Preparation method and application of ROS-sensitive and H2S donor-responsive nano-micelle

A nano-micelle and donor technology, applied in the field of medicine, to achieve good biocompatibility, lower concentration, and good ROS inhibition effect

Active Publication Date: 2021-06-29
潍坊中医药产业技术研究院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, there is no effective pharmacological approach to inhibit or reverse the progression of RIRI

Method used

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  • Preparation method and application of ROS-sensitive and H2S donor-responsive nano-micelle
  • Preparation method and application of ROS-sensitive and H2S donor-responsive nano-micelle
  • Preparation method and application of ROS-sensitive and H2S donor-responsive nano-micelle

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Experimental program
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Embodiment

[0035] This embodiment relates to a ROS sensitive and H 2 The preparation method of the s donor response type nano-micelle includes the following steps:

[0036] 1) Synthesis of hyaluronic acid - thirylene - paffle benzene urea (HATM) material: see figure 1 with figure 2 Down:

[0037] EDC 114 mg, DMAP 43.5 mg and TKL 67.2 mg were weed, dissolved in 2 ml of formamide, and dissolved. After dissolving, it was placed in a magnetic stirrer in a magnetic stirrer in a 30-40 ° C for 1-2 h, and the catalytic period was noted. After the completion of the catalysis, HA62.8 mg was weighed, dissolved in 5 ml of formamide, and heat it soled. The HA solution was dripped into TKL catalytic solution, and the magnetic force was stirred at 40-50 ° C for 24 h to give the reaction solution 1;

[0038] MPT 54 mg, HOBT 81 mg, EDC 114 mg, dissolved in a 2 ml DMF solution, and the ultrasound is dissolved. The dissolution was completed in a 30-40 ° C magnetic stirrer for 1-2 h to obtain a reaction solutio...

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Abstract

The invention provides a preparation method and application of an ROS-sensitive and H2S donor-responsive nano-micelle. The preparation method comprises the following steps that step 1, a reaction solution 1 is prepared, a reaction solution 2 is prepared, and the reaction solution 2 is dropwise added into the reaction solution 1 to obtain a reaction solution 3; step 2, impurities are removed through a dialysis method, and an HATM freeze-dried product is obtained through freeze-drying; and step 3, the HATM freeze-dried product and rapamycin are weighed, the HATM freeze-dried product and the rapamycin are dissolved in DMF, HATM@RAP is formed in a self-assembly mode, and non-entrapped free drugs are removed. According to the preparation method of the ROS-sensitive and H2S donor-responsive nano-micelle, hyaluronic acid is specifically combined with a CD44 receptor on the surface of the macrophage, so that the drug is gathered at the renal ischemia reperfusion injury part, and the targeting effect is realized; a ROS sensitive group is introduced, so that when a novel drug delivery system reaches a part with higher ROS concentration, the drug can be quickly released, and the effect of quick treatment is realized; and by introducing an H2S donor, H2S can be slowly released at the kidney part, and finally, the effects of preventing inflammatory injury and promoting renal ischemia reperfusion protection are achieved.

Description

Technical field [0001] The present invention relates to the field of medicine; in particular, there is a ROS sensitive and H 2 Preparation method and application of s donor response type nanocarchers. Background technique [0002] Renal ischemia-reperfusion injury (Riri) is one of the main reasons for acute kidney injury, common in various clinical events including cardiac surgery, kidney transplantation, cardiopulmonary recovery, shock, sepsis, and the like. Now the treatment is mainly to delay the progress of kidney disease, and there is no extractional drug. When ischemia-reperfusion injury in the kidney, ROS can cause oxidative stress and cause serious damage to the kidney. Macrophages play an important role in the occurrence and development of renal injury. Hide 2 S has the effect of preventing inflammation and leukocyte adhesion, resisting oxidative stress and renal ischemia-reperfusion injury. Nowadays, the method of treating Riri is mainly to delay the progress of kidney ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/61A61K31/17A61P13/12
CPCA61K9/1075A61K47/61A61K31/17A61P13/12
Inventor 陈大全周绣棣郭春静陈强李毅刘雪于彩薇苏彦国郭慧敏
Owner 潍坊中医药产业技术研究院
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