Journal of Drug Delivery Science and Technology, volume 57, pages 101609

Effects of spacers within a series of novel folate-containing lipoconjugates on the targeted delivery of nucleic acids

Publication typeJournal Article
Publication date2020-06-01
Quartile SCImago
Q1
Quartile WOS
Q1
Impact factor5
ISSN17732247, 25888943
Pharmaceutical Science
Abstract
Limitations regarding the targeted delivery of therapeutic nucleic acids into cancer cells can be overcome by developing a non-viral delivery system equipped with folate-containing conjugates. Here, we report the synthesis of novel folate-containing lipoconjugates (FLs), which differ by spacers between the hydrophobic domain and ligand (folic acid). FLs were incorporated into a liposome composed of the polycationic amphiphile 1,26-bis(cholest-5-en-3β-yloxycarbonylamino)-7,11,16,20-tetraazahexacosan tetrahydrochloride (2X3) and helper lipid 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE). At low (2/1) nitrogen to phosphate (N/P) ratio, liposomes containing 0.5 mol% FL with a short hydrophobic spacer and 2 mol% FL with medium hydrophilic spacer were compared with control liposomes containing 2 mol% FL with a polyethylene glycol spacer and showed higher transfection efficiency than non-targeted liposomal formulations and the commercial agent Lipofectamine 2000. At an N/P ratio of 4/1, the transfection efficiency of FL-containing liposomes were correlated neither with FL content within the liposomes nor FL structure.

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Shmendel E. et al. Effects of spacers within a series of novel folate-containing lipoconjugates on the targeted delivery of nucleic acids // Journal of Drug Delivery Science and Technology. 2020. Vol. 57. p. 101609.
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Shmendel E., Kabilova T., Morozova N., Зенкова М. А., Maslov M. Effects of spacers within a series of novel folate-containing lipoconjugates on the targeted delivery of nucleic acids // Journal of Drug Delivery Science and Technology. 2020. Vol. 57. p. 101609.
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RIS Copy
TY - JOUR
DO - 10.1016/j.jddst.2020.101609
UR - https://doi.org/10.1016%2Fj.jddst.2020.101609
TI - Effects of spacers within a series of novel folate-containing lipoconjugates on the targeted delivery of nucleic acids
T2 - Journal of Drug Delivery Science and Technology
AU - Shmendel, Elena
AU - Kabilova, Tatyana
AU - Morozova, Nina
AU - Зенкова, М. А.
AU - Maslov, Mikhail
PY - 2020
DA - 2020/06/01 00:00:00
PB - Elsevier
SP - 101609
VL - 57
SN - 1773-2247
SN - 2588-8943
ER -
BibTex
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BibTex Copy
@article{2020_Shmendel,
author = {Elena Shmendel and Tatyana Kabilova and Nina Morozova and М. А. Зенкова and Mikhail Maslov},
title = {Effects of spacers within a series of novel folate-containing lipoconjugates on the targeted delivery of nucleic acids},
journal = {Journal of Drug Delivery Science and Technology},
year = {2020},
volume = {57},
publisher = {Elsevier},
month = {jun},
url = {https://doi.org/10.1016%2Fj.jddst.2020.101609},
pages = {101609},
doi = {10.1016/j.jddst.2020.101609}
}
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