Publication details

Long circulating liposomal platform utilizing hydrophilic polymer-based surface modification: preparation, characterisation, and biological evaluation

Authors

TURANEK Jaroslav KOSZTYU Petr TURANEK KNOTIGOVA Pavlina BARTHELDYOVA Eliska HUBATKA Frantisek ODEHNALOVA Nikola MIKULÍK Robert VAŠKOVICOVÁ Naděžda ČELECHOVSKÁ Hana KRATOCHVILOVA Irena FEKETE Ladislav TAVARES Marina R. CHYTIL Petr RASKA Milan ETRYCH Tomas

Year of publication 2024
Type Article in Periodical
Magazine / Source International Journal of Pharmaceutics
MU Faculty or unit

Faculty of Medicine

Citation
Web https://www.sciencedirect.com/science/article/pii/S0378517324006999?via%3Dihub
Doi http://dx.doi.org/10.1016/j.ijpharm.2024.124465
Keywords Stealth liposomes; HPMA copolymer; Complement activation; Drug delivery system; Long-circulating liposomes
Description Liposomes are one of the most important drug delivery vectors, nowadays used in clinics. In general, polyethylene glycol (PEG) is used to ensure the stealth properties of the liposomes. Here, we have employed hydrophilic, biocompatible and highly non-fouling N-(2-hydroxypropyl) methacrylamide (HPMA)-based copolymers containing hydrophobic cholesterol anchors for the surface modification of liposomes, which were prepared by the method of lipid film hydration and extrusion through 100 nm polycarbonate filters. Efficient surface modification of liposomes was confirmed by transmission electron microscopy, atomic force microscopy, and gradient ultracentrifugation. The ability of long-term circulation in the vascular bed was demonstrated in rabbits after i.v. application of fluorescently labelled liposomes. Compared to PEGylated liposomes, HPMA-based copolymer-modified liposomes did not induce specific antibody formation and did not activate murine and human complement. Compared with PEGylated liposomes, HPMA-based copolymer-modified liposomes showed a better long-circulating effect after repeated administration. HPMA-based copolymer-modified liposomes thus represent suitable new candidates for a generation of safer and improved liposomal drug delivery platforms.
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