Blood retention and antigenicity of polycarboxybetaine-modified liposomes

Takaaki Ryujin, Taro Shimizu, Ryo Miyahara, Daisuke Asai, Rena Shimazui, Takuma Yoshikawa, Akihiro Kishimura, Takeshi Mori, Tatsuhiro Ishida, Yoshiki Katayama

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)


Zwitterionic polycarboxybetaines (PCBs) have gained attention as alternative stealth polymers whose liposomal formulation and protein conjugates were reported not to elicit anti-polymer antibodies. Here, we studied the blood retention and antigenicity of liposomes modified with PCBs focusing on their chemical structures and doses. We compared PCBs with either 1 or 3 (PCB1 or PCB3) spacer carbons between the carboxylate and ammonium groups. PCB3-modified liposomes had a short blood retention, whereas PCB1-modified liposomes demonstrated extended blood retention that was somewhat superior to PEGylated liposome. This confirmed the excellent non-fouling nature of PCB1 reported previously. Interestingly, PCB1-liposome as well as PCB3-liposome elicited specific IgMs toward each PCB. The dose-dependent production of specific IgMs to PCB-liposomes was similar to that of PEGylated liposome, i.e., high doses of PCB-liposomes reduced the production of specific IgMs, termed immunological tolerance. These results indicate the importance of investigating the effect of dose to clarify the existence of antigenicity of stealth polymers.

Original languageEnglish
Article number119521
JournalInternational Journal of Pharmaceutics
Publication statusPublished - Aug 30 2020

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science


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