Synthesis, gene transfection efficiency, and serum compatibility of β-sitosterol-based cationic lipids with different headgroups
4
Issued Date
2023-01-01
Resource Type
ISSN
11440546
eISSN
13699261
Scopus ID
2-s2.0-85174397080
Journal Title
New Journal of Chemistry
Rights Holder(s)
SCOPUS
Bibliographic Citation
New Journal of Chemistry (2023)
Suggested Citation
Thongbamrer C., Yingyongnarongkul B.E., Sakee U., Nguitragool W., Radchatawedchakoon W. Synthesis, gene transfection efficiency, and serum compatibility of β-sitosterol-based cationic lipids with different headgroups. New Journal of Chemistry (2023). doi:10.1039/d3nj02503a Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/90814
Title
Synthesis, gene transfection efficiency, and serum compatibility of β-sitosterol-based cationic lipids with different headgroups
Other Contributor(s)
Abstract
We report syntheses, gene delivery, and physicochemical properties of twelve plant sterol (β-sitosterol)-based cationic lipids with eight types of headgroups. In these lipid molecules, the cationic headgroup and the β-sitosterol tail were joined by a carbamate linkage. The synthesized cationic lipids were formulated into liposomes with helper lipid dioleoylphosphatidyl ethanolamine (DOPE). The physical and DNA-binding properties of the liposomes were characterized, and their formulations were optimized for cell transfection. We found that liposomes prepared from cationic 1B, which has the sperminium headgroup, had the highest transfection efficiency comparable to that of commercial transfection reagent Lipofectamine™ 2000 (L2K). The particle size and the zeta potential of the optimal 1B liposomes were 360 ± 30 nm and 49 ± 10 mV, respectively. Importantly, the liposome 1B had low toxicity, possibly due to the biodegradability of all of its components - the headgroup, the linker, and the tail. In addition, cationic liposome 1B can effectively protect DNA from degradation in the presence of serum, thus enabling high transfection efficiency in the presence of up to 40% fetal bovine serum.