Novel Antitubercular Agent-Loaded Liposomal Vesicles: Optimization, Characterization, and Cytotoxicity Studies

Abstract The treatment of tuberculosis is still a challenging process due to the wide spread of pathogen strains resistant to antibacterial drugs, as well as the undesirable effects of anti-tuberculosis therapy. Hence, the development of safe and effective new anti-antitubercular agents in addition to suitable nanocarrier systems has become of utmost importance and necessity. Our research aims to develop liposomal vesicles that contain newly synthesized compounds with antimycobacterial action. The compound being studied is a derivative of imidazo-tetrazine named 3- (3,5-dimethylpyrazole-1-yl) -6-(isopropylthio) imidazo [1,2-b] [1, 2, 4, 5] tetrazine (compound 1). Several factors that affect the liposomal characteristics were studied. The maximum encapsulation efficiency was 53.62 ± 0.09. The selected liposomal formulation T8* possessed mean particle size about 205.3 ± 3.94 nm with PDI 0.282, and zeta potential was + 36.37 ± 0.49 mv. The results of the in vitro release study indicated that the solubility of compound 1 was increased by its incorporation in liposomes. The free compound and liposomal preparation showed antimycobacterial activity against M. tuberculosis H 37 R v (ATCC 27294) at MIC value 0.94–1.88 µg/ml. We are predicting that the liposomes may be a good candidate for delivering of new antitubercular drugs.