title: Oil-in-water lecithin-based microemulsions as a potential delivery system for amphotericin B.
abstract: In this work the structural features of microemulsions (MEs) containing the pharmaceutical biocompatible Soya phosphatidylcholine/Tween 20 (1:1) as surfactant (S), Captex 200 as oil phase (O), and phosphate buffer 10mM, pH 7.2 as aqueous phase (W) were studied. Systems obtained with different proportions of the components were described by pseudo-ternary phase diagrams in order to characterize the microemulsions studied here. MEs were prepared with and without the polyene antifungal drug amphotericin B (AmB). The maximum AmB incorporation into the ME system was dependent on both the oil phase and surfactant proportions with 6.80 and 5.7 mg/mL in high contents, respectively. The incorporation of AmB into the ME systems significantly increased the profile of the droplet size of the ME for all ranges of surfactant proportions used in the formulations. The microstructures of the system were characterized by dynamic light scattering (DLS) and rheological behavior. The DLS results showed that the size of the oil droplets increases 4.6-fold when AmB is incorporated into the ME system. In all cases the increase in the proportion of the oil phase of the ME leads to a slight increase in the diameter of the oil droplets of the system. Furthermore, for both the AmB-loaded and AmB-unloaded MEs, the size of the oil droplets decrease significantly with the increase of the S proportion in the formulations, demonstrating the efficiency of the surfactant in stabilizing the ME. Depending on the ME composition, an anti-thixotropic behavior was found. The maximum increases of the consistency index caused by the increase of the oil phase of the ME were of 17- and 25-times for the drug-loaded and drug-unloaded MEs, respectively. However, the observed effect for the drug-loaded ME was about 4.6 times higher than that for the drug-unloaded one, demonstrating the strong effect of the drug on the rheological characteristics of the ME system. Therefore, it is possible to conclude that the investigated ME can be used as a very promising vehicle for AmB.
authors.affiliation: Departamento de Fármacos e Medicamentos, Faculdade de Ciências Farmacêuticas, UNESP, Rodovia Araraquara-Jaú km 01, Araraquara, SP, Brazil.
authors.forename: K C
authors.initials: KC
authors.lastname: Pestana
authors.forename: T P
authors.initials: TP
authors.lastname: Formariz
authors.forename: C M
authors.initials: CM
authors.lastname: Franzini
authors.forename: V H V
authors.initials: VH
authors.lastname: Sarmento
authors.forename: L A
authors.initials: LA
authors.lastname: Chiavacci
authors.forename: M V
authors.initials: MV
authors.lastname: Scarpa
authors.forename: E S T
authors.initials: ES
authors.lastname: Egito
authors.forename: A G
authors.initials: AG
authors.lastname: Oliveira
mesh_terms: D000666:Amphotericin B / Q000737:chemistry*; D002210:Caprylates / Q000737:chemistry*; D016503:Drug Delivery Systems; D004655:Emulsions; D054709:Lecithins / Q000737:chemistry*; D008027:Light; D008968:Molecular Conformation; D009821:Oils / Q000737:chemistry*; D010316:Particle Size; D010710:Phosphates / Q000737:chemistry; D010713:Phosphatidylcholines / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry*; D011136:Polysorbates / Q000737:chemistry; D012542:Scattering, Radiation; D013025:Glycine max / Q000737:chemistry; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry; D014867:Water / Q000737:chemistry
chemical_list: D002210:Caprylates; D004655:Emulsions; D054709:Lecithins; D009821:Oils; D010710:Phosphates; D010713:Phosphatidylcholines; D011136:Polysorbates; D013501:Surface-Active Agents; D014867:Water; D011092:Polyethylene Glycols; D000666:Amphotericin B