European Journal of Pharmaceutics and Biopharmaceutics, volume 123, pages 59-70
Targeted delivery of nucleic acids into xenograft tumors mediated by novel folate-equipped liposomes
Kabilova Tatyana O.
1
,
Morozova Nina G.
2
,
Maslov Mikhail A
,
Chernolovskaya Elena L.
1
,
Gladkikh Daniil V.
,
Zenkova Marina A
,
Shmendel Elena V
,
Markov Oleg V
1
,
Shmendel Elena
2
,
Maslov Michael
2
,
Publication type: Journal Article
Publication date: 2018-02-01
Quartile SCImago
Q1
Quartile WOS
Q1
Impact factor: 4.9
ISSN: 09396411, 18733441
General Medicine
Pharmaceutical Science
Biotechnology
Abstract
Folate receptors (FR) are cellular markers highly expressed in various cancer cells. Here, we report on the synthesis of a novel folate-containing lipoconjugate (FC) built of 1,2-di-O-ditetradecyl-rac-glycerol and folic acid connected via a PEG spacer, and the evaluation of the FC as a targeting component of liposomal formulations for nucleic acid (NA) delivery into FR expressing tumor cells. FR-targeting liposomes, based on polycationic lipid 1,26-bis(cholest-5-en-3β-yloxycarbonylamino)-7,11,16,20-tetraazahexacosan tetrahydrochloride (2X3), lipid helper dioleoylphosphatidylethanolamine (DOPE) and novel FC, formed small compact particles in solution with diameters of 60 ± 22 nm, and were not toxic to cells. Complexes of NAs with the liposomes were prepared at various nitrogen to phosphate ratios (N/P) to optimize liposome/cell interactions. We showed that FR-mediated delivery of different nucleic acids mediated by 2X3-DOPE/FC liposomes occurs in vitro at low N/P (1/1 and 2/1); under these conditions FC-containing liposomes display 3-4-fold higher transfection efficiency in comparison with conventional formulation. Lipoplexes formed at N/P 1/1 by targeted liposomes and cargo (Cy7-labeled siRNA targeting MDR1 mRNA) in vivo efficiently accumulate in tumor (∼15-18% of total amount), and kidneys (71%), and were retained there for more than 24 h, causing efficient downregulation of p-glycoprotein expression (to 40% of control) in tumors. Thus, FC containing liposomes provide effective targeted delivery of nucleic acids into tumor cells in vitro and in xenograft tumors in vivo.
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1 publication, 3.23%
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Springer Nature
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1 publication, 3.23%
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American Chemical Society (ACS)
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1 publication, 3.23%
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Taylor & Francis
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1 publication, 3.23%
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1 publication, 3.23%
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- We do not take into account publications that without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
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Shmendel E. V. et al. Targeted delivery of nucleic acids into xenograft tumors mediated by novel folate-equipped liposomes // European Journal of Pharmaceutics and Biopharmaceutics. 2018. Vol. 123. pp. 59-70.
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Shmendel E. V., Gladkikh D. V., Chernolovskaya E. L., Markov O. V., Morozova N. G., Maslov M. A., Zenkova M. A., Kabilova T. O., Shmendel E., Gladkikh D. V., Maslov M., Зенкова М. А. Targeted delivery of nucleic acids into xenograft tumors mediated by novel folate-equipped liposomes // European Journal of Pharmaceutics and Biopharmaceutics. 2018. Vol. 123. pp. 59-70.
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TY - JOUR
DO - 10.1016/j.ejpb.2017.11.010
UR - https://doi.org/10.1016%2Fj.ejpb.2017.11.010
TI - Targeted delivery of nucleic acids into xenograft tumors mediated by novel folate-equipped liposomes
T2 - European Journal of Pharmaceutics and Biopharmaceutics
AU - Shmendel, Elena V
AU - Gladkikh, Daniil V.
AU - Chernolovskaya, Elena L.
AU - Markov, Oleg V
AU - Morozova, Nina G.
AU - Maslov, Mikhail A
AU - Zenkova, Marina A
AU - Kabilova, Tatyana O.
AU - Shmendel, Elena
AU - Gladkikh, Daniil V.
AU - Maslov, Michael
AU - Зенкова, М. А.
PY - 2018
DA - 2018/02/01 00:00:00
PB - Elsevier
SP - 59-70
VL - 123
SN - 0939-6411
SN - 1873-3441
ER -
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@article{2018_Shmendel,
author = {Elena V Shmendel and Daniil V. Gladkikh and Elena L. Chernolovskaya and Oleg V Markov and Nina G. Morozova and Mikhail A Maslov and Marina A Zenkova and Tatyana O. Kabilova and Elena Shmendel and Daniil V. Gladkikh and Michael Maslov and М. А. Зенкова},
title = {Targeted delivery of nucleic acids into xenograft tumors mediated by novel folate-equipped liposomes},
journal = {European Journal of Pharmaceutics and Biopharmaceutics},
year = {2018},
volume = {123},
publisher = {Elsevier},
month = {feb},
url = {https://doi.org/10.1016%2Fj.ejpb.2017.11.010},
pages = {59--70},
doi = {10.1016/j.ejpb.2017.11.010}
}
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