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

ABSTRACT: 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-H₂ O). DCPA-H₂ O liposomes became protonated relatively fast already at pH<6.8, due to the high HOMO binding energy of DCPA-H₂ O. In murine models, DCPA-H₂ O liposomes had longer blood circulation times than natural DPPC or cationic DCPM liposomes, while after tail-vein injection DCPA-H₂ 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-H₂ O liposomes exceeded the ones of clinically applied ciprofloxacin as well as of ciprofloxacin-loaded DPPC or DCPM liposomes.

SUBMITTER: Wang DY

PROVIDER: S-EPMC8362074 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature

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

Wang Da-Yuan DY Yang Guang G van der Mei Henny C HC Ren Yijin Y Busscher Henk J HJ Shi Linqi L

Angewandte Chemie (International ed. in English) 20210701 32

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-H2 O). DCPA-H2 O liposomes became protonated relatively fast already at pH<6.8, due to the high HOMO binding energy of DCPA-H2 O. In murine models, DCPA-H2 O liposomes had longer blood circulation times than natural DPPC or cationic DCPM liposomes, while after tail-vein ...[more]

PMID: 34028150

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