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

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.

Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES Brazil)

Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES), Brazil

Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq), Brazil

Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq, Brazil)

Instituto do Milenio REDE-TB

Instituto do Milenio REDETB

Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP), Brazil

Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP, Brazil) [04/09465-7]