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Published on: September 20, 2011
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Formulation, Characterization and Cytotoxic Effect of Indomethacin-loaded Nanoparticles
Kaan Yalçınkaya1, Behiye Şenel2, Evrim Akyıl1
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
|January 6, 2025
Summary
This study developed indomethacin-loaded polymeric nanoparticles (PNPs) and solid lipid nanoparticles (SLNs) to improve drug delivery. The developed PNP formulation demonstrated enhanced stability, prolonged release, and reduced toxicity compared to indomethacin alone.
Area of Science:
- Nanotechnology
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Indomethacin (IND) is an anti-inflammatory drug with poor solubility and short half-life.
- It causes gastrointestinal side effects and requires frequent dosing.
- Biopharmaceutical Classification System (BCS) class 2 drugs like IND present formulation challenges.
Purpose of the Study:
- To enhance indomethacin's therapeutic efficacy by developing novel nanoparticle formulations.
- To overcome challenges of low solubility, short half-life, and adverse effects of indomethacin.
- To create sustained-release formulations for improved patient compliance and reduced toxicity.
Main Methods:
- Polymeric Nanoparticles (PNPs) prepared via emulsification/solvent evaporation.
- Solid Lipid Nanoparticles (SLNs) prepared using hot homogenization.
- Characterization included particle size, PDI, zeta potential, encapsulation efficiency, and drug-excipient compatibility (DSC, FT-IR, 1H NMR).
- In vitro drug release and cytotoxicity (MTT assay) were evaluated.
Main Results:
- Both PNP and SLN formulations exhibited good stability, particle size, PDI, and zeta potential.
- High encapsulation efficiencies were achieved for both nanoparticle types.
- In vitro studies confirmed prolonged drug release from both formulations compared to pure indomethacin.
- PNP formulations showed significantly lower toxicity to normal cells.
Conclusions:
- Successfully developed indomethacin-loaded PNP and SLN formulations.
- These formulations facilitate intestinal drug release and extend release duration.
- PNP nanocarriers offer a safer alternative for indomethacin delivery due to reduced cytotoxicity.

