One-third of the world's population is infected with tuberculosis (TB), a disease caused by Mycobacterium tuberculosis that survives and replicates within human macrophages. TB is characterized by a long chronic stage of infection and progressive pathology that mainly compromises (90% of cases) the respiratory system (World Health Organization, 2012). The current recommended TB chemotherapy includes: isoniazid, rifampicin, ethambutol and pyrazinamide. However, patient's noncompliance, several side effects and multi-drug resistant TB infections, often make ineffective the therapy. The present research aimed to improve the effectiveness of the treatment by a non-conventional therapy and using the respiratory tract as a novel administration route for rifampicin, a first-line anti-TB drug. This approach involved the design of solid lipid microparticles (SLM) as drug delivery system (DDS) showing benefits in terms of biocompatibility, easy of preparation without organic solvents, long-term stability, low cost of materials and procedures as well as scale-up. The study dealt with the formula optimization in order to provide SLM characterized by physicochemical properties proper for the delivery by a dry powder inhaler (DPI) device, for the targeting to alveolar macrophages and for the drug intracellular activity. SLM (~1 μm) loaded with rifampicin were developed by melt emulsification technique using biocompatible lipids and surfactants. They exhibited suitable breathability, negative surface charge promoting the uptake by the alveolar macrophages, good drug loading level, ability to be taken up by macrophage cell lines and antibiotic intracellular activity. Therefore, the lipid microcarrier proposed could be considered a promising DDS in a perspective of an inhaled therapy for the treatment of TB infection.
Inhaled lipid microcarrier for rifampicin intracellular delivery in tuberculosis treatment / Iannuccelli, Valentina. - In: CLINICAL PHARMACOLOGY & BIOPHARMACEUTICS. - ISSN 2167-065X. - STAMPA. - 3(2014), pp. 83-83. ((Intervento presentato al convegno 2nd International Summit on Clinical Pharmacy tenutosi a San Francisco, CA, USA nel 2-3 dicembre 2014.
|Data di pubblicazione:||2014|
|Titolo:||Inhaled lipid microcarrier for rifampicin intracellular delivery in tuberculosis treatment|
|Rivista:||CLINICAL PHARMACOLOGY & BIOPHARMACEUTICS|
|Titolo del libro:||Proceedings of 2nd International Summit on Clinical Pharmacy|
|Citazione:||Inhaled lipid microcarrier for rifampicin intracellular delivery in tuberculosis treatment / Iannuccelli, Valentina. - In: CLINICAL PHARMACOLOGY & BIOPHARMACEUTICS. - ISSN 2167-065X. - STAMPA. - 3(2014), pp. 83-83. ((Intervento presentato al convegno 2nd International Summit on Clinical Pharmacy tenutosi a San Francisco, CA, USA nel 2-3 dicembre 2014.|
|Tipologia||Abstract in Rivista|
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