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Surface-Engineered Ethambutol-Loaded Nanoparticles: Design, Fabrication, and In Vitro-In Vivo Evaluation for
Nimitt V Chokshi1, Jai Naik1, Vivek Bora1
1Institute of Pharmacy, Nirma Unilversity, SG Highway, Chharodi, Ahmedabad 382481, Gujarat, India.
Molecular Pharmaceutics
|December 31, 2025
Summary
This study developed mannose-conjugated solid lipid nanoparticles for oral delivery of ethylbutol, an anti-tuberculosis drug. The novel nanoparticles significantly enhanced drug bioavailability and targeted lung delivery for improved tuberculosis treatment.
Area of Science:
- Nanotechnology
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Tuberculosis (TB) poses a global health challenge, with current treatments limited by poor oral bioavailability, side effects, and noncompliance.
- Ethylbutol (ETB) is a first-line anti-TB drug facing challenges in effective oral administration.
Purpose of the Study:
- To develop and evaluate macrophage-targeted, mannose-conjugated solid lipid nanoparticles (Mn-ETB-SNs) for enhanced oral delivery of ETB.
- To improve the bioavailability and pulmonary targeting of ETB for more effective tuberculosis therapy.
Main Methods:
- Fabrication of Mn-ETB-SNs using high-pressure homogenization and surface mannosylation.
- Characterization of nanoparticles for size, ζ-potential, drug loading, entrapment efficiency, morphology, and stability.
- In vitro and in vivo studies including release, GI stability, cytotoxicity, cellular uptake, pharmacokinetics, and biodistribution.
Main Results:
- Optimized Mn-ETB-SNs showed uniform size (~491 nm), high entrapment (~84%), and stable physicochemical properties.
- Mannosylation increased macrophage uptake 2.02-fold; in vivo studies showed an 8.5-fold increase in ETB bioavailability.
- Significant lung accumulation (4.74-fold higher concentration at 48h) was observed due to mannose receptor-mediated uptake.
Conclusions:
- Orally administered Mn-ETB-SNs show promise as a nanocarrier for targeted TB therapy.
- The developed formulation improves bioavailability, enables site-specific delivery, and enhances pulmonary targeting, addressing limitations of conventional TB treatment.
