Respirable rifampicin-based microspheres containing isoniazid for tuberculosis treatment.

摘要: Department Farmaco Chimico Tecnologico, University of Cagliari, 09124 ItalyReceived 7 June 2011; revised 30 September accepted 11 October 2011Published online in Wiley Online Library (wileyonlinelibrary.com). DOI: 10.1002/jbm.a.33302Abstract: The purpose this investigation was to developsmall microspheres for delivering antimycobacterial drugs toinfected host macrophages. Rifampicin-based microparticleswere prepared. drug covalently linked acrylic moi-eties obtain a polymerizable derivative the preparation ofmaterials useful as delivery systems that then were loadedwith isoniazid acting synergy with rifampicin. Their antituber-cular activity determined vitro. Fourier transform infraredspectroscopy confirmed hydrogel structure. Morphological anal-ysis showed microparticles spherical shape and homoge-neous surface. In vitro release studies performed mediasimulating physiologic pH (7.4) endosomal alveolar mac-rophages (5.2). A similar amount deliveredwithin first 6 h at both pHs, while smaller thedrug delivered 7.4 last phase study. Invitro antitubercular behavior comparable tothat rifampicin free. Bioactive swelling matrices,showing high degree into medium miming intra al-veolar environment, obtained. They could be applied fortheir activity.