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A folic acid targeting carrier loaded with anticancer drugs and its preparation method and application

An anti-cancer drug, folic acid targeting technology, applied in the field of medicine, can solve the problems of energy supply and inability, and achieve the effects of enhancing toxicity, reducing toxicity and reducing organ toxicity

Active Publication Date: 2021-05-04
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chloroquine inhibits lysosomal activity, which in turn prevents the last step of autophagy, the degradation of autolysosomes, resulting in the inability to provide energy through the autophagic pathway

Method used

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  • A folic acid targeting carrier loaded with anticancer drugs and its preparation method and application
  • A folic acid targeting carrier loaded with anticancer drugs and its preparation method and application
  • A folic acid targeting carrier loaded with anticancer drugs and its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Example 1 Preparation of folic acid targeting carrier loaded with anticancer drug chloroquine phosphate

[0039] 1. Preparation of Chloroquine Phosphate-Zeolite Imidazole Skeleton Carrier (CQ-ZIF-8)

[0040]The anticancer drug chloroquine phosphate was encapsulated in the zeolite imidazole framework by in situ embedding method, and the chloroquine phosphate-zeolite imidazole framework carrier (CQ-ZIF-8) was synthesized. The specific reaction was as follows:

[0041] (1) Dissolve 50mg of chloroquine phosphate in 5ml of deionized water, mix with zinc nitrate, stir at room temperature for 1min, and use the zinc ions of zinc nitrate and anticancer drugs to form a coordination compound;

[0042] (2) Add 8ml of anhydrous methanol and 4g of 2-methylimidazole, and continue to stir at room temperature for 15min, 2-methylimidazole and the zinc ion of the coordination compound form ZIF-8;

[0043] (3) Centrifuge at a speed of 10000rmp / min for 10min, then wash with anhydrous metha...

Embodiment 2

[0049] The characterization of embodiment 2 carrier FA-PEG / CQ-ZIF-8

[0050] 1. The standard curve of chloroquine phosphate is attached figure 1 shown

[0051] Measure the chloroquine phosphate solution absorbance value of different concentrations at 257nm by ultraviolet spectrophotometry, thus draw figure 1 the standard curve, figure 1 R 2 = 0.9988 reached above 0.99 level, so this standard can be used. However, the range used for the standard curve is 10-40 μg / ml.

[0052] 2. Infrared spectrum detection

[0053] (1) Dry FA-PEG, CQ, ZIF-8, FA-PEG / CQ-ZIF-8, then put them into a mortar, add a certain amount (how much) of KBr, and grind the mixture evenly to The particle size is less than 2 μm, so as not to be affected by scattered light, and then placed in a dryer for drying treatment, and the mixture is pressed into a transparent sheet with a pressure of about 40 MPa on a hydraulic press, and measured on the machine;

[0054] (2) Infrared spectrum (FTIR) as attached F...

Embodiment 3

[0057] The CQ loading rate of ZIF-8 load in the carrier FA-PEG / CQ-ZIF-8 of embodiment 3

[0058] 1. Determination of the CQ loading rate of ZIF-8 loading

[0059] Ultraviolet spectrophotometer detection: consult the literature and know that the characteristic absorption peak of chloroquine phosphate is 254nm

[0060] (1) The specific steps for drawing the standard curve of chloroquine phosphate are as follows:

[0061] ① Preparation of curcumin stock solution

[0062] Accurately weigh 1mg of chloroquine phosphate and place it in a beaker, add an appropriate amount of deionized water to dissolve it, transfer it to a 10mL volumetric flask, and then dilute to the mark with deionized water, and use it as a chloroquine phosphate stock solution for later use;

[0063] ② Measure 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, and 4.0 mL from the stock solution and place them in seven 10 mL volumetric flasks, dilute to the mark with deionized water, and shake well. Using deionized water as the blank...

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Abstract

The invention discloses a folic acid targeting carrier loaded with anticancer drugs, a preparation method and application thereof. It first uses zinc nitrate and 2-methylimidazole as carrier materials, encapsulates the anticancer drug in the carrier through the original flavor embedding method, and synthesizes the anticancer drug-zeolite imidazole skeleton carrier; then through the anticancer drug-zeolite imidazole skeleton carrier The zinc ions in the compound form a coordination bond with folic acid-polyethylene glycol to connect folic acid, and the folic acid targeting carrier loaded with anticancer drugs is successfully prepared. The targeting drug carrier has good biocompatibility, simple synthesis method, targeting property, and can reduce drug toxicity and side effects. At the same time, the drug loading capacity of chloroquine phosphate in the carrier is as high as 18%, which improves the utilization rate and efficacy of the drug.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a folic acid targeting carrier loaded with anticancer drugs and its preparation method and application. Background technique [0002] The harm of cancer is increasing worldwide, and it has become the number one "killer" that threatens human health. At present, the most commonly used treatment methods in clinical practice are surgery, chemotherapy and radiotherapy. Chemotherapy causes a range of acute and chronic organ toxicities. Since many chemotherapeutic drugs and their metabolites are excreted by renal tubular epithelial cells, the kidney is vulnerable to chemotherapeutic drug damage. Therefore, the use of chemotherapy drugs is sometimes limited by their nephrotoxic side effects. Chemotherapy-associated kidney injury often leads to undertreatment of cancer because renal dysfunction requires clinicians to reduce chemotherapy doses to avoid further kidney injury...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/60A61K47/54A61K31/4706A61P35/00
CPCA61K31/4706
Inventor 雷群芳方文军郭永胜施浙琪陈雪瑞张莉
Owner ZHEJIANG UNIV