Prodrug-Based Targeting Approach for Inflammatory Bowel Diseases Therapy: Mechanistic Study of Phospholipid-Linker-Cyclosporine PLA


Journal

International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791

Informations de publication

Date de publication:
28 Feb 2022
Historique:
received: 29 12 2021
revised: 14 02 2022
accepted: 24 02 2022
entrez: 10 3 2022
pubmed: 11 3 2022
medline: 9 4 2022
Statut: epublish

Résumé

Therapeutics with activity specifically at the inflamed sites throughout the gastrointestinal tract (GIT) would be a major advance in our therapeutic approach to inflammatory bowel disease (IBD). We aimed to develop the prodrug approach that can allow such site-specific drug delivery. Currently, using cyclosporine as a drug of choice in IBD is limited to the most severe cases due to substantial systemic toxicities and narrow therapeutic index of this drug. Previously, we synthesized a series of a phospholipid-linker-cyclosporine (PLC) prodrugs designed to exploit the overexpression of phospholipase A

Identifiants

pubmed: 35269813
pii: ijms23052673
doi: 10.3390/ijms23052673
pmc: PMC8910962
pii:
doi:

Substances chimiques

Phospholipids 0
Prodrugs 0
Cyclosporine 83HN0GTJ6D
Phospholipases A2 EC 3.1.1.4

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : United States-Israel Binational Science Foundation
ID : 2015365

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Auteurs

Milica Markovic (M)

Department of Clinical Pharmacology, School of Pharmacy, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel.

Karina Abramov-Harpaz (K)

Department of Chemistry, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel.
Ilse Katz Institute for Nanoscale Science and Technology, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel.

Clil Regev (C)

Department of Chemistry, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel.
Ilse Katz Institute for Nanoscale Science and Technology, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel.

Shimon Ben-Shabat (S)

Department of Clinical Pharmacology, School of Pharmacy, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel.

Aaron Aponick (A)

Department of Chemistry, University of Florida, Gainesville, FL 32603, USA.

Ellen M Zimmermann (EM)

Department of Medicine, Division of Gastroenterology, University of Florida, Gainesville, FL 32610, USA.

Yifat Miller (Y)

Department of Chemistry, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel.
Ilse Katz Institute for Nanoscale Science and Technology, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel.

Arik Dahan (A)

Department of Clinical Pharmacology, School of Pharmacy, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel.

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Classifications MeSH