Nanoencapsulation of Antitubercular Drug Isoniazid and Its Lipopeptide Conjugate

• Published in: Journal of dispersion science and technology Vol. 32; no. 12; pp. 1728 - 1734
• Main Authors: Kiss, É., Schnöller, D., Pribranská, K., Hill, K., Pénzes, Cs. B., Horváti, K., Bősze, Sz
• Format: Journal Article Conference Proceeding
• Language: English
• Published: Philadelphia, PA Taylor & Francis Group 01.12.2011; Taylor & Francis; Taylor & Francis Ltd
• Subjects: Antituberculotic drug conjugate; Cellular; Chemistry; Colloidal state and disperse state; Conjugates; Dispersions; drug encapsulation; Drugs; Exact sciences and technology; General and physical chemistry; Hydrophobicity; Lipids; membrane affinity; Membranes; Nanoparticles; nanoprecipitation; Nanostructure; Peptides; Physical and chemical studies. Granulometry. Electrokinetic phenomena; PLGA nanoparticles; Water; Encapsulation; Monolayer; Peptides; Nanoparticle; Octanol; nanoprecipitation; Lipids; Partition coefficient; Hydrophobicity; Antituberculotic drug conjugate; Design; Synthesis; Glycolic acid; Bacteria; Membrane; Chemical composition; Drug; membrane affinity; Bioavailability; Hydrophily; Treatment; Mycobacterium tuberculosis; Mycobacteriales; drug encapsulation; Mycobacteriaceae; Affinity; Actinomycetes; Models; PLGA nanoparticles; Physicochemical properties
• ISSN: 0193-2691; 1532-2351
• DOI: 10.1080/01932691.2011.616128

Isoniazid (INH) is a first line drug for treatment of the widespread deadly disease caused by Mycobacterium tuberculosis. Peptide conjugate of INH was designed and synthesised for targeted and receptor mediated cellular uptake of INH. Chemical composition, hydrophobicity (n-octanol/water partition coefficient), and membrane affinity (using a Langmuir lipid monolayer as a model system) of the conjugate were characterised. Hydrophilicity of the drug was remarkably decreased by the conjugation which resulted in improved interaction with lipid layer and allowed its efficient encapsulation into polylactic/glycolic acid nanoparticles enhancing the bioavailability of the drug.