Hypoxia response lipidosome drug carrier as well as preparation method and application thereof
A technology of liposomes and drugs, which is applied in the field of pharmacy, can solve the problems of no reports of hypoxia-responsive liposome drug carriers, etc., and achieve the effects of improving anti-tumor effects, easy scale-up production, and simple preparation methods
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0043] The hypoxia response molecule selected for this implementation is a 2-nitroimidazole derivative, and its preparation method is as follows:
[0044]
[0045] Take 60 mg of 2-nitroimidazole and 70 mg of 1,12-dibromododecane and add them into 5 mL of dimethylformamide (DMF) to dissolve fully, then add K 2 CO 3 80 mg, stirred at 50°C for 24 hours; add 5 mL of deionized water to the reaction solution, then add 5 mL of ethyl acetate for extraction, repeat the extraction 3 times, combine the extraction solution, then add 2 mL of deionized water to the extraction solution for shaking, then let it stand for separation layer, remove the lower aqueous solution, repeat 3 times, and remove the ethyl acetate by vacuum rotary evaporation to obtain 2-nitroimidazole derivatives, that is, linear hypoxia responsive molecules HR (hypoxia responsive elements), its hydrogen nuclear magnetic resonance spectrum (1H NMR) Such as figure 1 shown.
Embodiment 2-1
[0047] Preparation of liposomal drug carrier with hypoxia response effect:
[0048] Dipalmitoylphosphatidylcholine (DPPC), high-purity cholesterol (HP-CHOL), dimyristoylphosphatidylcholine (DMPC), methoxy-polyethylene glycol-distearoylphosphatidylethanolamine ( DSPE-MPEG2K), hydrophobic aromatic nitro compound derivatives (HR) are dissolved in methanol and chloroform mixed solution (volume ratio 1:4) according to the mass ratio (total 20mg) of 70:20:3:3:16, minus Press rotary steaming to form a film, and use 10mL deionized water to ultrasonically hydrate at 50°C to obtain blank hypoxia-responsive liposome HR-LPs; the preparation method of control blank liposome LPs is the same as HR-LPs, and the liposome components DPPC, HP-CHOL, DMPC, and DSPE-MPEG2K are also mass ratio 70:20:3:3 (total 20mg), without adding hypoxia response molecules, vacuum rotary steaming to form a film, 10mL deionized water 50 ℃ ultrasonic hydration , to get blank liposome LPs.
Embodiment 2-2
[0050] Preparation of liposomal drug carrier with hypoxia response effect:
[0051] Dipalmitoylphosphatidylcholine (DPPC), high-purity cholesterol (HP-CHOL), dimyristoylphosphatidylcholine (DMPC), methoxy-polyethylene glycol-distearoylphosphatidylethanolamine ( DSPE-MPEG2K), hydrophobic aromatic nitro compound derivatives (HR) were dissolved in methanol and chloroform mixed solution (volume ratio 1:3) according to the mass ratio of 70:18:3:3:12 (total 20mg), and the rest The procedure was the same as that in Example 2-1, and blank hypoxia-responsive liposome HR-LPs were prepared.
PUM
Property | Measurement | Unit |
---|---|---|
Particle size | 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