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Purpose <p>Tuberculosis (TB) is a major cause of mortality worldwide. The most commonly used first-line anti-TB drugs in the treatment of TB are rifampicin and isoniazid. This research aimed to formulate and evaluate the anti-mycobacterium activity of isoniazid (INH) nano capsules against mycobacterium isolates (<i>M. smegmatis</i> and <i>M. bovis</i>).</p> Methods <p>Lecithin was extracted from locally sourced soybean (<i>Glycine max</i>) by aqueous degumming method. Nanoparticles of INH were prepared by mechanical dispersion method. Chitosan was dispersed in 100&#xa0;mL of acetic acid solution in distilled water overnight. Sodium tripolyphosphate (STPP) was dissolved in 10&#xa0;mL of distilled water, and added to the chitosan dispersion and stirred using magnetic stirrer at 100&#xa0;rpm for 30&#xa0;min. The chitosan/STPP solution and Labrasol® (0.2%), was then added to the organic solution in drops using a syringe and stirred at 10,000&#xa0;rpm for 45&#xa0;min using Ultra-turax homogenizer. Subsequently, the precipitate formed was collected after 3&#xa0;h by centrifugation at 4000&#xa0;rpm<i>.</i> Nanoparticles obtained were adsorbed by mixing with Neusilin® (0.5%) to form powdered products. Preformulation studies were done using Fourier Transform Infra-Red (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC) and Design Expert®. The nano formulations were characterized for particle size using zeta sizer, morphology by scanning electron microscopy (SEM), thermal properties, entrapment efficiency (EE) and in vitro release.</p> Results <p>The percentage yield of the extracted lecithin ranged from 31.0 ± 0.31% to 35.0 ± 0.32%. The DSC thermograph of pure INH was 168.0&#xa0;°C. The drug content of INH formulation with extracted lecithin (IEL) and isoniazid formulation with reference lecithin (IRL) ranged from 96.4 ± 0.29% to 93.5 ± 0.94% respectively. Encapsulation efficiency for both IEL and IRL were 95.40 ± 0.37% and 95.70 ± 0.10% respectively. INH nano capsule formulations showed significantly (<i>p</i> &lt; 0.05) lower MICs (0.03&#xa0;μg/mL) than the reference commercial nano capsule (0.05 and 0.10&#xa0;μg/mL) against <i>M. smegmatis</i> and <i>M. bovis</i> isolates, respectively.</p> Conclusion <p>The mycobacterium assay verified that the INH nano capsules had higher potential of activity against the mycobacterial isolates than the conventional nanocapsules. The higher activity may be attributed to increased permeation of the bacterial cell wall, because Labrasol® was used as a permeation enhancer.</p>

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Formulation, In Vitro Characterization and Anti-Tuberculosis Investigation of Isoniazid NANOCAPSULES.

  • 期刊论文

  • 发表日期：

    2025年7月5日

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  • Chekwube A. Ezegbe,
  • Chukwuemeka C. Mbah,
  • Amarachi G. Ezegbe,
  • Ifeanyi S. Ofoefule,
  • EZINNE C. OKORAFOR

摘要

Purpose

Tuberculosis (TB) is a major cause of mortality worldwide. The most commonly used first-line anti-TB drugs in the treatment of TB are rifampicin and isoniazid. This research aimed to formulate and evaluate the anti-mycobacterium activity of isoniazid (INH) nano capsules against mycobacterium isolates (M. smegmatis and M. bovis).

Methods

Lecithin was extracted from locally sourced soybean (Glycine max) by aqueous degumming method. Nanoparticles of INH were prepared by mechanical dispersion method. Chitosan was dispersed in 100 mL of acetic acid solution in distilled water overnight. Sodium tripolyphosphate (STPP) was dissolved in 10 mL of distilled water, and added to the chitosan dispersion and stirred using magnetic stirrer at 100 rpm for 30 min. The chitosan/STPP solution and Labrasol® (0.2%), was then added to the organic solution in drops using a syringe and stirred at 10,000 rpm for 45 min using Ultra-turax homogenizer. Subsequently, the precipitate formed was collected after 3 h by centrifugation at 4000 rpm. Nanoparticles obtained were adsorbed by mixing with Neusilin® (0.5%) to form powdered products. Preformulation studies were done using Fourier Transform Infra-Red (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC) and Design Expert®. The nano formulations were characterized for particle size using zeta sizer, morphology by scanning electron microscopy (SEM), thermal properties, entrapment efficiency (EE) and in vitro release.

Results

The percentage yield of the extracted lecithin ranged from 31.0 ± 0.31% to 35.0 ± 0.32%. The DSC thermograph of pure INH was 168.0 °C. The drug content of INH formulation with extracted lecithin (IEL) and isoniazid formulation with reference lecithin (IRL) ranged from 96.4 ± 0.29% to 93.5 ± 0.94% respectively. Encapsulation efficiency for both IEL and IRL were 95.40 ± 0.37% and 95.70 ± 0.10% respectively. INH nano capsule formulations showed significantly (p < 0.05) lower MICs (0.03 μg/mL) than the reference commercial nano capsule (0.05 and 0.10 μg/mL) against M. smegmatis and M. bovis isolates, respectively.

Conclusion

The mycobacterium assay verified that the INH nano capsules had higher potential of activity against the mycobacterial isolates than the conventional nanocapsules. The higher activity may be attributed to increased permeation of the bacterial cell wall, because Labrasol® was used as a permeation enhancer.