Purpose:
The work was performed to investigate the feasibility of preparing ocular inserts
loaded with Poly-ε-Caprolactone (PCL) nanoparticles as a sustained ocular delivery system.
Methods:
First, Atorvastatin Calcium-Poly-ε-Caprolactone (ATC-PCL) nanoparticles were prepared
and characterized. Then, the optimized nanoparticles were loaded within inserts formulated with
Methylcellulose (MC) and Polyvinyl Alcohol (PVA) by a solvent casting technique and evaluated
physically, for in-vitro drug release profile. Finally, an in-vivo study was performed on the selected
formulation to prove non-irritability and sustained ocular anti-inflammatory efficacy compared with
free drug-loaded ocuserts.
Results:
The results revealed (ATC-PCL) nanoparticles prepared with 0.5% pluronic F127 were optimized
with 181.72±3.6 nm particle size, 0.12±0.02 (PDI) analysis, -27.4± 0.69 mV zeta potential and
62.41%±4.7% entrapment efficiency. Nanoparticles loaded ocuserts manifested compatibility between
drug and formulation polymers. Moreover, formulations complied with average weight 0.055±0.002 to
0.143±0.023 mg, and accepted pH. ATC-PCL nanoparticles loaded inserts prepared by 5% MC
showed more sustained, prolonged in-vitro release over 24h. In-vivo study emphasized non-irritability,
ocular anti-inflammatory effectiveness represented by smaller lid closure scores, and statistically significant
lowering in PMN count after 3h.
Conclusion:
These findings proposed a possibly simple, new and affordable price technique to prepare
promising (ATC-PCL) nanoparticles loaded inserts to achieve sustained release with prolonged antiinflammatory
efficacy.
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