title: Development and characterization of repellent formulations based on nanostructured hydrogels.
abstract: Diseases caused by insects could lead to epidemic scenarios in urban areas and insect repellents are a shield against a wide range of insects, but they need to be safe without compromising efficacy. Ethyl butylacetylaminopropionate (EB) is a synthetic mosquito repellent, which could be used in products for adults and children due to its low-allergenic potential. The aim of this study was to develop and characterize EB and Poloxamer 407 nanoemulsions regarding their droplets mean size, pH, rheological properties, cytotoxicity and in vitro permeation profile. The developed formulations (F1 with 12.5% of EB and F2 with 25% of EB) were compared with a commercial formulation containing 12.5% of EB. Droplets mean size was determined by DLS, and for both nanoemulsions they were around 200 nm; however, the commercial formulation presented a droplets mean size of 10 nm, which could contribute to its high permeation. F1 and F2 presented a gel-like behavior, however F2 presented lower viscosity due to the presence of more EB between the polymer chains preventing them to interact with each other. Also, F2 was less retained by the epidermis when compared to F1 probably due to its lower viscosity. For the cytotoxicity assay only F2, which presented the highest concentration of EB was tested, and it was not toxic to the cells. This result could be also extended to F1 which presented half the EB concentration. The present study demonstrated that EB and Poloxamer 407 nanoemulsions are promising as new insect-repellent formulations.
authors.affiliation: a College of Pharmacy , Federal University of Rio de Janeiro , Rio de Janeiro , Brazil.
authors.forename: Isadora C
authors.initials: IC
authors.lastname: Pinto
authors.affiliation: b Institute of Macromolecules , Federal University of Rio de Janeiro , Rio de Janeiro , Brazil.
authors.forename: Cristal S
authors.initials: CS
authors.lastname: Cerqueira-Coutinho
authors.affiliation: a College of Pharmacy , Federal University of Rio de Janeiro , Rio de Janeiro , Brazil.
authors.forename: Elisabete Pereira
authors.initials: EP
authors.lastname: Santos
authors.affiliation: a College of Pharmacy , Federal University of Rio de Janeiro , Rio de Janeiro , Brazil.
authors.forename: Flavia A
authors.initials: FA
authors.lastname: Carmo
authors.affiliation: a College of Pharmacy , Federal University of Rio de Janeiro , Rio de Janeiro , Brazil.
authors.forename: Eduardo
authors.initials: E
authors.lastname: Ricci-Junior
mesh_terms: D000818:Animals; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D004339:Drug Compounding; D055808:Drug Discovery / Q000379:methods*; D000882:Haplorhini; D006801:Humans; D020100:Hydrogels / Q000008:administration & dosage / Q000138:chemical synthesis*; D007302:Insect Repellents / Q000008:administration & dosage / Q000138:chemical synthesis*; D049329:Nanostructures / Q000008:administration & dosage / Q000737:chemistry*; D009924:Organ Culture Techniques; D012869:Skin Absorption / Q000187:drug effects / Q000502:physiology; D013552:Swine
chemical_list: D020100:Hydrogels; D007302:Insect Repellents
keywords: Ethyl butylacetylaminopropionate; cytotoxicity; hydrogels; in vitro permeation assays; rheology