2017
DOI: 10.1016/j.bbamem.2017.06.010
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Changes in membrane biophysical properties induced by the Budesonide/Hydroxypropyl-β-cyclodextrin complex

Abstract: Budesonide (BUD), a poorly soluble anti-inflammatory drug, is used to treat patients suffering from asthma and COPD (Chronic Obstructive Pulmonary Disease). Hydroxypropyl-β-cyclodextrin (HPβCD), a biocompatible cyclodextrin known to interact with cholesterol, is used as a drug-solubilizing agent in pharmaceutical formulations. Budesonide administered as an inclusion complex within HPβCD (BUD:HPβCD) required a quarter of the nominal dose of the suspension formulation and significantly reduced neutrophil-induced… Show more

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Cited by 19 publications
(16 citation statements)
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“…Membrane permeabilization was followed as described previously 78 . Release of entrapped calcein at self-quenching concentrations from LUV composed by PLPC/sitosterol (80/20–16 µM) can be monitored by the fluorescence increase upon dilution following their leakage from the vesicles.…”
Section: Methodsmentioning
confidence: 99%
“…Membrane permeabilization was followed as described previously 78 . Release of entrapped calcein at self-quenching concentrations from LUV composed by PLPC/sitosterol (80/20–16 µM) can be monitored by the fluorescence increase upon dilution following their leakage from the vesicles.…”
Section: Methodsmentioning
confidence: 99%
“…LUVs of fish-like, holothuroid-like and sterol-free (Table 1 ) were prepared in a saline-Tris-HCl buffer (600 mM NaCl, 10 mM TRIS, pH 7.5) with a self-quenching concentration of calcein (10 mM). The un-encapsulated dye was removed on a gel column of Sephadex G75 42 .…”
Section: Methodsmentioning
confidence: 99%
“…To give insight on the molecular mechanisms involved in the protective effect of BUD:HPBCD and HPBCD, the potential role of cholesterol on ROS generation and PI3/Akt phosphorylation induced by H 2 O 2 + LPS as well as the protective effects of the BUD:HPβCD complex and HPβCD were investigated. The rationale was derived from the ability of cyclodextrins to interact with cholesterol [ 35 ], the effects of BUD:HPβCD and HPβCD on the biophysical membrane properties of cholesterol-enriched domains [ 27 ], the importance of lipid-ordered domains enriched in cholesterol in membrane called rafts for ROS generation [ 36 , 37 ] and PI3K/Akt signaling [ 23 , 26 ].…”
Section: Resultsmentioning
confidence: 99%
“…Cholesterol is largely known for its effect on biophysical membrane properties and cholesterol-enriched domains are linked to membrane signaling [ 23 , 24 , 25 , 26 ] including pathways involved in PI3K/Akt signaling and inflammation processes. On giant unilamellar vesicles (GUVs) and lipid monolayers, BUD:HPβCD induced the disruption of cholesterol-enriched raft-like liquid ordered domains—an increase in membrane permeability and fluidity [ 27 ]. Except for membrane fluidity, all these effects were enhanced when HPβCD was complexed with budesonide as compared with HPβCD [ 27 ].…”
Section: Introductionmentioning
confidence: 99%
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