Suitable excipient with certain characteristics is required in formulating dry powder inhaler (DPI), to deliver anti-TB drug into the lung and provide adequate drug concentration in the lung and in the alveolar macrophage, to overcome active and latent tuberculosis infection. This study aimed to explore combination of chitosan and alginate in formulating rifampicin DPI. Rifampicin DPI was prepared by spray drying using various combination of chitosan and alginate. The obtained rifampicin dry powder was characterized for its particle size distribution, morphology, moisture content, drug content, and entrapment efficiency. In addition to the dissolution study in phosphate buffer pH 7.4 with SLS 0.05% and in phthalate buffer pH 4.5, the cytotoxicity study towards cell line A549 was also conducted. Combination of chitosan and alginate in DPI F3 (RIF-Ch-Alg 2:1:1) provide suitable drug release profile of rifampicin DPI in both simulated lung fluid (78.301 ± 1.332 % in 2 hours) and in simulated macrophage fluid (41.355 ± 1.259% in 2 hours). DPI F3 also possessed aerodynamic particle size of 11.4288 ± 1.259 µm, and was also considered as safe toward pulmonary epithelial cells (viability 89.73%) in concentration up to 0.1 mg/mL. It is potential to further explore its efficiency in targeting active and latent tuberculosis in vivo.
Key words: rifampicin, dry powder inhaler, chitosan, alginate, drug release profile, cytotoxicity
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