Enhancing antimycobacterial activity of Isoniazid and Rifampicin incorporated norbornene nanoparticles


Kumarasingam, K.; Vincent, M.; Shivshankar, R.; Mane, S.R.; Shunmugam, R.; Sivakumar, S.; Uma Devi, K.R.


International Journal of Mycobacteriology; 2018; 7(1): 84-88.   


Abstract: Background: Tuberculosis (TB) has been identified in skeletons over 6000 years old and still remains as the most prevalent infectious disease in the world; thus, there is a need for development of new drugs or tuning of old drugs. Nanotechnology, an advanced technology, plays a vital role in research for the diagnosis and treatment of TB, thus preventing adverse effects and drug resistance. The objective of this study was to enhance the antimycobacterial activity of isoniazid- (INH) and rifampicin (RIF)-incorporated norbornene (NOR) nanoparticles in comparison with plain INH and RIF without nanoparticles.


Methods: Norbornene-polyethylene glycol Isoniazid copolymer (NOR-PEG- INH) and norbornene polyethylene rifampicin Co polymer (NOR-PEG-RIF) were used for this study. The percentage of INH and RIF in NOR nanoparticles was 35% and 74%, respectively. Mycobacterium growth indicator tube containing Middlebrook 7H9 broth, the liquid medium, was used to analyze in vitro activity of the NOR-based drug and the plain drug. Minimum inhibitory concentration (MIC) of the drugs was determined from H37Rv control strain of mycobacterium TB (MTB).


Results: The dosage of INH and RIF is minimal in the combination form with the NOR nanoparticles compared to the plain INH and RIF. The results indicate that the minimum concentration of NOR-PEG-INH and NOR-PEG-RIF required inhibiting H37Rv strain of MTB was 0.05 µg/ml and 0.5 µg/ml, respectively. The results were similar to plain INH and RIF MIC.


Conclusion: Low dosage of INH and RIF along with NOR nanocarrier has similar activity to that of INH and RIF; thus this is expected to reduce adverse effects and NOR did not alter the functional activity of INH and RIF, thus becoming eligible for the newer drug carrier in TB treatment.


Keywords: Isoniazid; norbornene; rifampicin; treatment; tuberculosis

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