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HPMA-polymer-modified-gold-nanorod medicine-carrying system and production method and application thereof

A gold nanorod, drug-carrying system technology, applied in pharmaceutical formulations, urinary system diseases, medical preparations with inactive ingredients, etc. The effect of increasing lethality

Active Publication Date: 2020-06-05
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to overcome the deficiencies in the prior art, one of the objectives of the present invention is to provide a gold nanorod drug-loading system modified by HPMA polymers, using water-soluble HPMA polymers to assemble chemotherapeutic drugs into GNRs, and to cooperate with hyperthermia and chemotherapy to solve the problem. Drug resistance of cells during prostate cancer treatment

Method used

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  • HPMA-polymer-modified-gold-nanorod medicine-carrying system and production method and application thereof
  • HPMA-polymer-modified-gold-nanorod medicine-carrying system and production method and application thereof
  • HPMA-polymer-modified-gold-nanorod medicine-carrying system and production method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0037] Preparation of CTAB-GNRs:

[0038](1) Preparation of seed solution: Add 5 mL, 0.0005 mol / L chloroauric acid solution to 5 mL, 0.2 mol / L cetyltrimethylammonium bromide (CTAB) solution in a water bath at 26 °C, and stir evenly Finally, 600 μL, 0.01mol / L ice-cold sodium borohydride solution was quickly added, the reaction solution changed from yellow to brown rapidly, stirred vigorously for 2 minutes, and stood at 26°C in the dark for 20 to 30 minutes.

[0039] (2) Preparation of growth solution: Add 200 μL, 0.004 mol / L silver nitrate (AgNO3) solution, 5 mL, 0.001 mol / L chloroauric acid solution to 5 mL, 0.2 mol / L CTAB solution in a water bath at 26 ° C, and stir Evenly, add 70 μL, 0.0788mol / L AA solution under slow stirring, the reaction solution changes from dark yellow to colorless quickly, quickly add 80 μL of the above seed solution, stir vigorously for 2 minutes, and stand overnight at 26°C in the dark to obtain CTAB-GNRs .

Embodiment 2

[0041] To prepare PDS-pHPMA-DOX, the synthetic route is as follows figure 1 As shown, the specific operation steps are as follows:

[0042] (1) Preparation of MA-GG-OH: Mix 8.71ml (0.091mol) of MA-Cl with 30ml of dichloromethane, dissolve 9.79g (0.075mmol) of GG-OH in 20ml of 4M sodium hydroxide solution, and store at -15°C Slowly drop the MA-Cl solution in dichloromethane into the GG-OH-containing sodium hydroxide solution while stirring, and at the same time drop into the 1M sodium hydroxide solution to adjust the pH to 9-10, and stir at room temperature for 1.5 h. After the dichloromethane layer was separated, it was washed with 20 ml of water, the aqueous layers were combined, and the pH was adjusted to 1-2 with 6M aqueous hydrochloric acid. The precipitate was recrystallized with 50% ethanol aqueous solution to obtain 6.44 g of white crystal MA-GG-OH, with a yield of 71.46%, M.p.136-138°C; MS: C 8 h 12 N 2 o 4 , 201.1 (M + ).

[0043] (2) Preparation of MA-GG-NHNH ...

Embodiment 3

[0048] To prepare pHPMA-DOX@GNRs, the synthetic route is as follows figure 1 As shown, the specific operation steps are as follows:

[0049] Take 1 mL (0.60 nM) of CTAB-GNRs prepared in Example 1 and resuspend in physiological saline, slowly add 1 mL (0.90 nM) of PDS-pHPMA-DOX in Example 2 dropwise under stirring conditions, and react in the dark for 12 hours to obtain 2 mL (0.3nM) product pHPMA-DOX@GNRs.

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Abstract

The invention discloses an HPMA-polymer-modified-gold-nanorod medicine-carrying system. According to the medicine-carrying system, a pH-sensitive HPMA polymer is used as modification chains of gold nanorods, and the pH-sensitive HPMA polymer is connected with a chemotherapeutic medicine through pH-sensitive chemical bonds. According to the provided HPMA-polymer-modified-gold-nanorod medicine-carrying system, the chemotherapeutic medicine is loaded with the GNRs (gold nanorods) by means of the water-soluble HPMA polymer, and hyperthermia and chemotherapy effects have a synergistic effect on prostate cancer cells, so that killing power of the chemotherapeutic medicine is improved. A production method of the HPMA-polymer-modified-gold-nanorod medicine-carrying system is further provided. A production process is simple and easy to operate. Application of the HPMA-polymer-modified-gold-nanorod medicine-carrying system in treatment of prostate cancer is further provided. Medicine resistanceof tumor cells is effectively overcome, and occurrence and metastasis of prostate cancer are delayed.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an HPMA polymer-modified gold nanorod drug-carrying system and a preparation method and application thereof. Background technique [0002] Prostate cancer is the most common malignant tumor among men in developed countries and regions such as Europe and the United States, and its mortality rate ranks second among various cancers. In Asia, its incidence rate is lower than that in Western countries, but it has been rising rapidly in recent years. When patients with metastatic prostate cancer are diagnosed at an early stage, surgery and endocrine therapy can temporarily effectively inhibit the metastasis of soft tissue lesions and reduce the level of prostate-specific antigen in serum. However, almost all prostate cancer patients will inevitably develop into metastatic castration-resistant prostate cancer (mCRPC), which is no longer sensitive to endocrine therapy and can ...

Claims

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Application Information

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IPC IPC(8): A61K47/58A61K31/704A61K41/00A61P13/08A61P35/00
CPCA61K31/704A61K41/0052A61K47/58A61P13/08A61P35/00A61K2300/00
Inventor 杨洋张绿萍李小昊王璐李建波李娜张丽果张婧
Owner ZHENGZHOU UNIV
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