Inhaled Solid Lipid Microparticles to target alveolar macrophages for tuberculosis
| Autor: | Moreno Bondi, Valentina Iannuccelli, Eleonora Maretti, Miriam Hanuskova, Eliana Grazia Leo, Tiziana Rossi, Maria Antonietta Croce, Francesca Sacchetti |
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| Rok vydání: | 2014 |
| Předmět: |
Taurocholic Acid
Alveolar Epithelium media_common.quotation_subject Cell Antitubercular Agents Pharmaceutical Science Tuberculosis Solid Lipid Microparticles Rifampicin Inhaled therapy Pharmacology Endocytosis Cell Line Mice Drug Delivery Systems Administration Inhalation Macrophages Alveolar medicine Animals Particle Size Microparticle Internalization Cytotoxicity media_common Drug Carriers Microscopy Confocal Chemistry Dry Powder Inhalers Flow Cytometry Lipids Microspheres In vitro medicine.anatomical_structure Cell culture Biophysics Rifampin Stearic Acids Bacillus subtilis |
| Zdroj: | International Journal of Pharmaceutics. 462:74-82 |
| ISSN: | 0378-5173 |
| DOI: | 10.1016/j.ijpharm.2013.12.034 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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