Article (Scientific journals)
Liposomes and drug-in-cyclodextrin-in-liposomes formulations encapsulating 17β-estradiol: an innovative drug delivery system that prevents the activation of the membrane-initiated steroid signaling (MISS) of estrogen receptor α
Gallez, Anne; Palazzo, Claudio; Blacher, Silvia et al.
2020In International Journal of Pharmaceutics, 573, p. 118861
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Keywords :
Estradiol; Estrogen Receptor α; Drug-in Cyclodextrin-in-Liposomes; Liposomes
Abstract :
[en] The encapsulation into liposomes of several types of molecules presents the advantages to protect the activity of these molecules and to target specific tissues. Nevertheless, a major obstacle remains the incomplete understanding of nano-bio interactions. Specifically, the impact that inclusion of drug into liposomes or of drug-in-cyclodextrin-in liposomes (DCL) could have on the molecular and cellular mechanism of drug action is largely unknown. As a proof of concept, we evaluated the impact of 17β-estradiol (E2) included into liposomes or DCL on estrogen receptor (ER)α signaling pathways. Indeed, ERα relays the pleiotropic actions of E2 in physiology and pathophysiology through two major pathways: (1) the genomic/nuclear effects associated to the transcriptional activity of the ERα and (2) the rapid/nongenomic/membrane-initiated steroid signaling (MISS) effects related to the induction of fast signaling pathways occurring when ERα is anchored to the plasma membrane. We evidenced that the inclusion of E2 into liposomes (Lipo-E2) or into DCL (DCL-E2) prevented the activation of the rapid/nongenomic/extranuclear/MISS pathway of ERα, while the activation of the genomic/nuclear pathway was maintained. These results support that Lipo-E2 and DCL-E2 could be a useful tool to delineate the complex molecular mechanisms associated to ERα. In conclusion, this study supports the notion that inclusion of drugs into liposomes or DCL could modify some specific pathways of their molecular and cellular mechanisms of action. These results emphasized that attention should be paid to nano-bio interactions induced by the use of nanovectors in medicine.
Research center :
CIRM - Centre Interdisciplinaire de Recherche sur le Médicament - ULiège
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Gallez, Anne  ;  Université de Liège - ULiège > Cancer-Tumours and development biology
Palazzo, Claudio  ;  Université de Liège > Département de pharmacie > Département de pharmacie
Blacher, Silvia ;  Université de Liège - ULiège > Cancer-Tumours and development biology
Tskitishvili, Ekaterine  ;  Université de Liège - ULiège > Cancer-Tumours and development biology
Noël, Agnès ;  Université de Liège - ULiège > Département des sciences cliniques > Labo de biologie des tumeurs et du développement
Foidart, Jean-Michel ;  Université de Liège - ULiège > Département des sciences cliniques > Département des sciences cliniques
Evrard, Brigitte  ;  Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Pequeux, Christel   ;  Université de Liège - ULiège > Département des sciences biomédicales et précliniques > Département des sciences biomédicales et précliniques
Piel, Géraldine  ;  Université de Liège - ULiège > Département de pharmacie > Développement de nanomédicaments
 These authors have contributed equally to this work.
Language :
English
Title :
Liposomes and drug-in-cyclodextrin-in-liposomes formulations encapsulating 17β-estradiol: an innovative drug delivery system that prevents the activation of the membrane-initiated steroid signaling (MISS) of estrogen receptor α
Publication date :
05 January 2020
Journal title :
International Journal of Pharmaceutics
ISSN :
0378-5173
eISSN :
1873-3476
Publisher :
Elsevier, Netherlands
Volume :
573
Pages :
118861
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 25 November 2019

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