Affiliation:
1. MAEER’S Maharashtra Institute of Pharmacy, S. No. 124, MIT Campus, Paud Road, Kothrud, Pune,
Maharashtra, 411038, India
2. Lakshmi Narain College of Pharmacy, Raisen Road, Kalchuri
Nagar, Bhopal, Madhya Pradesh, 461062, India
Abstract
Background:
Tuberculosis (TB) is still a major cause of death worldwide, despite
possibly curable therapies. Neurotoxicity, optic neuritis, and severe liver damage
are side effects of isoniazid, a powerful first-line anti-TB drug.
Objective:
We investigated the use of PCL-PEG copolymer to sustain the release of isoniazid
to reduce its adverse effects.
Methods:
In the present work, PCL-PEG copolymer was synthesized and characterized.
Isoniazid-loaded nanoparticles (Inp) were prepared using a PCL-PEG copolymer. Furthermore,
a 23 half factorial design was employed for the optimization of drug and emulsifier
concentration in Inp. Full characterization of the nanoparticles was performed in
terms of drug loading, entrapment efficiency, particle size, zeta potential, and in vitro
drug release. The morphology, FTIR, DSC, and PXRD evaluation of the optimized Batch
Inp F13 were studied. Stability was evaluated by storing the freeze-dried Inp F13 at various
temperatures.
Results:
The entrapment efficiency and drug loading of nanoparticles prepared by double
emulsion solvent evaporation were found to be the highest. The release study revealed
that all batches of nanoparticles exhibited sustained drug release (60.26 - 88.59%) for 5
days. The cytotoxicity study conducted on Mycobacterium tuberculosis revealed a gradual
release of isoniazid from Inp, reaching the maximum (on the 15th day) compared to
plain isoniazid (on the 4th day). At 0.8 μg/mL concentration, the inhibitory activity of Inp
F13 was maintained for 15 days, indicating sustained release of isoniazid.
Conclusion:
The nanoparticles having PCL:PEG in a 95:5 ratio, with 0.5% PVA and initial
drug loading of 3 mg, produced the optimum batch. Isoniazid-loaded PCL-PEG nanoparticles
allowed controlled (sustained) release of isoniazid.
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology (medical),Infectious Diseases,Drug Discovery
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