The goal of the work was to evaluate an anti-tubercular strategy based on breathable Solid Lipid Microparticles (SLM) to target alveolar macrophages and to increase the effectiveness of the conventional tuberculosis (TB) therapy. Rifampicin loaded SLM composed of stearic acid and sodium taurocholate were characterized for aerodynamic diameter, surface charge, physical state of the components, drug loading and release as well as drug biological activity on Bacillus subtilis strain. Moreover, SLM cytotoxicity and cell internalization ability were evaluated on murine macrophages J774 cell lines by MTT test, cytofluorimetry and confocal laser microscopy. SLM exhibited aerodynamic diameter proper to be transported up to the alveolar epithelium, negative charged surface able to promote uptake by the macrophages and preserved drug antimicrobial activity. The negligible in vitro release of rifampicin indicated the capacity of the microparticle matrix to entrap the drug preventing its spreading over the lung fluid. In vitro studies on J774 cell lines demonstrated SLM non-cytotoxicity and ability to be taken up by cell cytoplasm. The microparticulate carrier, showing features suitable for the inhaled therapy and for inducing endocytosis by alveolar macrophages, could be considered promising in a perspective of an efficacious TB inhaled therapy by means of a Dry Powder Inhaler device.

Inhaled Solid Lipid Microparticles to target alveolar macrophages for tuberculosis / Maretti, Eleonora; Rossi, Tiziana; Bondi, Moreno; Croce, Maria Antonietta; Hanuskova, Miriam; Leo, Eliana Grazia; Sacchetti, Francesca; Iannuccelli, Valentina. - In: INTERNATIONAL JOURNAL OF PHARMACEUTICS. - ISSN 0378-5173. - STAMPA. - 462:1-2(2014), pp. 74-82. [10.1016/j.ijpharm.2013.12.034]

Inhaled Solid Lipid Microparticles to target alveolar macrophages for tuberculosis

MARETTI, ELEONORA;ROSSI, Tiziana;BONDI, Moreno;CROCE, Maria Antonietta;HANUSKOVA, Miriam;LEO, Eliana Grazia;SACCHETTI, FRANCESCA;IANNUCCELLI, Valentina
2014

Abstract

The goal of the work was to evaluate an anti-tubercular strategy based on breathable Solid Lipid Microparticles (SLM) to target alveolar macrophages and to increase the effectiveness of the conventional tuberculosis (TB) therapy. Rifampicin loaded SLM composed of stearic acid and sodium taurocholate were characterized for aerodynamic diameter, surface charge, physical state of the components, drug loading and release as well as drug biological activity on Bacillus subtilis strain. Moreover, SLM cytotoxicity and cell internalization ability were evaluated on murine macrophages J774 cell lines by MTT test, cytofluorimetry and confocal laser microscopy. SLM exhibited aerodynamic diameter proper to be transported up to the alveolar epithelium, negative charged surface able to promote uptake by the macrophages and preserved drug antimicrobial activity. The negligible in vitro release of rifampicin indicated the capacity of the microparticle matrix to entrap the drug preventing its spreading over the lung fluid. In vitro studies on J774 cell lines demonstrated SLM non-cytotoxicity and ability to be taken up by cell cytoplasm. The microparticulate carrier, showing features suitable for the inhaled therapy and for inducing endocytosis by alveolar macrophages, could be considered promising in a perspective of an efficacious TB inhaled therapy by means of a Dry Powder Inhaler device.
2014
462
1-2
74
82
Inhaled Solid Lipid Microparticles to target alveolar macrophages for tuberculosis / Maretti, Eleonora; Rossi, Tiziana; Bondi, Moreno; Croce, Maria Antonietta; Hanuskova, Miriam; Leo, Eliana Grazia; Sacchetti, Francesca; Iannuccelli, Valentina. - In: INTERNATIONAL JOURNAL OF PHARMACEUTICS. - ISSN 0378-5173. - STAMPA. - 462:1-2(2014), pp. 74-82. [10.1016/j.ijpharm.2013.12.034]
Maretti, Eleonora; Rossi, Tiziana; Bondi, Moreno; Croce, Maria Antonietta; Hanuskova, Miriam; Leo, Eliana Grazia; Sacchetti, Francesca; Iannuccelli, V...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/992913
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