title: The use of Eudragit RS 100/cyclodextrin nanoparticles for the transmucosal administration of glutathione.
abstract: The aim of this work was to develop and characterize new nanoparticle systems based on Eudragit RS 100 and cyclodextrins (CDs) for the transmucosal administration of glutathione (GSH). For this purpose, nanoparticles (NPs) with the mucoadhesive properties of Eudragit RS 100 and the penetration enhancing and peptide protective properties of CDs were prepared and evaluated. The quasi-emulsion solvent diffusion technique was used to prepare the NPs with natural and chemically modified (HP-beta-CD and Me-beta-CD) CDs. The NPs prepared showed homogeneous size distribution, mean diameters between 99 and 156nm, a positive net charge and spherical morphology. Solid state FT-IR, thermal analysis (DSC), and X-ray diffraction studies suggest that the nanoencapsulation process produces a marked decrease in crystallinity of GSH. The encapsulation efficiency of the peptide was found to be between 14.8% and 24%. The results indicate that mean diameters, surface charges and drug-loaded NPs were not markedly affected by the CD, whereas the presence of the latter influences drug release and to some extent peptide stability and absorption. Finally, it has been shown that CD/Eudragit RS 100 NPs may be used for transmucosal absorption of GSH without any cytotoxicity using the epithelial human HaCaT and murine monocyte macrophage RAW264.7 cell lines.
authors.affiliation: Dipartimento Farmaco-Chimico, Università degli Studi di Bari, Bari, Italy.
authors.forename: Angela
authors.initials: A
authors.lastname: Lopedota
authors.forename: Adriana
authors.initials: A
authors.lastname: Trapani
authors.forename: Annalisa
authors.initials: A
authors.lastname: Cutrignelli
authors.forename: Laura
authors.initials: L
authors.lastname: Chiarantini
authors.forename: Elena
authors.initials: E
authors.lastname: Pantucci
authors.forename: Rosa
authors.initials: R
authors.lastname: Curci
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Manuali
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Trapani
mesh_terms: D000180:Acrylic Resins / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D002460:Cell Line; D003505:Cyclodextrins / Q000008:administration & dosage* / Q000493:pharmacokinetics; D005978:Glutathione / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006736:Horses; D006801:Humans; D051379:Mice; D009092:Mucous Membrane / Q000187:drug effects* / Q000378:metabolism; D053758:Nanoparticles / Q000008:administration & dosage*; D011893:Rana esculenta; D013552:Swine; D014961:X-Ray Diffraction
chemical_list: D000180:Acrylic Resins; D003505:Cyclodextrins; C050528:Eudragit RS; D005978:Glutathione