Dexamethasone Conjugates: Synthetic Approaches and Medical Prospects

Dexamethasone (DEX) is the most commonly prescribed glucocorticoid (GC) and has a wide spectrum of pharmacological activity. However, steroid drugs like DEX can have severe side effects on non-target organs. One strategy to reduce these side effects is to develop targeted systems with the controlled...

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Main Authors: Natallia V. Dubashynskaya, Anton N. Bokatyi, Yury A. Skorik
Format: Article
Language:English
Published: MDPI AG 2021-03-01
Series:Biomedicines
Subjects:
Online Access:https://www.mdpi.com/2227-9059/9/4/341
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author Natallia V. Dubashynskaya
Anton N. Bokatyi
Yury A. Skorik
author_facet Natallia V. Dubashynskaya
Anton N. Bokatyi
Yury A. Skorik
author_sort Natallia V. Dubashynskaya
collection DOAJ
description Dexamethasone (DEX) is the most commonly prescribed glucocorticoid (GC) and has a wide spectrum of pharmacological activity. However, steroid drugs like DEX can have severe side effects on non-target organs. One strategy to reduce these side effects is to develop targeted systems with the controlled release by conjugation to polymeric carriers. This review describes the methods available for the synthesis of DEX conjugates (carbodiimide chemistry, solid-phase synthesis, reversible addition fragmentation-chain transfer [RAFT] polymerization, click reactions, and 2-iminothiolane chemistry) and perspectives for their medical application as GC drug or gene delivery systems for anti-tumor therapy. Additionally, the review focuses on the development of DEX conjugates with different physical-chemical properties as successful delivery systems in the target organs such as eye, joint, kidney, and others. Finally, polymer conjugates with improved transfection activity in which DEX is used as a vector for gene delivery in the cell nucleus have been described.
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spelling doaj.art-363cb3ec8a17470191b64164991f34d12023-11-21T13:06:52ZengMDPI AGBiomedicines2227-90592021-03-019434110.3390/biomedicines9040341Dexamethasone Conjugates: Synthetic Approaches and Medical ProspectsNatallia V. Dubashynskaya0Anton N. Bokatyi1Yury A. Skorik2Institute of Macromolecular Compounds of the Russian Academy of Sciences, Bolshoy pr. V.O. 31, 199004 St. Petersburg, RussiaInstitute of Macromolecular Compounds of the Russian Academy of Sciences, Bolshoy pr. V.O. 31, 199004 St. Petersburg, RussiaInstitute of Macromolecular Compounds of the Russian Academy of Sciences, Bolshoy pr. V.O. 31, 199004 St. Petersburg, RussiaDexamethasone (DEX) is the most commonly prescribed glucocorticoid (GC) and has a wide spectrum of pharmacological activity. However, steroid drugs like DEX can have severe side effects on non-target organs. One strategy to reduce these side effects is to develop targeted systems with the controlled release by conjugation to polymeric carriers. This review describes the methods available for the synthesis of DEX conjugates (carbodiimide chemistry, solid-phase synthesis, reversible addition fragmentation-chain transfer [RAFT] polymerization, click reactions, and 2-iminothiolane chemistry) and perspectives for their medical application as GC drug or gene delivery systems for anti-tumor therapy. Additionally, the review focuses on the development of DEX conjugates with different physical-chemical properties as successful delivery systems in the target organs such as eye, joint, kidney, and others. Finally, polymer conjugates with improved transfection activity in which DEX is used as a vector for gene delivery in the cell nucleus have been described.https://www.mdpi.com/2227-9059/9/4/341dexamethasonedrug conjugatedrug delivery systemgene delivery systembiopolymers
spellingShingle Natallia V. Dubashynskaya
Anton N. Bokatyi
Yury A. Skorik
Dexamethasone Conjugates: Synthetic Approaches and Medical Prospects
Biomedicines
dexamethasone
drug conjugate
drug delivery system
gene delivery system
biopolymers
title Dexamethasone Conjugates: Synthetic Approaches and Medical Prospects
title_full Dexamethasone Conjugates: Synthetic Approaches and Medical Prospects
title_fullStr Dexamethasone Conjugates: Synthetic Approaches and Medical Prospects
title_full_unstemmed Dexamethasone Conjugates: Synthetic Approaches and Medical Prospects
title_short Dexamethasone Conjugates: Synthetic Approaches and Medical Prospects
title_sort dexamethasone conjugates synthetic approaches and medical prospects
topic dexamethasone
drug conjugate
drug delivery system
gene delivery system
biopolymers
url https://www.mdpi.com/2227-9059/9/4/341
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