title: Improvement of in vitro efficacy of a novel schistosomicidal drug by incorporation into nanoemulsions.
abstract: The aim of this article included the development and evaluation of the capacity of nanoemulsions to improve the activity of the novel schistosomicidal drug-2-(butylamino)-1-phenyl-1-ethanethiosulfuric acid (BphEA). BphEA is a compound with a poor solubility in water, which makes its application as a drug difficult. Nanoemulsion formulations presenting anionic (NANOSTOA, NANOST and NANOLP) and cationic (NANOSTE) interfacial charges were prepared to encapsulate BphEA. These formulations were characterized by the encapsulation rate, diameter, and zeta potential. NANOSTOA, NANOST, and NANOLP presented an entrapment efficiency and zeta potential of 18.7+/-1.8% and -33.6+/-1.2 mV; 20.5+/-3.0% and -31.5+/-5.7 mV; as well as 33.8+/-7.2% and -62.6+/-1.3 mV, respectively. NANOSTE presented an entrapment efficiency of 51.8+/-5.0% and a zeta potential of 25.7+/-3.9 mV. The mean droplet size (between 200 and 252 nm) and polydispersity index (between 0.158 and 0.294) were similar for all formulations. The stability study showed no alteration in these formulations' zeta potential and size. The in vitro schistosomicidal activity of BphEA was higher with the use of NANOSTE than with free BphEA. In addition, release studies revealed a good stability of NANOSTE containing BphEA in a biological medium. These results indicate that cationic nanoemulsions can represent an interesting delivery system for the pharmaceutical formulation of BphEA.
authors.affiliation: Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Av. Antônio Carlos 6627, 31270-901 Belo Horizonte, MG, Brazil.
authors.forename: Sávia Caldeira
authors.initials: SC
authors.lastname: de Araújo
authors.forename: Ana Carolina Alves
authors.initials: AC
authors.lastname: de Mattos
authors.forename: Helder Ferreira
authors.initials: HF
authors.lastname: Teixeira
authors.forename: Paulo Marcos Zech
authors.initials: PM
authors.lastname: Coelho
authors.forename: David Lee
authors.initials: DL
authors.lastname: Nelson
authors.forename: Mônica Cristina
authors.initials: MC
authors.lastname: de Oliveira
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D004655:Emulsions; D007700:Kinetics; D008055:Lipids / Q000737:chemistry*; D008566:Membranes / Q000187:drug effects; D053758:Nanoparticles; D021261:Parasitic Sensitivity Tests; D010316:Particle Size; D012550:Schistosoma mansoni / Q000187:drug effects; D012556:Schistosomicides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D012995:Solubility; D013463:Sulfuric Acid Esters / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014867:Water / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D004655:Emulsions; D008055:Lipids; D012556:Schistosomicides; D013463:Sulfuric Acid Esters; D014867:Water