In vitro physicochemical characterization and short term in vivo tolerability study of ethionamide loaded PLGA nanoparticles: potentially effective agent for multidrug resistant tuberculosis

Author： Kumar Gaurav Malhotra Samir Shafiq Nusrat Pandhi Promila Khuller Gopal Krishan Sharma Sadhna

Publisher： Informa Healthcare

ISSN： 1464-5246

Source： Journal of Microencapsulation, Vol.28, Iss.8, 2011-12, pp. : 717-728

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Abstract

Purpose: To achieve prolonged drug release for the treatment of multidrug resistant tuberculosis and to improve the patient compliance, ethionamide loaded PLGA nanoparticles were developed.Material and methods: They were developed by solvent evaporation method and optimized. The optimized formulation was subjected to various physico-chemical characterization, In vitro release studies and in vivo tolerability study.Results and discussion: There was no significant drug-polymer interaction and drug was encapsulated as crystalline form in nanoparticles. In vitro release was sustained up to 15 days in various media. Ethionamide loaded nanoparticles in mice did not reveal any statistically significant treatment related effects on body weight gain and clinical signs. Likewise, no treatment-related toxic effect was found in hematology, clinical chemistry and histopathology. Our results indicate the development of an orally effective safe formulation of ethionamide with sustained release property.Conclusion: Hence, ethionamide loaded nanoparticles offer excellent potential for further preclinical and clinical studies.