Evaluation of antitubercular drug-loaded surfactants as inhalable drug-delivery systems for pulmonary tuberculosis

Autor: Rangan Banerjee, G. Chimote
Rok vydání: 2009
Předmět:
Zdroj: Journal of Biomedical Materials Research Part A. :281-292
ISSN: 1552-4965
1549-3296
DOI: 10.1002/jbm.a.31959
Popis: Pulmonary tuberculosis is associated with a year-long chemotherapy, poor alveolar drug levels, drug-related systemic toxicity, and patient noncompliance. In this study, exogenous pulmonary surfactant is proposed as a drug carrier for antitubercular drugs. Dipalmitoylphosphatidylcholine (DPPC), the major lung-surfactant lipid, has been combined with antitubercular drugs isoniazid (INH), rifampicin (RFM), and ethambutol (ETH) in 1:1 ratio by weight, in which drugs had a ratio of 1:2:3 by weight. At 37°C, the formulation had better surfactant function with quicker reduction of surface tension on adsorption (32.71 ± 0.65 mN/m) than DPPC liposomes (44.67 ± 0.57 mN/m) and maintained 100% airway patency in a capillary surfactometer. Drug-loaded surfactant liposomes were about 2 μm and had entrapment efficiency of 30.04% ± 2.05%, 18.85% ± 2.92%, and 61.47% ± 3.32% for INH, RFM, and ETH, respectively. Sustained release of the drugs from surfactants was observed over 24 h. In vitro alveolar deposition efficiency using the twin impinger showed 12.06% ± 1.87% of INH, 43.30% ± 0.87% of RFM, and 22.07% ± 2.02% of ETH deposited in the alveolar chamber upon nebulization for a minute using a jet nebulizer. The formulation was biocompatible and stable with physicochemical properties being retained even after storage for a month at 4°C. Antitubercular drug-loaded surfactants developed could serve dual purposes of alveolar stabilization due to surfactant action and better reach of these drugs to the alveoli due to antiatelectatic effect of the surfactant. © 2008 Wiley Periodicals, Inc. J Biomed Mater Res, 2009
Databáze: OpenAIRE