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Optimization, characterization, and cytotoxicity studies of novel anti-tubercular agent-loaded liposomal vesicles
Manar M Obiedallah1,2, Maxim A Mironov3, Danila V Belyaev4,5
1Institute of Chemical Technology, Ural Federal University, Yekaterinburg, Russia. m.mh.obid@gmail.com.
Abstract:
The treatment of tuberculosis is still a challenging process due to the widespread 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. Several factors that affect liposomal characteristics were studied. The maximum encapsulation efficiency was 53.62 ± 0.09. The selected liposomal formulation T8* possessed a mean particle size of 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 I was increased by its incorporation in liposomes. The free compound and liposomal preparation showed antimycobacterial activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) at MIC value 0.94-1.88 μg/ml. We predict that the liposomes may be a good candidate for delivering new antitubercular drugs.
Insights
Researchers developed novel liposomes encapsulating a new antimycobacterial imidazo-tetrazine compound. This liposomal drug delivery system enhanced compound solubility and demonstrated potent activity against Mycobacterium tuberculosis.
Area of Science:
- Pharmaceutical Sciences
- Medicinal Chemistry
- Nanotechnology
Background:
- Tuberculosis treatment faces challenges due to drug-resistant strains and adverse effects.
- Novel antitubercular agents and effective drug delivery systems are urgently needed.
Purpose of the Study:
- To develop and characterize liposomal vesicles containing a newly synthesized imidazo-tetrazine derivative with antimycobacterial properties.
- To evaluate the efficacy of the liposomal formulation as a drug delivery system for tuberculosis treatment.
Main Methods:
- Synthesis of a novel imidazo-tetrazine compound (3-(3,5-dimethylpyrazole-1-yl)-6-(isopropylthio) imidazo [1,2-b] [1,2,4,5] tetrazine).
- Formulation and characterization of liposomal vesicles, including encapsulation efficiency, particle size, polydispersity index (PDI), and zeta potential.
- In vitro release studies to assess compound solubility.
- Antimycobacterial activity testing against Mycobacterium tuberculosis H37Rv.
Main Results:
- Maximum encapsulation efficiency of 53.62% ± 0.09%.
- Selected liposomal formulation (T8*) exhibited a particle size of 205.3 ± 3.94 nm, PDI of 0.282, and zeta potential of +36.37 ± 0.49 mV.
- Liposomal incorporation significantly increased the solubility of the studied compound.
- Both free compound and liposomal preparation showed significant antimycobacterial activity with a minimum inhibitory concentration (MIC) of 0.94-1.88 μg/ml.
Conclusions:
- Liposomes are a promising nanocarrier system for delivering novel antitubercular agents.
- The developed liposomal formulation enhances compound solubility and retains antimycobacterial efficacy.
- Further investigation into liposomes for tuberculosis drug delivery is warranted.
