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Isoniazid Loaded PCL-PEG Copolymer Nanoparticles for Sustained Release Application.

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Pharmaceutical Sciences

Background:

  • Tuberculosis remains a global health threat, with isoniazid treatment causing significant side effects like neurotoxicity and liver damage.
  • Developing safer drug delivery systems for first-line anti-tuberculosis drugs is crucial.

Purpose of the Study:

  • To create sustained-release isoniazid nanoparticles using a PCL-PEG copolymer to mitigate adverse effects.
  • To optimize and characterize these novel drug delivery systems.

Main Methods:

  • Synthesis and characterization of PCL-PEG copolymer.
  • Preparation of isoniazid-loaded nanoparticles (Inp) via double emulsion solvent evaporation.
  • Optimization using a 2^3 half factorial design and comprehensive characterization (drug loading, entrapment efficiency, particle size, zeta potential, in vitro release, morphology, FTIR, DSC, PXRD, stability).

Main Results:

  • Optimized nanoparticles demonstrated high entrapment efficiency and drug loading.
  • All formulations exhibited sustained isoniazid release over 5 days (60.26-88.59%).
  • Inp F13 showed sustained drug release and maintained inhibitory activity against Mycobacterium tuberculosis for 15 days, compared to 4 days for plain isoniazid.

Conclusions:

  • The optimal isoniazid-loaded PCL-PEG nanoparticles were achieved with a 95:5 PCL:PEG ratio, 0.5% PVA, and 3 mg initial drug loading.
  • These nanoparticles facilitate controlled, sustained release of isoniazid, offering a promising approach to reduce drug toxicity.