Nano-carrier particle prepared from sugar-modified folic acid derivative and application of nano-carrier particle
A folic acid derivative and sugar modification technology, applied in the field of biomedicine, can solve the problems of affecting the therapeutic effect, uneven particle size of nanoparticles, immunogenicity reaction, etc. simple effect
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0043] This embodiment provides a nanocarrier particle FA-2-DG. FA-2-DG is formed by linking deoxyglucose and folic acid via aminoethanol, wherein the carboxyl group of folic acid is connected with the amino group of aminoethanol to form an amide bond, and the aminoethanol The hydroxyl group and the hydroxyl group of deoxyglucose are connected to form a glycosidic bond. The chemical structural formula of the FA-2-DG is as figure 2 shown.
[0044] Deoxyglucose has multiple hydroxyl groups. During the reaction, the hydroxyl groups have high reactivity, so they need to be protected with acetyl groups before the reaction. The acetyl-protected reaction proceeds from deoxyglucose and acetic anhydride in anhydrous pyridine. The amino group of aminoethanol will also have relatively high reactivity during the reaction process, so aminoethanol is not used directly in the reaction process, but 2-bromoethanol is used to react with acetyl deoxyglucose first, and this step requires trifl...
Embodiment 2
[0073] This embodiment provides a nanocarrier particle—glucose-modified folic acid derivative. The folic acid derivative is formed by linking glucose and folic acid through a linking arm of two carbon atoms, aminoethanol, and is a kind of nanocarrier particle. The 1-hydroxyl group of glucose and the hydroxyl group of aminoethanol form a glycosidic bond, and the carboxyl group of folic acid and the amino group of aminoethanol form an amide bond. The structure formed in this way can maintain good stability in vitro, and can be widely used in vivo by amidase and Hydrolyzed by glycosidase, quickly metabolized and excreted from the body, not easy to cause accumulation.
[0074] Such as Figure 6 As shown, taking glucose and connecting arm as an example of aminoethanol with 2 carbon atoms, the synthesis of the folic acid derivative comprises the following steps:
[0075] (1) Preparation of 6-(acetoxymethyl)-tetrahydro-2,3,4,5-tetraacetoxy-pyran (compound 2)
[0076] Dissolve 5.0 g...
Embodiment 3
[0095] In this example, the nano-carrier particles prepared in Example 1 were used to carry the anti-tumor drug cisplatin to obtain a targeted anti-tumor nano-particle, which was connected to the nano-carrier particles described in Example 1 and cisplatin through a coordination bond. To prepare the complex of FA-2-DG and cisplatin, mix the aqueous solution of cisplatin and FA-2-DG of the same concentration and stir at room temperature. After two hours, cisplatin and FA-2-DG are formed as Figure 8 The coordination compound (FA-2-DG-Pt) shown. The mixed solution was injected into HPLC-MS analysis, and the formation of the complex was confirmed. For mass spectrometry results, see Figure 9 .
[0096] The morphological characterization techniques of atomic force microscopy, transmission electron microscopy and scanning electron microscopy all confirmed that FA-2-DG itself can self-assemble to form nanoparticles, and form a coordination bond with cisplatin, and obtain FA-2-DG-Pt...
PUM
Property | Measurement | Unit |
---|---|---|
molecular weight | aaaaa | aaaaa |
particle diameter | aaaaa | aaaaa |
particle diameter | aaaaa | aaaaa |
Abstract
Description
Claims
Application Information
- R&D Engineer
- R&D Manager
- IP Professional
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com