Nebulizable Cycloserine Loaded PLGA Nanoparticles: Formulation Design, in vitro Evaluation and Stability Studies

Author(s): Jessy Shaji, Mahmood Shaikh

Journal Name: Current Nanomedicine
(Formerly Recent Patents on Nanomedicine)

Volume 6 , Issue 3 , 2016

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Graphical Abstract:


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.

Keywords: Nanoparticles, PLGA, D-Cycloserine, inhalable, sustained release, tuberculosis.

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Article Details

Year: 2016
Published on: 11 July, 2016
Page: [219 - 239]
Pages: 21
DOI: 10.2174/2468187306666160711170333
Price: $65

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PDF: 20