Study by inverse gas chromatography of the solubility of rifabutin in water in the presence of cyclodextrin

Anshakova, A. V.; Konyukhov, V. Yu.

doi:10.1134/s1070427217020082

Cited by 2 publications

(1 citation statement)

References 5 publications

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“…The fact that both drugs were associated with similar efficiencies demonstrates that the process was independent of the aqueous solubility of the drugs (125 mg/mL for INH and 0.19 mg/mL for RFB) [20,21].…”

Section: Resultsmentioning

confidence: 99%

Inhalable Fucoidan Microparticles Combining Two Antitubercular Drugs with Potential Application in Pulmonary Tuberculosis Therapy

et al. 2018

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The pulmonary delivery of antitubercular drugs is a promising approach to treat lung tuberculosis. This strategy not only allows targeting the infected organ instantly, it can also reduce the systemic adverse effects of the antibiotics. In light of that, this work aimed at producing fucoidan-based inhalable microparticles that are able to associate a combination of two first-line antitubercular drugs in a single formulation. Fucoidan is a polysaccharide composed of chemical units that have been reported to be specifically recognised by alveolar macrophages (the hosts of Mycobacterium ). Inhalable fucoidan microparticles were successfully produced, effectively associating isoniazid (97%) and rifabutin (95%) simultaneously. Furthermore, the produced microparticles presented adequate aerodynamic properties for pulmonary delivery with potential to reach the respiratory zone, with a mass median aerodynamic diameter (MMAD) between 3.6–3.9 µm. The formulation evidenced no cytotoxic effects on lung epithelial cells (A549), although mild toxicity was observed on macrophage-differentiated THP-1 cells at the highest tested concentration (1 mg/mL). Fucoidan microparticles also exhibited a propensity to be captured by macrophages in a dose-dependent manner, as well as an ability to activate the target cells. Furthermore, drug-loaded microparticles effectively inhibited mycobacterial growth in vitro. Thus, the produced fucoidan microparticles are considered to hold potential as pulmonary delivery systems for the treatment of tuberculosis.

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Section: Resultsmentioning

confidence: 99%

Inhalable Fucoidan Microparticles Combining Two Antitubercular Drugs with Potential Application in Pulmonary Tuberculosis Therapy

et al. 2018

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Inhalable chitosan microparticles for simultaneous delivery of isoniazid and rifabutin in lung tuberculosis treatment

Cunha

Rodrigues

Costa

et al. 2019

Drug Development and Industrial Pharmacy

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The direct delivery of antibiotics to the lung has been considered an effective approach 19 to treat pulmonary tuberculosis, which represents approximately 80% of total cases. In 20 this sense, this work aimed at producing inhalable chitosan microparticles simultaneously associating isoniazid and rifabutin, for an application in pulmonary tuberculosis therapy. 22 Spray-dried chitosan microparticles were obtained with adequate flow properties for deep 23 lung delivery (aerodynamic diameter of 4 µm) and high drug association efficiencies 24 (93% for isoniazid and 99% for rifabutin). The highest concentration of microparticles 25 that was tested (1 mg/mL) decreased the viability of macrophage-differentiated THP-1 26 cells to around 60% after 24 h exposure, although no deleterious effect was observed in 27 human alveolar epithelial (A549) cells. The release of LDH was, however, increased in 28 both cells. Chitosan microparticles further evidenced capacity to activate macrophage-29 like cells, inducing cytokine secretion well above basal levels. Moreover, the propensity 30 of macrophages to internalise microparticles was demonstrated, with uptake levels over 31 90%. Chitosan microparticles also inhibited bacterial growth by 96%, demonstrating that 32 the microencapsulation preserved drug antibacterial activity in vitro. Overall, the obtained 33 data suggest the potential of chitosan microparticles systems for inhalable lung 34 tuberculosis therapy.

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Study by inverse gas chromatography of the solubility of rifabutin in water in the presence of cyclodextrin

Cited by 2 publications

References 5 publications

Inhalable Fucoidan Microparticles Combining Two Antitubercular Drugs with Potential Application in Pulmonary Tuberculosis Therapy

Inhalable Fucoidan Microparticles Combining Two Antitubercular Drugs with Potential Application in Pulmonary Tuberculosis Therapy

Inhalable chitosan microparticles for simultaneous delivery of isoniazid and rifabutin in lung tuberculosis treatment

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