Planned intervention: On Wednesday April 3rd 05:30 UTC Zenodo will be unavailable for up to 2-10 minutes to perform a storage cluster upgrade.
Published December 7, 2021 | Version v1
Journal article Open

DEVELOPMENT AND CHARACTERIZATION OF LECITHIN-BASED NANOFORMULATION FOR ENHANCED DELIVERY OF ISONIAZID IN THE TREATMENT OF TUBERCULOSIS

Description

Background: Isoniazid (INH) is a synthetic antimicrobial agent used in the treatment of tuberculosis.  It is rapidly and completely absorbed after oral administration. With the advent of nanoscience and nanotechnology, nanoparticles are able to encapsulate drugs, thus protecting them against the effect of chemical and enzymatic degradation. Objectives: To develop a low dose lecithin-based nano-formulation of isoniazid, to characterize some physiochemical properties of the isoniazid nanocapsules, to evaluate the antimycobacterial activities of the isoniazid nanoparticles against Mycobacterium isolates. Methods: INH nanocapsules were formulated by mechanical dispersion method. Preformulation studies were done using Fourier Transform Infra-red (FTIR) spectroscopy, DSC and Design Expert® version 13, Stat-Ease Inc; Minneapolis). The final products were made into tablets and enteric coated capsules using entrisic (Capsugel®). The nanoformulations were characterized for particle size using zeta sizer, morphology by scanning electron microscopy (SEM), thermal properties by Differential Scanning Calorimetry (DSC), entrapment efficiency (EE) and in vitro release. The in vitro anti-mycobacterium activities of the nanoformulations were assessed by the method of Pires et al., (2014) comparatively with commercial brands of INH tablets. Result: The isoniazid nanocapsules had a polydispersity index range from 0.294 ± 0.04 to 0.295 ± 0.04, while the particle size ranged from 106.0 ± 0.05 to 106.1 ± 0.05 nm. The encapsulation efficiency ranged from 95.4 ± 0.37 to 95.7 ± 0.10 %. The percentage drug content ranged from 93.5 ± 0.94 to 96.4 ± 0.29 %. The weight uniformity ranged from 0.25 ± 0.04 to 0.26 ± 0.04 g, while the disintegration time ranged from 12.3 ± 0.01 to 13.2 ± 0.01 min. The in vitro release studies showed that at 8 h, 80.5 % of drug was released in batch IRL, while 99.2 % of drug was released in batch IEL. The results of the antimycobacterial studies indicated that the MICs of the INH nanocapsule formulations (IEL and IRL), were 0.03 and 0.03 µg/ml against M. smegmatis and M. bovis, respectively, which were significantly (p < 0.05) lower than that of the conventional tablet (0.1 µg/ml). Conclusion: Chitosan-fortified lecithin-based nanocapsules containing INH were formulated using locally-extracted lecithin. The nanoformulations could be further developed for application in the treatment of MDR-TB.

Keywords: Isoniazid, Tuberculosis, Nanoparticles, Antimycobacterium studies, Nanotechnology.

Files

06.Ezegbe Chekwube Andrew-ISONIAZID PROJECT WORK FOR PUBLICATION 2.pdf