Antimycobacterial activity of 2-phenoxy-1-phenylethanone, a synthetic analogue of neolignan, entrapped in polymeric microparticles

Autor(es)

Minarini, Paulo R. R. ^{[1, 2, 3]} ; de Souza, Ana O. ^[4] ; Soares, Edson G. ^[5] ; Barata, Lauro E. S. ^[6] ; Silva, Celio L. ^[2] ; Bentley, Maria Vitoria L. B. ^[3]

Afiliação do(s) autor(es)

^[1] Univ Fed Sao Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Diadema, SP - Brazil

^[2] Univ Sao Paulo, Fac Med Ribeirao Preto, Dept Bioquim & Imunol, Ribeirao Preto, SP - Brazil

^[3] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, BR-14049 Ribeirao Preto, SP - Brazil

^[4] Inst Butantan, Lab Bioquim & Biofis, Sao Paulo - Brazil

^[5] Univ Sao Paulo, Fac Med Ribeirao Preto, Dept Patol, Ribeirao Preto, SP - Brazil

^[6] Univ Estadual Campinas, Inst Quim, Campinas, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY; v. 38, n. 3, p. 259-263, MAR 2012.
• Citações Web of Science: 3

Resumo

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. (AU)

• Processo FAPESP: 04/09465-7 - Laboratório multiusuário de caracterização de sistemas de liberação micro - e nanodispersos de fármacos
• Beneficiário: Maria Vitória Lopes Badra Bentley
• Modalidade de apoio: Auxílio à Pesquisa - Programa Equipamentos Multiusuários