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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‐H 2 O). DCPA‐H 2 O liposomes became protonated relatively fast already at pH<6.8, due to the high HOMO binding energy of DCPA‐H 2 O. In murine models, DCPA‐H 2 O liposomes had longer blood circulation times than natural DPPC or cationic DCPM liposomes, while after tail‐vein injection DCPA‐H 2 O 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‐H 2 O liposomes exceeded the ones of clinically applied ciprofloxacin as well as of ciprofloxacin‐loaded DPPC or DCPM liposomes.

Liposomes with Water as a pH‐Responsive Functionality for Targeting of Acidic Tumor and Infection Sites