title: Cyclodextrin and Meglumine-Based Microemulsions as a Poorly Water-Soluble Drug Delivery System.
abstract: Cyclodextrins (CDs) and meglumine (MEG) are pharmaceutical excipients widely used to improve solubility of poorly water-soluble drugs. The purpose of this work was to study the effect of CDs or MEG on the internal microstructure of soya oil-based O/W microemulsions (MEs) and on the modulation of the solubility and release rate of Class II model hydrophobic drugs, sulfamerazine and indomethacin. The pseudoternary phase diagrams revealed that higher proportions of oil phase, as well as the presence of β-cyclodextrin (ßCD), methyl-ßCD, and MEG, favored the incorporation of the drugs. The conductivity studies, particle size, and zeta potential analysis showed that the O/W ME structure remained unaffected and that the ME presented reduced droplet sizes after the incorporation of the ligands. The drug-component interactions were assessed by proton nuclear magnetic resonance studies. The highest incorporations of sulfamerazine (35.6 mg/mL) and indomethacin (73.1 mg/mL) were obtained with the ME with W = 5%, MEG and W = 1.8% ßCD in a phosphate buffer solution of pH 8, respectively. In addition, the ligands in ME significantly enhanced the released amount of the drugs, probably due to a solubilizing effect that facilitates the drug to penetrate the unstirred water layer adjacent to membranes.
authors.affiliation: Unidad de Investigación y Desarrollo en Ciencia y Tecnología Farmacéutica (UNITEFA-CONICET), Departamento de Farmacia, Facultad de Ciencias Químicas-Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina; UNESP-Universidade Estadual Paulista, Faculdade de Ciências Farmacêuticas, 14801-902 Araraquara, SP, Brazil.
authors.forename: Carolina
authors.initials: C
authors.lastname: Aloisio
authors.affiliation: UNESP-Universidade Estadual Paulista, Faculdade de Ciências Farmacêuticas, 14801-902 Araraquara, SP, Brazil.
authors.forename: Anselmo
authors.initials: A
authors.lastname: G de Oliveira
authors.affiliation: Unidad de Investigación y Desarrollo en Ciencia y Tecnología Farmacéutica (UNITEFA-CONICET), Departamento de Farmacia, Facultad de Ciencias Químicas-Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina. Electronic address: mrlcor@fcq.unc.edu.ar.
authors.forename: Marcela
authors.initials: M
authors.lastname: Longhi
mesh_terms: D000465:Algorithms; D016503:Drug Delivery Systems; D004553:Electric Conductivity; D004655:Emulsions / Q000737:chemistry*; D005079:Excipients; D007213:Indomethacin / Q000737:chemistry; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D008536:Meglumine / Q000737:chemistry*; D008958:Models, Molecular; D010316:Particle Size; D012995:Solubility; D013416:Sulfamerazine / Q000737:chemistry; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D004655:Emulsions; D005079:Excipients; D047392:beta-Cyclodextrins; C108732:methyl-beta-cyclodextrin; D008536:Meglumine; D013416:Sulfamerazine; D007213:Indomethacin
keywords: cyclodextrin; meglumine; microemulsion; release; solubilization