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Preparation method for nucleic acid nano-particle wrapping pharmacological active substances

A nucleic acid nanoparticle and pharmacologically active technology, applied in drug combinations, pharmaceutical formulations, organic active ingredients, etc., can solve problems such as targeting limitations, achieve the effects of small medication volume, short medication time, and improved cost efficiency

Active Publication Date: 2012-01-11
南京从一医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these methods partially achieve the targeting of drugs, these technologies are based on the surface modification of nucleic acids on polymer materials, so they will bring certain immunogenicity
In addition, the nucleic acids used here are usually fragments of tens of bases, and their targeting has certain limitations.
At the same time, since the three-dimensional structure of the nucleic acid aptamer has a gap of tens or even hundreds of times compared with the size of the nanoparticle, when using the nucleic acid aptamer to guide the nanoparticle to the target site, its limitations are also obvious

Method used

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  • Preparation method for nucleic acid nano-particle wrapping pharmacological active substances
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  • Preparation method for nucleic acid nano-particle wrapping pharmacological active substances

Examples

Experimental program
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Effect test

Embodiment 1

[0042] Example 1. Circular DNA Primer Synthesis

[0043] Mix 5 μl of water, 1 μl of 10x reaction buffer, 0.5 μl of 1 mM ATP, 0.5 μl of 50 mM MnCl2, 2.5 μl of 100 μM linear DNA (CTCTACTACCTTCTCCCCCCCCAAAACGCAAACCCACTACCACCAAAC) and 0.5 μl of DNA cyclase ligase, react at 62°C for 2 hours, then 85°C React for 15 minutes to inactivate the cyclase enzyme. Samples were stored at -20°C.

Embodiment 2

[0044] Example 2. Rolling Circle Replication (RCA)

[0045] Mix 14.1 μl water, 2.5 μl Phi29 buffer, 2.5 μl 25 mM dNTPs, 4 μl 1% BSA, 2.5 μl 100 μM DTT, 2.5 μl 100 μM DNA template, 2.5 μl circular DNA primers and 0.25 μl 100U / μl Phi29, at 37°C The reaction was carried out for 3 hours. The RCA reaction product was detected by 1.2% agarose gel electrophoresis ( figure 1 ).

Embodiment 3

[0046] Example 3. Preparation of paclitaxel-nucleic acid nanoparticles

[0047] Take 2.5 μl of RCA reaction product, react at 80°C for two hours, add 0.6 μL of 25mM paclitaxel (dissolved in ethanol) solution after the end, mix for 2 minutes, put it into ice-water mixture, until the suspension is transparent, and the average The particle size is 50-200nm, (BIC 90plus Particle Size Analyzer). The encapsulation efficiency of paclitaxel was determined by a reversed-phase C18 column, the mobile phase was acetonitrile: water (60:40), and the detection wavelength was 227nm. HPLC analysis showed that the drug loading in this experiment was 1%.

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Abstract

The invention relates to a preparation method for nucleic acid nano-particles wrapping pharmacological active substances. According to the invention, nucleic acid spherical or spheroidic structure with a great amount of repetitive sequences is prepared by using the principle of DNA rolling circle replication, and pharmacological active substances are wrapped into the structure to form the nano-particles used for drug delivery in bodies.

Description

technical field [0001] The invention relates to a method for encapsulating nucleic acid nanoparticles of pharmacologically active substances, and belongs to the field of in vivo delivery of pharmacologically active substances and their clinical applications. Specifically, the present invention is a method of encapsulating pharmacologically active substances into nucleic acids to form nanoparticles for drug delivery in vivo. Background technique [0002] Intravenous administration can quickly and directly act on the body. In order to reduce the side effects of intravenous administration, one of the effective methods is to encapsulate pharmacologically active substances into micron or nanoscale particles. On the one hand, the intravenously injected particles can release the pharmacologically active substances slowly and prolong the half-life of the pharmacologically active substances; on the other hand, the targeting material can release the pharmacologically active substance...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/26A61K31/337A61K31/704A61P35/00
Inventor 吴锦慧陈晶王永毅
Owner 南京从一医药科技有限公司