Synthesis method and application of miRNA-carrying VB12 binding type nano-composite

A technology of nanocomposites and synthesis methods, which is applied in the field of synthesis of nanomedicines, can solve problems such as poor stability of VB12, and achieve the effects of convenient operation, low toxicity and anti-tumor effect, and good stability

Active Publication Date: 2020-07-31
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, VB12 has poor stability and is sensitive to light and heat. How to couple VB12 to nanocarriers under mild reaction conditions is a challenging task.

Method used

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  • Synthesis method and application of miRNA-carrying VB12 binding type nano-composite
  • Synthesis method and application of miRNA-carrying VB12 binding type nano-composite
  • Synthesis method and application of miRNA-carrying VB12 binding type nano-composite

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preparation example Construction

[0040] In some examples, the synthesis method of the PLGA-PEG nanocarrier comprises:

[0041] 1) Mix PLGA, NHS and EDC in anhydrous solvent B, activate, and after full reaction, wash with anhydrous solvent C to remove unreacted small molecules, and dry to obtain PLGA-NHS pellets;

[0042] 2) Dissolve PLGA-NHS pellets in anhydrous solvent D, add bifunctional modified NH 2 - PEG-COOH and diisopropylethylamine, continuous reaction for 24 hours;

[0043] 3) After the reaction is finished, wash with anhydrous solvent C, and finally vacuum-dry to obtain the PLGA-PEG nanocarrier.

[0044] In some embodiments, a method for synthesizing vitamin B12-binding nanocarriers includes:

[0045] 1) Mixing and dissolving PLGA-PEG nanocarriers, vitamin B12, EDC and DMAP in anhydrous solvent A, stirring and reacting at 15-40°C;

[0046]2) After the reaction is completed, dialyze and remove the solvent to obtain a vitamin B12-binding nanocarrier, which is denoted as VB12-PLGA-PEG nanocarrier. ...

Embodiment 1

[0077] Example 1: Synthesis and physical and chemical characterization of miR-532-3p@PLGA-PEG-VB12 nanocomposite

[0078] (1). Material synthesis:

[0079] 1) Synthesis of PLGA-PEG-COOH derivatives: First, 250 mg of PLGA solution was mixed with NHS and EDC in dry dichloromethane (CH 2 Cl 2 ) conditions; after 4 hours, the mixture was collected and washed with pre-cooled MeOH / Et 2 O(1:1) washed twice, and then dried in a vacuum environment; subsequently, the dried PLGA-NHS pellets were dissolved in dry chloroform, and the bifunctional modified NH 2 -PEG-COOH and diisopropylethylamine were reacted; after 24 hours, MeOH / Et 2 O (1:1) washing, and vacuum drying to obtain PLGA-PEG-COOH complex;

[0080] 2) Preparation of VB12-labeled PLGA-PEG nanocomposites: PLGA-PEG nanocomposites (1mol), vitamin B12 (1mol) and EDC (1.1mol) obtained in step ① were added to the mixture containing or not containing DMAP (0.1mol) Butylene oxide solution, stirred at room temperature for 4 hours. ...

Embodiment 2

[0089] Embodiment 2: the safety of VB12-PLGA-PEG nano carrier

[0090] After co-incubating different concentrations of PLGA-PEG and PLGA-PEG-VB12 nanocarriers (2-500ug / mL) with gastric normal mucosal epithelial cells (GES-1) for 24 hours, the Cell Counting Kit (CCK-8) was used to experiment Detection of cell viability.

[0091] figure 2 is the safety result of miR-532-3p@PLGA-PEG-VB12 nanocomplex. The results of CCK-8 showed that under the treatment of PLGA-PEG and VB12-PLGA-PEG nanocarriers at multiple concentrations in the range of 2-500 μg / mL, the cell survival rate of GES-1 cells was above 90% ( figure 2 ), so PLGA-PEG and VB12-PLGA-PEG nanocarriers are relatively safe nanomaterials.

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Abstract

The invention discloses a synthesis method and application of an miRNA-carrying VB12 binding type nano-composite. The synthesis method comprises the following steps: mixing and dissolving a PLGA-PEG nano-composite, vitamin B12, EDC and DMAP in an anhydrous solvent A, and performing stirring for reaction at 15-40 DEG C; and after the reaction is finished, performing dialyzing, and removing the solvent to obtain the vitamin B12 combined nano-composite. The synthesis method has the advantages of mild preparation conditions, cheap required raw materials, convenient operation, simple process, highefficiency and practicability. The prepared nano-composite optimizes nucleic acid drugs from three aspects of water solubility, stability and tumor targeting, endows the nucleic acid drugs with efficient and low-toxicity anti-tumor effects, and has a wide application prospect in the field of tumor treatment.

Description

technical field [0001] The invention relates to a method for synthesizing nano-medicines, in particular to a method for synthesizing nano-medicines with better targeting to tumor cells. Background technique [0002] MicroRNAs (miRNAs) are small single-stranded non-coding RNAs with a length of about 22 nucleotides, which bind to the 3' untranslated regions (UTRs) of target genes through complementary base pairing, and then cut target genes The translation of the transcript or the translation of the transcript, and finally play a role in inhibiting the post-transcriptional regulation of the expression of the target gene. However, miRNAs themselves are small molecular nucleic acids, which are easily degraded by nucleases in the blood and become ineffective in the free state. Therefore, how to achieve efficient and targeted delivery of miRNAs to tumor lesions is the key to tumor therapy. [0003] Traditional gene delivery systems mainly include two categories: viral vectors and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/22A61K31/7105A61P35/00
CPCA61K9/5146A61K9/5123A61K31/7105A61P35/00
Inventor 郭伟洪胡彦锋陈志安梁延锐黄慧琳沈国栋陈昭宇李时祺李国新
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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