Reference : Liposomes and drug-in-cyclodextrin-in-liposomes formulations encapsulating 17β-estrad...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/241638
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
English
Gallez, Anne* mailto [Université de Liège - ULiège > > Cancer-Tumours and development biology >]
Palazzo, Claudio* mailto [Université de Liège > Département de pharmacie > Département de pharmacie >]
Blacher, Silvia mailto [Université de Liège - ULiège > > Cancer-Tumours and development biology >]
Tskitishvili, Ekaterine mailto [Université de Liège - ULiège > > Cancer-Tumours and development biology >]
Noël, Agnès mailto [Université de Liège - ULiège > Département des sciences cliniques > Labo de biologie des tumeurs et du développement >]
Foidart, Jean-Michel mailto [Université de Liège - ULiège > Département des sciences cliniques > Département des sciences cliniques >]
Evrard, Brigitte mailto [Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique >]
Pequeux, Christel* mailto [Université de Liège - ULiège > Département des sciences biomédicales et précliniques > Département des sciences biomédicales et précliniques >]
Piel, Géraldine* mailto [Université de Liège - ULiège > Département de pharmacie > Développement de nanomédicaments >]
* These authors have contributed equally to this work.
5-Jan-2020
International Journal of Pharmaceutics
Elsevier
573
118861
Yes (verified by ORBi)
International
0378-5173
1873-3476
Netherlands
[en] Estradiol ; Estrogen Receptor α ; Drug-in Cyclodextrin-in-Liposomes ; Liposomes
[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.
Centre Interdisciplinaire de Recherche sur le Médicament - CIRM
http://hdl.handle.net/2268/241638
10.1016/j.ijpharm.2019.118861

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