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Targeting polymer micelle containing acid-sensitive subsurface, and preparation method thereof

A polymer glue and polymer technology, applied in the fields of pharmacy, biomedical engineering, and chemistry, can solve the problems that fluorescent organic dye molecules are prone to photobleaching and cannot effectively overcome the masking, and achieve the effect of real-time monitoring of fluorescence imaging

Inactive Publication Date: 2012-05-09
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There are two major difficulties in the development and research of fluorescence imaging technology and fluorescent probes: one is that the autofluorescence of cells in the visible light region cannot effectively cover the signals sent by labeled molecules; the other is that fluorescent organic dye molecules are prone to photobleaching and cannot Better realization of long-term fluorescent labeling observation of research molecules

Method used

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  • Targeting polymer micelle containing acid-sensitive subsurface, and preparation method thereof
  • Targeting polymer micelle containing acid-sensitive subsurface, and preparation method thereof
  • Targeting polymer micelle containing acid-sensitive subsurface, and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027]Synthesis of Folic Acid Modified Triblock Copolymer FA-PEG-P(Asp-dip)-CA with Acid Sensitive Middle Block

[0028] (1) Synthesis of polyethylene glycol (Allyl-PEG-OH) with an allyl group at one end and a hydroxyl group at the other end

[0029] A solution of potassium naphthyl (4 mL) in tetrahydrofuran and allyl alcohol (0.75 mL) was mixed evenly and stirred in a dry reaction flask for 15 minutes. Then under the protection of argon, anhydrous tetrahydrofuran (20 mL) and 18-crown-6 tetrahydrofuran solution (containing 1.5 g 18-crown-6 and 5 mL anhydrous tetrahydrofuran) were added, stirred for 15 minutes, and the mixture was placed in Cool in an ice-salt bath, slowly pass through dry ethylene oxide, keep the low temperature for 24 hours to keep the polymerization reaction going, and continue the reaction at room temperature for 72 hours.

[0030] (2) Polyethylene glycol with an allyl group at one end and an amino group at the other end (Allyl-PEG-NH 2 )Synthesis

[003...

Embodiment 2

[0046] Preparation of targeted polymeric micelles with acid-sensitive subsurface

[0047] (1) Sample preparation of loaded QD micelles: a mixture of FA-PEG-P(Asp-dip)-CA (2.0 mg) and PEG-P(Asp-dip)-CA (8.0 mg) was dissolved in tetrahydrofuran (THF, 1.0 mL), added dropwise into PBS (10 mL, pH=5.0) under ultrasonic conditions, stirred overnight, THF was naturally volatilized, filtered with a filter membrane with a pore size of 0.22 μm, and then added negative electron dots CdSe / ZnS (100 μL, 8 μmoL / L), mix well and rest for 30 minutes, adjust the pH to 7.4, and centrifuge at 6000r / min to remove unloaded quantum dots.

[0048] (2) Sample preparation of loaded QDs and paclitaxel micelles: a mixture of FA-PEG-P(Asp-dip)-CA (2.0 mg) and PEG-P(Asp-dip)-CA (8.0 mg) was mixed with PTX (1.0 mg) was dissolved in tetrahydrofuran (THF, 1.0 mL), added dropwise into PBS (10 mL, pH=5.0) under ultrasonication, stirred overnight, THF was naturally volatilized, and PTX was filtered through a fil...

Embodiment 4

[0053] In vitro drug release test of targeted polymeric micelles with acid-sensitive subsurface (take paclitaxel-loaded micelles as an example)

[0054] The in vitro release experiment of paclitaxel was done by dialysis. The newly prepared paclitaxel-loaded PEG-P(Asp-dip)-CA micelles were divided into two parts, one part maintained its pH value at 5.0, and the other part was adjusted to 7.4. The samples at each pH value were divided into three (parallel experiments) and loaded into dialysis bags with a molecular weight cut-off of 14,000 Da, and the dialysis bags were placed in 100 mL of PBS buffer with the same pH value. Placed in a shaker at 37°C at a speed of 75 r / min, samples were taken at set time points, and then the same volume of fresh buffer solution was added. The concentration of the sample was detected by HPLC, and the cumulative release at different time points was calculated. The chromatographic column model used in HPLC is Ultimate from Welch Materials Company ...

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Abstract

The invention relates to a targeting polymer micelle containing acid-sensitive subsurface, and a preparation method thereof. The polymer micelle is in a core-shell structure. Targeting ligand molecules are grafted on a hydrophilic segment terminal of the shell, and a hydrophobic anti-tumor medicine is loaded by a hydrophobic segment of the core. An acid-sensitive response subsurface exists between the core and the shell, wherein the acid-sensitive response subsurface can load negative electricity quantum dots. When a pH value is 5.0, the acid-sensitive layer is hydrophobic; when the pH value is 7.4, the acid-sensitive layer is hydrophobic. According to the invention, with the targeting molecules, the tumor targeting function of the micelle is realized; with the quantum dots loaded on the acid-sensitive subsurface, a visualizing function is realized; with low-pH-responsibility of the acid-sensitive subsurface, a controlled-release function can be realized, and the release of the medicine can be controlled. With the micelle system provided by the invention, the release behavior of the medicine is improved, and a premature-release problem of the micelle system in blood circulation ispossible to be solved. With an internalization behavior mediated by the targeting molecules, the treatment effect of the medicine is enhanced. With the loaded quantum dots, monitoring during the treatment process can be realized.

Description

[0001] technical field [0002] The invention relates to the fields of chemistry, pharmacy and biomedical engineering, in particular to the preparation of a targeting polymer micelle with an acid-sensitive subsurface layer and its application in drug controlled release and imaging. Background technique [0003] Tumors are a serious threat to human health, and the mortality rate remains high. There are three main approaches to cancer treatment: surgery, radiation therapy, and chemotherapeutic drugs (chemotherapy). The first two are localized treatments, and chemotherapy is usually given when the tumor has spread and metastasized. Most of the chemotherapeutic drugs commonly used in clinic are hydrophobic drugs, and their solubility in water is very low, which limits their application. In clinical use, small molecule surfactants are often used to emulsify and solubilize hydrophobic chemotherapy drugs, but the blood stability of this dosage form is very poor, the added excipien...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/34A61K45/00A61K49/00A61P35/00A61K47/22
Inventor 帅心涛王伟伟程度巩发明
Owner SUN YAT SEN UNIV
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