Open Access
Open access
volume 557 pages 43-52

Bioresorbable filomicelles for targeted delivery of betulin derivative – In vitro study

Shan-Ming Hsu 2
Thi Hong Nguyen 3
Arkadiusz Orchel 4
Ewa Chodurek 4
Piotr Paduszyński 4
Marzena Jaworska Kik 4
Elwira Chrobak 5
Ewa Bębenek 5
Stanisław Boryczka 5
Magdalena Jarosz Biej 6
Ryszard Smolarczyk 6
Aleksander Forys 7
Publication typeJournal Article
Publication date2019-02-01
scimago Q1
wos Q1
SJR0.988
CiteScore10.1
Impact factor5.2
ISSN03785173, 18733476
Pharmaceutical Science
Abstract
Filomicelles (worm-like micelles) possess high drug loading capacity and long circulation time in the bloodstream. A novel approach can be filomicelles with folic acid (FA) as a targeting moiety. Folate-drug delivery systems can target FA receptors (FAR) that are overexpressed in several human carcinomas, which can potentially maximize therapeutic efficacy while minimizing side effects. The aim of this study was to develop filomicelles from combination of poly(L-lactide)-Jeffamine-folic acid and poly(L-lactide)-poly(ethylene glycol) for delivery of betulin derivative. Phosphate derivative of betulin reveals high cytotoxicity against cancer cells, however its application is restricted due to poor solubility in water. Incorporation into hydrophobic core of micelles can effectively solubilize the drug. Three kinds of micelles were obtained with high drug loading capacity. Based on TEM analysis, the copolymers formed exclusively filomicelles or mixture of filomicelles and spherical micelles. All kinds of micelles provided release of betulin derivative for over 9 days and apart the very initial phase displayed similar release profile. The influence of PLA block on initial burst effect was revealed. The in vitro cytotoxicity of betulin derivative loaded micelles against FAR-positive HeLa cells was confirmed, which proves their usefulness for targeted delivery of cytostatic drug.
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GOST Copy
Jelonek K. et al. Bioresorbable filomicelles for targeted delivery of betulin derivative – In vitro study // International Journal of Pharmaceutics. 2019. Vol. 557. pp. 43-52.
GOST all authors (up to 50) Copy
Jelonek K., Hsu S., Nguyen T. H., Orchel A., Chodurek E., Paduszyński P., Jaworska Kik M., Chrobak E., Bębenek E., Boryczka S., Jarosz Biej M., Smolarczyk R., Forys A. Bioresorbable filomicelles for targeted delivery of betulin derivative – In vitro study // International Journal of Pharmaceutics. 2019. Vol. 557. pp. 43-52.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.ijpharm.2018.12.033
UR - https://doi.org/10.1016/j.ijpharm.2018.12.033
TI - Bioresorbable filomicelles for targeted delivery of betulin derivative – In vitro study
T2 - International Journal of Pharmaceutics
AU - Jelonek, Katarzyna
AU - Hsu, Shan-Ming
AU - Nguyen, Thi Hong
AU - Orchel, Arkadiusz
AU - Chodurek, Ewa
AU - Paduszyński, Piotr
AU - Jaworska Kik, Marzena
AU - Chrobak, Elwira
AU - Bębenek, Ewa
AU - Boryczka, Stanisław
AU - Jarosz Biej, Magdalena
AU - Smolarczyk, Ryszard
AU - Forys, Aleksander
PY - 2019
DA - 2019/02/01
PB - Elsevier
SP - 43-52
VL - 557
PMID - 30576789
SN - 0378-5173
SN - 1873-3476
ER -
BibTex
Cite this
BibTex (up to 50 authors) Copy
@article{2019_Jelonek,
author = {Katarzyna Jelonek and Shan-Ming Hsu and Thi Hong Nguyen and Arkadiusz Orchel and Ewa Chodurek and Piotr Paduszyński and Marzena Jaworska Kik and Elwira Chrobak and Ewa Bębenek and Stanisław Boryczka and Magdalena Jarosz Biej and Ryszard Smolarczyk and Aleksander Forys},
title = {Bioresorbable filomicelles for targeted delivery of betulin derivative – In vitro study},
journal = {International Journal of Pharmaceutics},
year = {2019},
volume = {557},
publisher = {Elsevier},
month = {feb},
url = {https://doi.org/10.1016/j.ijpharm.2018.12.033},
pages = {43--52},
doi = {10.1016/j.ijpharm.2018.12.033}
}