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Nanometer micelle capable of intelligently releasing medicine as well as preparation method and application thereof

A nano-micelle and drug-loaded nano-technology, which is applied in the fields of polymer chemistry and biomedical engineering, can solve the problems of easy disintegration of assemblies, easy disintegration, and easy phagocytosis of micellar particle size, so as to prolong blood circulation time, good Chain flexibility, beneficial effect of cell absorption

Active Publication Date: 2012-03-28
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the general nano drug-loaded micelles also have their shortcomings: ( ) the size of the micelles is easy to be swallowed, and the half-life in the body is not long. () Under physiological conditions, micelles are not very stable and easy to disintegrate, resulting in burst release. The drug cannot be maintained at a stable and effective concentration for a long time; () the drug loading capacity of the micelle itself is not high, which greatly Limit its application as a drug carrier
Moreover, these acid-sensitive nanomicelles do not leak drugs under neutral conditions, but they still undergo burst drug release after a few hours of sample preparation.
Moreover, in blood circulation, supramolecular nanoassemblies are prone to disintegration when the concentration of polymer micelles gradually decreases below the CMC, which is another reason for drug loss during drug delivery.
Although the loss of free drug due to burst release and disintegration can be overcome by covalently binding the drug to the delivery vehicle, unfortunately most drugs do not have active groups that can covalently interact

Method used

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  • Nanometer micelle capable of intelligently releasing medicine as well as preparation method and application thereof
  • Nanometer micelle capable of intelligently releasing medicine as well as preparation method and application thereof
  • Nanometer micelle capable of intelligently releasing medicine as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1 Preparation of Nanomicelle PEG-PAsp(MEA)-PAsp(DIP)

[0068] 1. Preparation of polymer PEG-PBLA:

[0069] The polymer is PEG-NH 2 As an initiator, it can be obtained by ring-opening polymerization of BLA-NCA. 0.8 g PEG-NH 2 (0.4mmol, 2000 g / mol) was added to a 100 mL reaction flask and dissolved in 50 mL of anhydrous dichloromethane. Weigh 1.0 g of BLA–NCA (4 mmol, 249.22 g / mol), add 5 mL of anhydrous DMF (N,N-dimethylformamide) to dissolve. Transfer the dissolved BLA–NCA solution into the PEG-NH 2 In a reaction flask, the reaction was stirred at 35°C for 72h. After the reaction, the reaction solution was dropped into excess cold ether (eg 500ml) for precipitation, and the final product was obtained by suction filtration, repeated washing with anhydrous ether, and vacuum drying.

[0070] 2. Polymer PEG-PBLA-COCH 2 Preparation of Br:

[0071] Weigh 0.9 g PEG-PBLA (3025 g / mol, 0.3 mmol) in a 25 mL reaction vial, add 15 mL CHCl 3 To dissolve, then add 0.2...

Embodiment 2

[0089] Example 2 Preparation of drug-loaded nanomicelles

[0090] 5mg PEG-PAsp(MEA)-PAsp(DIP) polymer and 1mg DOX were co-dissolved in a mixed solvent of THF and DMSO (1mL, v / v=1 / 1), and triethylamine was added to adjust the pH value of the solution to 10, At the same time, DTT (10 eq in the polymer) was added to reduce the disulfide bonds present in the polymer for 30 min. Under ultrasonic conditions, the above solution was slowly dripped into the PBS (pH 7.4) solution, and the resulting mixture was passed through oxygen for 2 hours, then placed in a dialysis bag (MWCO: 1000 Da), and passed through in the PBS (pH 7.4) solution Dialyzed under oxygen for 2 days to obtain drug-loaded nanomicelles.

[0091] The particle size of the obtained drug-loaded nanomicelles is measured by a dynamic light scattering system, and the test results are shown in figure 2 . From the dynamic light scattering parabola diagram, it can be seen that the average particle size of the drug-loaded na...

Embodiment 3

[0092] Example 3 Preparation of loaded nano-gold nano-binding gel

[0093] Take 1 mL of the nanomicelle solution (0.4 mg / mL, pH 7.4) prepared in Example 1, add 20 μL of HauCl 4 (1mg / mL), adjust and maintain the pH value at 7.4, stir for 15min, then add 20μL of hydroxylamine (50wt%), and continue stirring for 15min to obtain.

[0094] The particle size of the nano-micelle loaded with nano-gold was measured by a dynamic light scattering system, and its shape was determined by observation with a transmission electron microscope. The test results are shown in image 3 and Figure 7 . It can be seen from the dynamic light scattering parabola diagram that the average particle size of nano-gold modified micelles is 103.6nm.

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Abstract

The invention discloses a nanometer micelle capable of intelligently releasing medicine as well as a preparation method and an application thereof. The nanometer micelle provided by the invention comprises the components of polyethylene glycol-poly (aspartate-cysteine)-poly (aspartate-diisopropyl ethanediamine). The preparation method comprises the following steps of: firstly, synthesizing PEG-PBLA-N3 and PA-PAsp (DIP); then, taking cuprous bromide / pentamethyldiethylenetriamine as a catalyst system, and synthesizing PEG-PBLA-PAsp (DIP) through a click reaction of PEG-PBLA-N3 and PA-PAsp (DIP); and finally, carrying out an aminolysis reaction on 2-aminoethyl mercaptan to obtain the final polymer PEG-PAsp (MEA)-PAsp (DIP). The nanometer micelle provided by the invention can be used as a hydrophobic medicine carrier. The nanometer micelle is sensitive to pH value, the disulfide bond in the intermediate cross-linking layer is sensitive to a reducing agent, and the nanometer micelle has the characteristic of intelligently releasing medicine.

Description

technical field [0001] The invention belongs to the fields of macromolecule chemistry and biomedical engineering, and in particular relates to a novel drug carrier material—nano micelles capable of intelligently releasing drugs, as well as its preparation method and application. Background technique [0002] Cancer is one of the most important diseases that endanger human health. According to the data released by the International Union Against Cancer, in 2008, 12.7 million people worldwide suffered from cancer and 7.6 million died. If effective measures are not taken, it is estimated that by 2030, there will be 26 million new cancer cases and 17 million cancer deaths every year. Whether in the world or in China, cancer has become the first cause of death for human beings. Therefore, the development of effective cancer treatment methods is of great significance to the promotion of people's health. [0003] Anticancer drugs Chemotherapy is the most important cancer treatme...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00C08G69/48C08G69/40A61K47/34A61K9/14A61K45/00A61P35/00
Inventor 帅心涛戴箭林树东
Owner SUN YAT SEN UNIV
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