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Preparation method of nano delivery system between targeted redox-sensitive co-load chemotherapeutic drugs and P-gp resistance reversal agents

A chemotherapeutic drug and drug resistance reversal technology, which is applied in drug delivery, pharmaceutical formulation, drug combination, etc., can solve the problems of restricting the application of anti-tumor drugs, poor water solubility of anti-tumor drugs, and large adverse reactions, so as to reduce cytotoxicity and avoid adverse reactions. Effects of stability, improved active targeting, and good biocompatibility

Active Publication Date: 2018-10-09
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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AI Technical Summary

Problems solved by technology

[0002] Chemotherapy is currently the most important means of clinical treatment of tumors. Due to the poor water solubility, large adverse reactions and poor selectivity of most anti-tumor drugs, the clinical application of anti-tumor drugs is seriously restricted.
In addition, a major problem in cancer treatment is the development of drug resistance in patients' tumor tissue

Method used

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  • Preparation method of nano delivery system between targeted redox-sensitive co-load chemotherapeutic drugs and P-gp resistance reversal agents
  • Preparation method of nano delivery system between targeted redox-sensitive co-load chemotherapeutic drugs and P-gp resistance reversal agents
  • Preparation method of nano delivery system between targeted redox-sensitive co-load chemotherapeutic drugs and P-gp resistance reversal agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] A method for preparing blank reduction-sensitive polymer vesicles (Blank PS), comprising the following steps:

[0048] (1) Add 25 mg PCL 7500 -ss-PEG 7500 -ss-PCL 7500 (PCL 7500 -ss-PEG 7500 -ss-PCL 7500 , see the applicant’s application on the same day for the preparation method, titled: folic acid targeted reduction-sensitive drug-loaded polymer nanomicelles and its preparation method and application) fully dissolved in methylene chloride (or a mixed organic solvent of methanol and methylene chloride) , remove the organic solvent with a rotary evaporator to form a uniform film on the inner wall of the eggplant-shaped bottle, dry the residual methylene chloride with nitrogen, put it in a vacuum drying oven, and dry it in vacuum at room temperature for 12 hours;

[0049] (2) Add 5 mL of pH7.4 phosphate buffered saline solution (PBS) to the eggplant-shaped bottle, shake to disperse the film in the solution, hydrate at 65°C for 5 h, mix well, place at room temperatur...

Embodiment 2

[0051] A method for preparing reduction-sensitive doxorubicin and paclitaxel-loaded polymer vesicles (Co-PS), comprising the following steps:

[0052] (1) Fully dissolve the amphiphilic copolymer PCL-ss-PEG-ss-PCL (25 mg) and 2.5 mg paclitaxel in dichloromethane (or a mixed organic solvent of methanol and dichloromethane), and use a rotary evaporator Remove the organic solvent to form a uniform film on the inner wall of the eggplant-shaped bottle, and dry it in vacuum for 12 hours;

[0053] (2) Prepare 300 mM ammonium sulfate aqueous solution, disperse the sample film in 5ml ammonium sulfate solution, and hydrate at 65°C for 5 h. Mix well, place at room temperature, and sonicate for 30 min in an ice bath (5 mm probe, Ampl 30%) to obtain a stable and uniform dispersion of drug-loaded reduction-sensitive polymersomes;

[0054] (3) After the polymersome suspension was placed in a treated dialysis bag (MWCO8000-14000 Da), it was dialyzed in a sucrose solution (102.69 g sucrose + ...

Embodiment 3

[0062] A preparation method of reduction-sensitive polymersomes loaded with Tariquidar, paclitaxel and doxorubicin (TQR-Co-PS). Including the following steps:

[0063] (1) When TQR-Co-PS was prepared, 5% (wt) TQR was added during rotary evaporation in step (1) of Example 2. TQR-Co-PS was prepared according to the same steps as (1), (2), (3), (4) and (5) of Example 2.

[0064] (2) Encapsulation efficiency of TQR-Co-PS

[0065] The prepared polymersome suspension was centrifuged at 23,000 rpm for 3 times, each time for 30 min, and washed with deionized water to remove unencapsulated drug. Finally, the precipitate was resuspended with 5 mL of water and freeze-dried. Weigh a certain amount of freeze-dried powder, dissolve it in DMSO, detect its absorbance at 480 nm with an ultraviolet spectrophotometer (UV), and quantify the concentration of doxorubicin in combination with the UV absorption standard curve at 480 nm of the doxorubicin-DMSO solution. drug content. In addition, w...

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Abstract

The invention relates to a preparation method of a nano delivery system between targeted redox-sensitive co-load chemotherapeutic drugs and P-gp resistance reversal agents. The redox-sensitive amphiphilic copolymers PCL7500-ss-PEG7500-ss-PCL7500 is utilized to build redox-sensitive polymer vesicle, intermolecular hydrophobic force is used to load hydrophobic taxol and Tarigquidar, adriamycin is loaded inside the hydrophilic chamber of the polymer vesicle via pH gradient method, folate targeting group is decorated on the surface of the polymer vesicle via covalent bond, thereby the polymer vesicle with synergistic activity with targeting, reduction and response and chemotherapy is built. P-glycoprotein(P-gp) of small molecules inhibitor Tariguidar reduces the drug resistance of drug resistance cells by blocking the efflux function of P-gp to the base drug, the picking up of drugs of drug resistance cells is increased, thereby the multiple drug resistance is reversed. The nano delivery system is capable of loading hydrophobic drugs and hydrophilic drugs, tumor targeting and having reducing and response to the tumor micro environment and realizing killing tumors by reserving the multiple drug resistance.

Description

technical field [0001] The invention relates to a preparation method of a nano-delivery system for targeted reduction sensitive co-loading chemotherapeutic drugs and P-gp drug resistance reversing agent, in particular to a targeted reduction sensitive polymer loaded with chemotherapeutic drugs and P-gp drug resistance reversing agent Preparation method of vesicle nano-delivery system. The nano-delivery carrier of the present invention can carry hydrophobic chemotherapeutic drugs and hydrophilic chemotherapeutic drugs at the same time, has tumor targeting and has reduction responsiveness to the tumor microenvironment, can realize the reversal of multidrug resistance of tumors and pass different chemotherapeutic drugs Synergistically kill tumors. Background technique [0002] Chemotherapy is currently the most important means of treating tumors clinically. Due to the poor water solubility, large adverse reactions and poor selectivity of most antineoplastic drugs, the clinical...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K45/06A61K31/4725A61P35/00
CPCA61K31/337A61K31/4725A61K31/704A61K45/06A61K47/54A61K47/6915A61P35/00A61K2300/00
Inventor 张琳华朱敦皖秦玉樊帆张志明
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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