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.

目的：进行这项工作以研究制备载有聚-ε-己内酯（PCL）纳米颗粒作为持续眼部递送系统的眼插入物的可行性。

方法：首先，制备和表征阿托伐他汀钙-聚-ε-己内酯钙（ATC-PCL）纳米颗粒。然后，通过溶剂浇铸技术将优化的纳米颗粒加载到由甲基纤维素（MC）和聚乙烯醇（PVA）配制的插入物中，并进行物理评估，以进行体外药物释放。最后，对选定的制剂进行了一项体内研究，以证明与自由药物负载的使用者相比，该药物具有非刺激性和持续的眼部抗炎功效。

结果：结果显示，以0.5.7％的Puronic F127制备的（ATC-PCL）纳米粒子具有181.72±3.6 nm的粒径，0.12±0.02（PDI）分析，-27.4±0.69 mV的ζ电势和62.41％±4.7％的包封效率进行了优化。载有纳米颗粒的使用者表现出药物和制剂聚合物之间的相容性。此外，该制剂符合平均重量0.055±0.002至0.143±0.023mg，并具有可接受的pH。由5％MC制备的装有ATC-PCL纳米颗粒的插入物在24小时内显示出更持续，更长的体外释放。体内研究强调了不易怒，以较小的眼睑闭合分数表示的眼部抗炎效果，以及3h后PMN计数有统计学意义的降低。

结论：这些发现提出了一种可能简单，新颖且价格合理的价格技术，以制备有前途的（ATC-PCL）纳米颗粒负载插入物，以实现持续释放和延长的抗炎功效。