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Taxol/DNA tetrahedral drug loading system and preparation method thereof

A paclitaxel and tetrahedron technology, applied in the paclitaxel/DNA tetrahedron drug-carrying system and its preparation field, can solve the problems of poor killing effect of cancer cells, drug resistance, difficulty of paclitaxel, etc., to improve lethality, reverse PTX resistance medicine, significant effect

Inactive Publication Date: 2017-12-22
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a paclitaxel / DNA tetrahedron drug-carrying system and its preparation method to solve the problems of existing paclitaxel insoluble in water, poor killing effect on cancer cells and drug resistance

Method used

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Experimental program
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Effect test

Embodiment 1

[0029] DNA single strands were added to TM buffer at the same concentration (1μM), TM buffer was 10mM Tris-HCl, 50mM MgCl 2 , pH=8.0. Vortex, centrifuge, mix well and place in a PCR instrument, rapidly raise the temperature to 95°C and stabilize for 10 minutes, then cool to 4°C and stabilize for 20 minutes to obtain TDNs. PTX was dissolved in DMSO to prepare a 0.8mM stock solution. Dilute the stock solution to a concentration of 60 μM PTX solution. Take 60μM PTX solution and mix with 150nM TDNs. The volume ratio of PTX solution to TDNs solution was 4:1. After incubating at room temperature for 20 h under low-speed vibration at 400 rpm / min, centrifuge at 10,000 rpm / min for 10 min, discard the supernatant, dissolve the precipitate in ultrapure water, and store at 4°C.

Embodiment 2

[0031] DNA single strands were added to TM buffer at the same concentration (1μM), TM buffer was 10mM Tris-HCl, 50mM MgCl 2 , pH=8.0. Vortex, centrifuge, mix well and place in a PCR instrument, rapidly raise the temperature to 95°C and stabilize for 10 minutes, then cool to 4°C and stabilize for 20 minutes to obtain TDNs. PTX was dissolved in DMSO to prepare 1 mM stock solution. Dilute the stock solution to a concentration of 80 μM PTX solution. Take 80μM PTX solution and mix with 180nM TDNs. The volume ratio of PTX solution to TDNs solution was 9:2. After incubating at room temperature for 21 h under low-speed vibration at 300 rpm / min, centrifuge at 9000 rpm / min for 12 min, discard the supernatant, dissolve the precipitate in ultrapure water, and store at 4°C.

Embodiment 3

[0033] DNA single strands were added to TM buffer at the same concentration (1μM), TM buffer was 10mM Tris-HCl, 50mM MgCl 2 , pH=8.0. Vortex, centrifuge, mix well and place in a PCR instrument, rapidly raise the temperature to 95°C and stabilize for 10 minutes, then cool to 4°C and stabilize for 20 minutes to obtain TDNs. PTX was dissolved in DMSO to prepare a 1.2mM stock solution. Dilute the stock solution to a concentration of 100 μM PTX solution. Take 100μM PTX solution and mix with 250nM TDNs. The volume ratio of PTX solution to TDNs solution was 10:3. After incubating at room temperature for 19 h under low-speed vibration at 420 rpm / min, centrifuge at 11,000 rpm / min for 8 min, discard the supernatant, dissolve the precipitate in ultrapure water, and store at 4°C.

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Abstract

The invention discloses a preparation method of a taxol / DNA tetrahedral drug loading system and belongs to the field of biological drugs. The preparation method includes: mixing a taxol solution with a DNA tetrahedral solution, hatching, then centrifuging, and removing supernate to obtain the taxol / DNA tetrahedral drug loading system. The preparation method has the advantages that the water solubility of PTX is increased, the anaphylactic reaction of an existing PTX solvent which is the mixture of polyoxyethylated castor oil and anhydrous ethanol, lethal dose of 50% is lowered, the resource limitation problem is relieved effectively, the drug tolerance of the PTX can be reversed, and lethality to drug-tolerant tumors is increased.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a paclitaxel / DNA tetrahedron drug-carrying system and a preparation method thereof. Background technique [0002] Paclitaxel (abbreviated as PTX) is currently the only antineoplastic drug that can promote microtubule polymerization and stabilize the polymerized microtubules. After tumor cells are exposed to paclitaxel, a large number of microtubules will accumulate in the cells. The accumulation of these microtubules interferes with various functions of the cells, especially stopping cell division at the mitotic stage, thus blocking the normal division of cells. [0003] PTX has been widely used since its discovery, but the application of PTX faces three major problems at present: one, insoluble in water, the solvent of paclitaxel used clinically now is the mixture of polyoxyethylene castor oil and dehydrated alcohol, and Polyoxyethylene castor oil may cause severe allergic ...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K31/337A61P35/00
CPCA61K31/337
Inventor 林云锋谢雪萍蔡潇潇邵晓茹马文娟
Owner SICHUAN UNIV
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