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Composite nano-drug constructed by nanoparticles coupled with pharmaceutical ingredients as well as preparation method and application of composite nano-drug

A nanoparticle and nanomedicine technology, which can be used in drug combinations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., and can solve problems such as difficulties

Active Publication Date: 2018-08-17
郑州天兆医疗科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is still no effective way to construct a firmly combined nano-small molecule drug through chemical bonds for drugs that do not contain amine and / or carboxyl groups (such as zirol, saponins)
It is usually very difficult to chemically couple these drugs or small organic molecules without active amine or carboxyl groups to nanoparticles

Method used

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  • Composite nano-drug constructed by nanoparticles coupled with pharmaceutical ingredients as well as preparation method and application of composite nano-drug
  • Composite nano-drug constructed by nanoparticles coupled with pharmaceutical ingredients as well as preparation method and application of composite nano-drug
  • Composite nano-drug constructed by nanoparticles coupled with pharmaceutical ingredients as well as preparation method and application of composite nano-drug

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Experimental program
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Effect test

Embodiment 1

[0045] The present invention uses microfluidic technology to synthesize Fe@Fe containing hydroxyl groups on the surface 3 o 4 The nanoparticle with core-shell structure is used as a model particle, and ginsenoside is used as a model drug to illustrate the process of the invention.

[0046] (1) However, most nanoparticles can be alloyed or hybridized with elements that are easily oxidized (such as Fe, Zn, Co, Al). Because the surface atoms of nanoparticles are very active, the surface elements have sufficient oxidized characteristics, A large number of -OH groups can be generated on the surface by aqueous solution, physiological saline, PBS buffer, etc. It can be prepared as figure 1 shown, by controlling N 2 The flow rate controls the oxygen content, and then controls the generated hydroxyl groups. Please refer to 201510395518.4. Preparation of Fe@Fe with hydroxyl groups on the surface 3 o 4 Core-shell nanoparticles.

[0047] (2) They can form silicon-oxygen-metal (nano...

Embodiment 2

[0067] The ginsenoside in Example 1 was replaced by paclitaxel which also contains multiple hydroxyl groups, and the nanoparticles and paclitaxel were coupled through the same process. last drug see Figure 8 As shown, due to the change of its molecular structure during the synthesis process and the use of surfactants such as PVP, the nano-medicine has better solubility in aqueous solution. Through nanoparticle-conjugated paclitaxel, because the nanoparticle itself has the function of awakening immune cells T-cells, and paclitaxel itself has a strong inhibitory effect on cell mitosis, they have a stronger synergistic effect and promote the rapid apoptosis of tumor cells. Cell and animal experiments show that the therapeutic effect of the nano-medicine on the nuclear tissue of malignant tumors such as breast cancer, ovarian cancer, liver cancer, head and neck cancer and lung cancer is 2-5 times higher than that of paclitaxel alone. , It can greatly reduce the patient's edema, ...

Embodiment 3

[0069] The ginsenoside in Example 1 was replaced by vincristine which also contains multiple hydroxyl groups, and the nanoparticles and vincristine were conjugated by the same process. last drug see Figure 9 Shown is nanoparticle conjugated vincristine. Like nanoparticle-conjugated paclitaxel, it not only improves its therapeutic effect on acute lymphoblastic leukemia, acute myeloid leukemia, Hodgkin's lymphoma, neuroblastoma and small cell lung cancer, but also adds nanoparticles to its therapeutic effect. The side effects are greatly reduced, reducing the patient's hair loss, diarrhea, fatigue, oral pain, edema, vision and confusion.

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Abstract

The invention discloses a composite nano-drug constructed by nanoparticles coupled with pharmaceutical ingredients as well as a preparation method and an application of the composite nano-drug, and belongs to the technical field of composite drugs. The method for preparing the nano-drug comprises the following operations: modifying amino on the surfaces of nanoparticles which contain hydroxy in the surfaces, and activating biological or small-molecular drugs containing hydroxy; and then conducting a conjugate coupling reaction on the nanoparticles and the drugs, so that a plurality of chemicalbonds are constructed, combining the plurality of chemical bonds so as to prepare the nano-drug. Based upon researches, it is indicated that an anti-cancer effect can be greatly improved on the basisof a synergistic effect between active ingredients of natural drugs (such as taxol, ginsenoside and other traditional Chinese medicines) and a nano-material, and meanwhile, key and breakthrough points can be also provided for researching and producing efficient anti-cancer nano-drugs which are low or free from toxic and side effects and have targeting and autonomous targeting performances.

Description

technical field [0001] The invention belongs to the technical field of novel composite medicines, in particular to the technical fields of antineoplastic medicines and Parkinson's syndrome medicines, and relates to the coupling of nanoparticles and active ingredients of traditional Chinese medicines into a type of composite nanomedicine and a preparation method. Background technique [0002] In recent years, due to environmental changes, food safety and the gradual increase in the proportion of elderly population with high incidence of cancer and other factors, the number of patients and deaths of malignant tumors in the world and in my country has shown a trend of accelerated development. In 2010, the global malignant tumor The number of morbidity and death toll is 12.34 million and 7.7 million respectively. It is estimated that by 2050, these two figures will reach 23.83 million and 16 million. The morbidity and mortality in developing countries are significantly higher than...

Claims

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Application Information

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IPC IPC(8): A61K47/52A61K49/04A61K49/08A61K36/16A61K31/337A61K36/258A61P35/00A61P25/16A61K127/00
CPCA61K31/337A61K36/16A61K36/258A61K49/04A61K49/08A61K47/52A61P25/16A61P35/00
Inventor 宋玉军
Owner 郑州天兆医疗科技有限公司
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