system
  • Degradable polyethyleneimine (PCFC-PEI) polymer preparation method and application in drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 The preparation of PCFC-PEI of the present invention

[0040] Poloxamer (Pluronic105) Mn=1900g / mol

[0041] ε-caprolactone (ε-CL) Mn=114g / mol

[0042] Glycidyl methacrylate (GMA) Mn=142g / mol d=1.04g / ml

[0043] Dimethylaminopyridine DMAP Mn=122g / mol

[0044] Branched PEI (Sigma, USA) Mn=25000g / mol

[0045] 1. PCFC synthesis:

[0046] In a three-necked flask equipped with a stirrer, add Pluronic 105 (Mn=1900) and caprolactone (ε-CL) according to the reaction formula, use stannous octoate as a catalyst, and react for 5 hours at 130 ° C under nitrogen protection, and then the reaction system Pump down to vacuum. After 1 hour, the reaction was terminated. After the temperature of the reaction system dropped to room temperature, the polymer was dissolved with chloroform, then poured into cold petroleum ether for precipitation, and the solution was dissolved and precipitated three times. Finally, the purified polymer was vacuum-dried for later use. , Theore...

Embodiment 2

[0057] Example 2 Preparation of PCFC-PEI of the present invention

[0058] Poloxamer (Pluronic 105) Mn=1900g / mol

[0059] Caprolactone (ε-CL) Mn=114g / mol

[0060] Glycidyl methacrylate (GMA) Mn=142g / mol d=1.04g / ml

[0061] Dimethylaminopyridine DMAP Mn=122g / mol

[0062] Branched PEI (Sigma, USA) Mn=1800g / mol

[0063] Use the PEI of Mn=1800 to synthesize PCFC-PEI cross-linked copolymer of the present invention:

[0064] See Example 1 for specific reaction conditions. The main steps are: 1, PCFC synthesis; 2, the synthesis of GMA-PCFC-GMA (GCFCG), the nuclear magnetic spectrum of the product is as follows image 3 Shown; 3, Michael's addition reaction synthesis PCFC-PEI, the nuclear magnetic spectrum of the product is as Figure 4 As shown, the results indicated that the product was successfully synthesized.

Embodiment 3

[0065] Example 3 Preparation and Loading of Chemotherapeutic Drugs in PCFC-PEI Nanomicelles

[0066] Weigh 10 mg of PCFC-PEI copolymer and add it to 1 ml of distilled water at 50° C. After 5 minutes, PCFC-PEI micelles are formed due to temperature. Cool the PCFC-PEI micelles to 37°C and store them for later use. The particle size was detected by a Malvern particle size analyzer, and it was found that the particle size of the PCFC-PEI micelles and the Zeta potential changed with the temperature. The results show that the size of PCFC-PEI nanomicelles can be controlled by temperature.

[0067] The chemotherapeutic drugs curcumin, honokiol, paclitaxel, etc. are easily loaded in the PCFC-PEI copolymer nanomicelles of the present invention. (JY92-2D, Ningbo Xinzhi) for ultrasonic dispersion. After 30 minutes, the mixture of chemotherapeutic drugs and micelles was separated by high-speed centrifugation, and the chemotherapeutic drugs that were not loaded into the nanomicelles were...

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Abstract

The invention belongs to the field of pharmaceutical polymer materials, in particular to a degradable polyethyleneimine (PCFC-PEI) cross-linked polymer capable of transferring chemotherapy drugs and gene drugs simultaneously, a preparation method and an application thereof. The PCFC-PEI carrier is a novel carrier material obtained by coupling polycaprolactone poloxamer-polycaprolactone and the polyethyleneimine, wherein the poloxamer is triblock copolymer of polyethylene glycol-polypropylene glycol-polyethylene glycol, the molecular weight thereof is 1100-12500, and the molecular weight of polyethyleneimine section is 600-25000. The degradable polyethyleneimine cross-linked polymer can be used as a novel drug-release carrier, and can transfer the micromolecular chemotherapy drugs and genetherapy drugs simultaneously, thus having wide application prospect in the preparation of anti-tumor drugs.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical polymer materials, and in particular relates to a degradable polyethylenimine cross-linked polymer PCFC-PEI for simultaneous delivery of chemotherapeutic drugs and gene drugs, a preparation method thereof and an application in a drug delivery system. Background technique: [0002] In the process of tumor treatment, if chemotherapy and gene therapy can be combined, the therapeutic effect will be synergistic or additive. However, there are still few simultaneous delivery systems for chemotherapy drugs and gene drugs, so a new type of delivery system has been developed. System is very important. [0003] There are many literatures about polyethyleneimine (PEI) as gene therapy carrier. Among them, the polyethylene glycol graft copolymer of PEI (PEI-g-PEG), water-soluble lipopolymer, degradable PEI, and PEI combined with targeting units are reviewed; in the literature, hyaluronic acid grafted polyethyle...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00A61K47/34
Inventor 钱志勇魏于全赵霞邓洪新
Owner SICHUAN UNIV
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