title: Clotrimazole-loaded Eudragit® RS100 nanocapsules: preparation, characterization and in vitro evaluation of antifungal activity against Candida species.
abstract: Clotrimazole is a common choice for the treatment of vulvovaginal infections, but its low solubility and some side effects pose a challenge to its application. This work evaluated the feasibility to formulate clotrimazole-loaded cationic nanocapsules using Eudragit® RS100 and medium chain triglycerides as polymer and oily core, respectively, by the method of interfacial deposition of a preformed polymer. The physicochemical characteristics of nanocapsule formulations were evaluated at 0 day and 60 days after preparation. Particle size, zeta potential, polydispersity index, pH and drug content were stable during this period. In addition, nanocapsules were able to protect clotrimazole from photodegradation under UV radiation. By the dialysis bag diffusion technique, the nanosized formulations showed prolonged release of clotrimazole by anomalous transport and first order kinetics. A microbiological study was carried out by the microdilution method and showed that nanocapsules (mean size: 144 nm; zeta potential: +12 mV) maintained the antifungal activity of clotrimazole against Candida albicans and Candida glabrata strains susceptible and resistant to fluconazole.
authors.affiliation: Department of Industrial Pharmacy, Federal University of Santa Maria, Santa Maria, Brazil.
authors.forename: Sara S
authors.initials: SS
authors.lastname: Santos
authors.forename: Alessandra
authors.initials: A
authors.lastname: Lorenzoni
authors.forename: Luana M
authors.initials: LM
authors.lastname: Ferreira
authors.forename: Juliane
authors.initials: J
authors.lastname: Mattiazzi
authors.forename: Andréa I H
authors.initials: AI
authors.lastname: Adams
authors.forename: Laura B
authors.initials: LB
authors.lastname: Denardi
authors.forename: Sydney H
authors.initials: SH
authors.lastname: Alves
authors.forename: Scheila R
authors.initials: SR
authors.lastname: Schaffazick
authors.forename: Letícia
authors.initials: L
authors.lastname: Cruz
mesh_terms: D000935:Antifungal Agents / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects* / Q000528:radiation effects; D003022:Clotrimazole / Q000494:pharmacology* / Q000528:radiation effects; D007700:Kinetics; D008826:Microbial Sensitivity Tests; D053769:Nanocapsules / Q000737:chemistry*; D010316:Particle Size; D011109:Polymethacrylic Acids / Q000737:chemistry*; D012996:Solutions; D055672:Static Electricity; D013535:Suspensions; D014466:Ultraviolet Rays
chemical_list: D000935:Antifungal Agents; D053769:Nanocapsules; D011109:Polymethacrylic Acids; D012996:Solutions; D013535:Suspensions; C038300:methylmethacrylate-methacrylic acid copolymer; D003022:Clotrimazole
keywords: Antifungal activity; Candida; Clotrimazole; Eudragit® RS100; Nanocapsules