title: Clove essential oil-in-cyclodextrin-in-liposomes in the aqueous and lyophilized states: From laboratory to large scale using a membrane contactor.
abstract: This work is dedicated to prepare liposomal dry powder formulations of inclusion complexes of clove essential oil (CEO) and its main component eugenol (Eug). Ethanol injection method and membrane contactor were applied to prepare liposomes at laboratory and large scale, respectively. Various liposomal formulations were tested: (1) free hydroxypropyl-β-cyclodextrin loaded liposomes; (2) drug in hydroxypropyl-β-cyclodextrin in liposomes (DCL); (3) DCL2 obtained by double loading technique, where the drug is added in the organic phase and the inclusion complex in the aqueous phase. Liposomes were characterized for their particle size, polydispersity index, Zeta potential, morphology, encapsulation efficiency of CEO components and Eug loading rate. Reproducible results were obtained with both injection devices. Compared to Eug-loaded liposomes, DCL and DCL2 improved the loading rate of Eug and possessed smaller vesicles size. The DPPH(•) scavenging activity of Eug and CEO was maintained upon incorporation of Eug and CEO into DCL and DCL2. Contrary to DCL2, DCL formulations were stable after 1 month of storage at 4°C and upon reconstitution of the dried lyophilized cakes. Hence, DCL in aqueous and lyophilized forms, are considered as a promising carrier system to preserve volatile and hydrophobic drugs enlarging their application in cosmetic, pharmaceutical and food industries.
authors.affiliation: Bioactive Molecules Research Group, Faculty of Sciences, Doctoral School of Sciences and Technologies, Lebanese University, B.P. 90656 Jdaidet el-Matn, Lebanon; Laboratoire d'Automatique et de Génie des Procédés (LAGEP), UMR-CNRS 5007, Université Claude Bernard Lyon 1, CPE Lyon, Bat 308G, 43 Boulevard du 11 Novembre 1918, F-69622 Villeurbanne Cedex, France.
authors.forename: Carine
authors.initials: C
authors.lastname: Sebaaly
authors.affiliation: Laboratoire d'Automatique et de Génie des Procédés (LAGEP), UMR-CNRS 5007, Université Claude Bernard Lyon 1, CPE Lyon, Bat 308G, 43 Boulevard du 11 Novembre 1918, F-69622 Villeurbanne Cedex, France.
authors.forename: Catherine
authors.initials: C
authors.lastname: Charcosset
authors.affiliation: Laboratoire d'Automatique et de Génie des Procédés (LAGEP), UMR-CNRS 5007, Université Claude Bernard Lyon 1, CPE Lyon, Bat 308G, 43 Boulevard du 11 Novembre 1918, F-69622 Villeurbanne Cedex, France.
authors.forename: Serge
authors.initials: S
authors.lastname: Stainmesse
authors.affiliation: Laboratoire d'Automatique et de Génie des Procédés (LAGEP), UMR-CNRS 5007, Université Claude Bernard Lyon 1, CPE Lyon, Bat 308G, 43 Boulevard du 11 Novembre 1918, F-69622 Villeurbanne Cedex, France.
authors.forename: Hatem
authors.initials: H
authors.lastname: Fessi
authors.affiliation: Bioactive Molecules Research Group, Faculty of Sciences, Doctoral School of Sciences and Technologies, Lebanese University, B.P. 90656 Jdaidet el-Matn, Lebanon. Electronic address: hgreige@ul.edu.lb.
authors.forename: Hélène
authors.initials: H
authors.lastname: Greige-Gerges
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D002626:Chemistry, Pharmaceutical; D005054:Eugenol / Q000737:chemistry; D016166:Free Radical Scavengers / Q000737:chemistry; D005612:Freeze Drying; D008081:Liposomes / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D009822:Oils, Volatile / Q000737:chemistry*; D010316:Particle Size; D016062:Porosity; D027842:Syzygium / Q000378:metabolism; D014867:Water / Q000737:chemistry; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D016166:Free Radical Scavengers; D008081:Liposomes; D009822:Oils, Volatile; D047392:beta-Cyclodextrins; D014867:Water; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D005054:Eugenol
keywords: Clove essential oil; Double loading technique; Drug in cyclodextrin in liposomes; Eugenol; Freeze-drying; Scale-up