Background: By applying controlled release nanotechnology the dosing frequency,
high doses and side effects of anti-tubercular drugs may be reduced and patient compliance
can be achieved, preventing resistance of mycobacterium tuberculosis.
Objective: The aim of this research work was the formulation, optimization and characterization
of D-Cycloserine, a second-line anti-tubercular drug loaded PLGA nanoparticles for the
better management of multi-drug resistant tuberculosis.
Method: D-Cycloserine loaded PLGA nanoparticles were prepared by a modified double
emulsion solvent evaporation method and characterized. The optimization of these nanoparticles
was done with 23
factorial designs of experiments using Design Expert®
V9. The entrapment
of drug in the nanoparticulate matrix was confirmed by differential scanning calorimetry,
Fourier transform infrared and x-ray diffraction analysis. Particle morphology was determined
by scanning electron microscopy.
Results: The entrapment efficiency of 87.52 ±0.42% and drug loading of 40.70 ±0.22% was
observed for the optimized batch of nanoparticles. These nanoparticles also showed 192 ±4
nm of particle size, 74 ±4 nm of particle size’s standard deviation and -24±6.35mV of zeta
potential respectively. The smooth and spherical shaped particles were measured by scanning
electron microscopy. The nanoparticles showed a sustained release up to 48 hours and 79.01
±0.5% of respirable fraction.
Conclusion: These results showed that the modified double emulsion solvent evaporation
method can be utilized to make nanoparticles suitable for lung deposition having high entrapment
efficiency, drug loading and optimum particle size with controlled release characteristics.
Thus, these nanoparticles can be used as an efficient carrier system for the D-Cycloserine and
possess a potential for better management of multi-drug resistant tuberculosis.