title: Design of Magnetic Polymeric Particles as a Stimulus-Responsive System for Gastric Antimicrobial Therapy.
abstract: The treatment of peptic ulcers induced by H. pylori remains challenging due to the deep mucous layer location of bacteria preventing antimicrobial drug access. The present work aimed to design and evaluate in vitro dual responsive (both pH and magnetic field-sensitive) polymeric magnetic particles loaded with amoxicillin as a smart drug carrier for deep mucous layer penetration and in situ drug release. Magnetite particles were produced by the co-precipitation method and subsequently coated with the Eudragit®S100 and amoxicillin by using the spray-drying technique. The physicochemical characterization of the obtained particles was carried out by optical and scanning electron microscopy, X-ray powder diffraction, Fourier transform infrared spectroscopy, nitrogen adsorption/desorption isotherms, and vibrating sample magnetometry. Additionally, drug release tests and antibacterial activity tests were evaluated in vitro. Microparticles presented 17.2 ± 0.4 μm in size and their final composition was 4.3 ± 1.5% of amoxicillin, 87.0 ± 2.3% of Eudragit, and 9.0 ± 0.3% of magnetite. They were both pH and magnetic field responsive while presenting antimicrobial activity. On one side, magnetic field responsiveness of particles is expected to prompt them to reach bacterium niche in deep mucous layer by means of magnetic forces. On the other side, pH responsiveness is expected to enable drug release in the neutral pH of the deep mucous layer, preventing undesired delivery in the acidic gastric lumen. Smart microparticles were designed presenting both pH and magnetic field responsiveness as well as antimicrobial activity. These may be promising assets for peptic ulcer treatment.
authors.affiliation: Departamento de Análises de Produtos e Ambiente, Setor de Análise de Medicamentos, Laboratório Central Dr. Almino Fernandes, Natal, RN, Brazil.|Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Natal, RN, Brazil.
authors.forename: Erica L
authors.initials: EL
authors.lastname: Silva-Freitas
authors.affiliation: Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Natal, RN, Brazil.
authors.forename: Thales R F
authors.initials: TRF
authors.lastname: Pontes
authors.affiliation: Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Natal, RN, Brazil.
authors.forename: Rafael P
authors.initials: RP
authors.lastname: Araújo-Neto
authors.affiliation: Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Natal, RN, Brazil.
authors.forename: Ítalo H M
authors.initials: ÍHM
authors.lastname: Damasceno
authors.affiliation: Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Natal, RN, Brazil.
authors.forename: Kátia L
authors.initials: KL
authors.lastname: Silva
authors.affiliation: Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Natal, RN, Brazil.
authors.forename: Juliana F
authors.initials: JF
authors.lastname: Carvalho
authors.affiliation: Departamento de Cirurgia, Universidade Federal do Rio Grande do Norte, Natal, RN, Brazil.
authors.forename: Aldo C
authors.initials: AC
authors.lastname: Medeiros
authors.affiliation: Departamento de Física Teórica e Experimental, Universidade Federal do Rio Grande do Norte, UFRN, Avenida Senador Salgado Filho, 3000, 59078-970, Natal, RN, Brazil.
authors.forename: Rodolfo B
authors.initials: RB
authors.lastname: Silva
authors.affiliation: Laboratoire Matière et Systèmes Complexes, UMR 7057, CNRS, Université Paris Diderot, Paris, France.
authors.forename: Amanda K A
authors.initials: AKA
authors.lastname: Silva
authors.affiliation: Departamento de Física Teórica e Experimental, Universidade Federal do Rio Grande do Norte, UFRN, Avenida Senador Salgado Filho, 3000, 59078-970, Natal, RN, Brazil.
authors.forename: Marco A
authors.initials: MA
authors.lastname: Morales
authors.affiliation: Departamento de Farmácia, Universidade Federal do Rio Grande do Norte, Natal, RN, Brazil.
authors.forename: Eryvaldo S T
authors.initials: EST
authors.lastname: Egito
authors.affiliation: Departamento de Física, Universidade do Estado do Rio Grande do Norte, Mossoró, RN, Brazil.
authors.forename: Ana L
authors.initials: AL
authors.lastname: Dantas
authors.affiliation: Departamento de Física Teórica e Experimental, Universidade Federal do Rio Grande do Norte, UFRN, Avenida Senador Salgado Filho, 3000, 59078-970, Natal, RN, Brazil. ascarrico@gmail.com.
authors.forename: Artur S
authors.initials: AS
authors.lastname: Carriço
mesh_terms: D000658:Amoxicillin / Q000138:chemical synthesis* / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000494:pharmacology; D004339:Drug Compounding / Q000379:methods; D005765:Gastrointestinal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D016480:Helicobacter pylori / Q000187:drug effects; D060328:Magnetic Phenomena; D008855:Microscopy, Electron, Scanning / Q000379:methods; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D004337:Drug Carriers; D005765:Gastrointestinal Agents; D011108:Polymers; D000658:Amoxicillin
keywords: antimicrobial activity; drug delivery; magnetite; smart microsystems; spray drier