title: Antimycobacterial activity of 2-phenoxy-1-phenylethanone, a synthetic analogue of neolignan, entrapped in polymeric microparticles.
abstract: Conventional treatment of tuberculosis (TB) demands a long course therapy (6 months), known to originate multiple drug resistant strains (MDR-TB), which emphasizes the urgent need for new antituberculous drugs. The purpose of this study was to investigate a novel treatment for TB meant to improve patient compliance by reducing drug dosage frequency. Polymeric microparticles containing the synthetic analogue of neolignan, 1-phenyl-2-phenoxiethanone (LS-2), were obtained by a method of emulsification and solvent evaporation and chemically characterized. Only representative LS-2-loaded microparticles were considered for further studies involving experimental murine TB induced by Mycobacterium tuberculosis H37Rv ATCC 27294. The LS-2-loaded microparticles were spherical in shape, had a smooth wall and showed an encapsulation efficiency of 93% in addition to displaying sustained release. Chemotherapeutic potential of LS-2 entrapped in microparticles was comparable to control groups. These findings are encouraging and indicate that LS-2-loaded microparticles are a potential alternative to conventional chemotherapy of TB.
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo , Ribeirão Preto, SP, Brazil.
authors.forename: Paulo R R
authors.initials: PR
authors.lastname: Minarini
authors.forename: Ana O
authors.initials: AO
authors.lastname: de Souza
authors.forename: Edson G
authors.initials: EG
authors.lastname: Soares
authors.forename: Lauro E S
authors.initials: LE
authors.lastname: Barata
authors.forename: Célio L
authors.initials: CL
authors.lastname: Silva
authors.forename: Maria Vitória L B
authors.initials: MV
authors.lastname: Bentley
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage*; D001672:Biocompatible Materials; D004195:Disease Models, Animal; D004337:Drug Carriers; D024881:Drug Resistance, Bacterial; D006801:Humans; D019344:Lactic Acid; D017705:Lignans / Q000008:administration & dosage*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008863:Microspheres; D023421:Models, Animal; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D010316:Particle Size; D010349:Patient Compliance; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D013997:Time Factors; D014397:Tuberculosis, Pulmonary / Q000188:drug therapy*
chemical_list: C561330:2-phenoxy-1-phenylethanone; D000900:Anti-Bacterial Agents; D001672:Biocompatible Materials; D004337:Drug Carriers; D017705:Lignans; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid