Preparation method and application of zinc organic framework drug-loading system entrapping rapamycin

A technology of rapamycin and organic framework, which is applied in the field of anti-tumor drug preparation, can solve the problems of toxic side effects, difficult tumor tissue resection, large cancer patients, etc., achieve low systemic toxicity, obvious killing and inhibiting effect, and enhance chemotherapy effect of effect

Pending Publication Date: 2020-01-17
THE FIRST AFFILIATED HOSPITAL OF ANHUI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, surgical treatment is difficult to remove all tumor tissue, and surgical treatment will become helpless for areas where tumor resection is difficult or non-solid tumors
Chemoradiation and chemotherapy usually have a large dose, which will cause greater toxic and side effects on normal cells, and may eventually cause greater toxic and side effects in cancer patients

Method used

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  • Preparation method and application of zinc organic framework drug-loading system entrapping rapamycin
  • Preparation method and application of zinc organic framework drug-loading system entrapping rapamycin
  • Preparation method and application of zinc organic framework drug-loading system entrapping rapamycin

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Experimental program
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Effect test

Embodiment 1

[0044] A method for preparing a zinc organic framework drug-loading system loaded with rapamycin, the specific preparation method comprising the following steps:

[0045] Step 1: dissolving zinc nitrate in methanol, adding rapamycin to the zinc nitrate hexahydrate solution;

[0046] Step 2: After mixing and stirring for 5 minutes, add 2-methylimidazole solution dropwise, and then stir for 15 minutes, and collect by centrifugation at a stirring rate of 1500 rpm, and continue stirring during the dropping process;

[0047] Step 3: wash three times with a mixture of H2O and methanol, and then vacuum-dry to obtain solid nanoparticles of zinc organic framework drug-loading system loaded with rapamycin, that is, Rapa@ZIF-8 NPs, and vacuum-dry at room temperature Carry out vacuum drying for 1 h.

[0048] The entrapment efficiency and encapsulation efficiency of the Rapa@ZIF-8 NPs were 9.39% and 58.2%, respectively.

[0049] The amounts of materials taken during the preparation proce...

Embodiment 2

[0051] The present invention also provides an application of a zinc organic framework drug-carrying system carrying rapamycin. A zinc organic framework drug-carrying system carrying rapamycin is prepared by the method prepared in Example 1, Namely Rapa@ZIF-8.

[0052] The application of the organic framework drug delivery system, the zinc organic framework drug delivery system containing rapamycin has a zinc organic framework drug delivery system released from the tumor microenvironment.

[0053] Zinc organic framework drug-loading system containing rapamycin is uniformly dispersed in water under ultrasonic conditions to prepare intravenous injection preparations, used alone or in combination with doxorubicin for the treatment or alleviation of cancer in a certain tissue or organ, cancer includes but not Limited to leukemia and solid tumors.

Embodiment 3

[0055] Refer to the attached Figure 1-8 Shown:

[0056]In the preparation process of the zinc organic framework drug-loading system encapsulating rapamycin, Rapa@ZIF-8 nanoparticles (NPs) were prepared, and ZIF-8 nanoparticles were synthesized by a similar method; using electron microscopy ( TEM) characterized the morphology and size of Rapa@ZIF-8 and ZIF-8, and found that these two nanoparticles have very similar size and shape, both of which are composed of uniform rhombic dodecahedra with a size of less than 100nm;

[0057] Then the Zeta potential of Rapa@ZIF-8NPs and ZIF-8NPs was measured, and the surface Zeta potentials of Rapa@ZIF-8NPs and ZIF-8NPs were 18.4mV and 17.6mV, respectively;

[0058] The hydrated particle size (DLS) measurement of Rapa@ZIF-8NPs and ZIF-8NPs, the average particle size measured by Rapa@ZIF-8NPs and ZIF-8NPs is about 137.5nm and 138.6nm;

[0059] Rapa@ZIF-8NPs and ZIF-8NPs were tested by powder X-ray diffraction (XRD). The characteristic peaks...

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Abstract

The invention belongs to the field of anti-tumor drugs, and particularly relates to a preparation method and application of a zinc organic framework drug-loading system entrapping rapamycin. A following solution is put forward currently, specifically, the preparation method comprises the following steps: 1, zinc nitrate is dissolved in methanol, and the rapamycin is added into a zinc nitrate hexahydrate solution; 2, after mixing and stirring for 5 min, a 2-methylimidazole solution is dropwise added, then stirring is conducted for 15 min, and centrifuging for collection is conducted; and 3, washing is conducted with a mixture of H2O and methanol for three times, and after washing, solid nanoparticles are obtained through vacuum drying. The rapamycin is taken as a raw material to prepare thezinc organic framework drug-loading system entrapping the rapamycin, the zinc organic framework drug-loading system can be uniformly dispersed in water under the ultrasonic condition to prepare an intravenous injection preparation, the reagent can cooperatively conduct autophagy induction and inhibit an mTOR signal pathway to enable MCF-7 / ADR to restore sensitivity to chemotherapy, cancer of certain tissue or a certain organ can be treated or relieved, and obvious killing and inhibiting effects on tumor cells are achieved.

Description

technical field [0001] The invention relates to the technical field of preparation of antitumor drugs, in particular to a preparation method and application of a zinc organic framework drug-carrying system carrying rapamycin. Background technique [0002] Cancer is an incurable disease that occurs in various groups of people, ages and different human organs due to the mutation of related genes that control the cell cycle and the accumulation of genetic instability, which seriously threatens human health and life. [0003] At present, the main means of treating cancer are: surgical operation to directly remove the tumor at the lesion, radiotherapy, chemotherapy or a combination of the above treatment means. However, surgical treatment is difficult to remove all tumor tissues, and surgical treatment will become helpless for parts where tumor resection is difficult or non-solid tumors. Chemotherapy and radiotherapy usually have a large dose, which will cause greater toxic and ...

Claims

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Application Information

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IPC IPC(8): A61K31/436A61K31/704A61K47/22A61K47/02A61P35/00
CPCA61K31/436A61K31/704A61K9/0019A61K47/22A61K47/02A61P35/00A61K2300/00
Inventor 李平徐梦冉胡翼
Owner THE FIRST AFFILIATED HOSPITAL OF ANHUI MEDICAL UNIV
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