| LIBÁNSKÁ, Alena, Eva RANDÁROVÁ, Daniela RUBANOVÁ, Svitlana SKOROPLYAS, Josef BRYJA, Lukáš KUBALA, Rafal KONEFAL, Adéla NAVRÁTILOVÁ, Lucie A. CEREZO, Ladislav ŠENOLT and Tomáš ETRYCH. Dexamethasone nanomedicines with optimized drug release kinetics tailored for treatment of site-specific rheumatic musculoskeletal diseases. International Journal of Pharmaceutics. Elsevier B.V., 2024, vol. 654, April 2024, p. 1-10. ISSN 0378-5173. Available from: https://dx.doi.org/10.1016/j.ijpharm.2024.123979. |
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@article{2410760,
author = {Libánská, Alena and Randárová, Eva and Rubanová, Daniela and Skoroplyas, Svitlana and Bryja, Josef and Kubala, Lukáš and Konefal, Rafal and Navrátilová, Adéla and Cerezo, Lucie A. and Šenolt, Ladislav and Etrych, Tomáš},
article_number = {April 2024},
doi = {http://dx.doi.org/10.1016/j.ijpharm.2024.123979},
keywords = {Controlled drug release; Polymer conjugates; HPMA; Dexamethasone; Hydrazone bond},
language = {eng},
issn = {0378-5173},
journal = {International Journal of Pharmaceutics},
title = {Dexamethasone nanomedicines with optimized drug release kinetics tailored for treatment of site-specific rheumatic musculoskeletal diseases},
url = {https://www.sciencedirect.com/science/article/pii/S0378517324002138},
volume = {654},
year = {2024}
}
TY - JOUR
ID - 2410760
AU - Libánská, Alena - Randárová, Eva - Rubanová, Daniela - Skoroplyas, Svitlana - Bryja, Josef - Kubala, Lukáš - Konefal, Rafal - Navrátilová, Adéla - Cerezo, Lucie A. - Šenolt, Ladislav - Etrych, Tomáš
PY - 2024
TI - Dexamethasone nanomedicines with optimized drug release kinetics tailored for treatment of site-specific rheumatic musculoskeletal diseases
JF - International Journal of Pharmaceutics
VL - 654
IS - April 2024
SP - 1-10
EP - 1-10
PB - Elsevier B.V.
SN - 03785173
KW - Controlled drug release
KW - Polymer conjugates
KW - HPMA
KW - Dexamethasone
KW - Hydrazone bond
UR - https://www.sciencedirect.com/science/article/pii/S0378517324002138
N2 - The application of polymer-based drug delivery systems is advantageous for improved pharmacokinetics, controlled drug release, and decreased side effects of therapeutics for inflammatory disease. Herein, we describe the synthesis and characterization of linear N-(2-hydroxypropyl)methacrylamide-based polymer conjugates designed for controlled release of the anti-inflammatory drug dexamethasone through pH-sensitive bonds. The tailored release rates were achieved by modifying DEX with four oxo-acids introducing reactive oxo groups to the DEX derivatives. Refinement of reaction conditions yielded four well-defined polymer conjugates with varied release profiles which were more pronounced at the lower pH in cell lysosomes. In vitro evaluations in murine peritoneal macrophages, human synovial fibroblasts, and human peripheral blood mononuclear cells demonstrated that neither drug derivatization nor polymer conjugation affected cytotoxicity or anti-inflammatory properties. Subsequent in vivo tests using a murine arthritis model validated the superior anti-inflammatory efficacy of the prepared DEX-bearing conjugates with lower release rates. These nanomedicines showed much higher therapeutic activity compared to the faster release systems or DEX itself.
ER -
LIBÁNSKÁ, Alena, Eva RANDÁROVÁ, Daniela RUBANOVÁ, Svitlana SKOROPLYAS, Josef BRYJA, Lukáš KUBALA, Rafal KONEFAL, Adéla NAVRÁTILOVÁ, Lucie A. CEREZO, Ladislav ŠENOLT and Tomáš ETRYCH. Dexamethasone nanomedicines with optimized drug release kinetics tailored for treatment of site-specific rheumatic musculoskeletal diseases. \textit{International Journal of Pharmaceutics}. Elsevier B.V., 2024, vol.~654, April 2024, p.~1-10. ISSN~0378-5173. Available from: https://dx.doi.org/10.1016/j.ijpharm.2024.123979.
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