Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 60, Issue 32, Pages 17714-17719Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202106329
Keywords
hydrogen bonding; pH-responsive; pyridine betaine; self-targeting; zwitterionic lipids
Categories
Funding
- National Natural Science Foundation of China [21620102005, 51933006]
Ask authors/readers for more resources
DCPA-H2O liposomes with high protonation capability demonstrated enhanced targeting to solid tumors and intra-abdominal infectious biofilms in murine models. Additionally, therapeutic efficacy of ciprofloxacin-loaded DCPA-H2O liposomes in infected wound-healing model exceeded that of clinically applied ciprofloxacin and other liposomes loaded with ciprofloxacin.
A lipid named DCPA was synthesized under microwave-assisted heating. DCPA possesses a pyridine betaine, hydrophilic group that can be complexed with water through hydrogen bonding (DCPA-H2O). DCPA-H2O liposomes became protonated relatively fast already at pH<6.8, due to the high HOMO binding energy of DCPA-H2O. In murine models, DCPA-H2O liposomes had longer blood circulation times than natural DPPC or cationic DCPM liposomes, while after tail-vein injection DCPA-H2O liposomes targeted faster to solid tumors and intra-abdominal infectious biofilms. Therapeutic efficacy in a murine, infected wound-healing model of tail-vein injected ciprofloxacin-loaded DCPA-H2O liposomes exceeded the ones of clinically applied ciprofloxacin as well as of ciprofloxacin-loaded DPPC or DCPM liposomes.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available