Piroxicam (PX), a main member of non-steroidal anti-inflammatory drugs (NSAIDs), is mainly used orally, which causes side effects of the gastrointestinal tract. It also has systemic effects when administered intramuscularly. Intra-articular (IA) delivery and encapsulation of PX in biodegradable poly-ε-caprolactone (PCL) nanoparticles (NPs) offer potential advantages over conventional oral delivery. The purpose of this study is the development of a new type of anti-inflammatory bio-agents containing collagen and PX-loaded NPs, as an example for an oral formulation replacement, for the prolonged release of PX. In this study, the PX was encapsulated in PCL NPs (size 102.7 ± 19.37 nm, encapsulation efficiency 92.83 ± 0.4410) by oil-in-water (o/w) emulsion solvent evaporation method. Nanoparticles were then characterized for entrapment efficiency, percent yield, particle size analysis, morphological characteristics, and in vitro drug release profiles. Eventually, the NPs synthesized with collagen were conjugated so that the NPs were trapped in the collagen sponges using a cross-linker. Finally, biocompatibility tests showed that the anti-inflammatory agents made in this study had no toxic effect on the cells. Based on the results, it appears that PX-loaded PCL NPs along with collagen (PPCLnp-Coll) can be promising for IA administration based on particulate drug delivery for the treatment of arthritis.

中文翻译：

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基于负载吡罗昔康的聚-ε-己内酯纳米颗粒的新型抗炎生物制剂的制备和表征，用于持续 NSAID 递送。


吡罗昔康（PX）是非甾体抗炎药（NSAIDs）的主要成员，主要口服使用，会引起胃肠道副作用。肌肉注射时，它还具有全身作用。关节内（IA）递送和将 PX 封装在可生物降解的聚ε-己内酯（PCL）纳米颗粒（NP）中比传统的口服递送具有潜在优势。本研究的目的是开发一种含有胶原蛋白和负载 PX 的纳米粒子的新型抗炎生物制剂，作为口服制剂替代品的一个例子，用于延长 PX 的释放。在本研究中，通过水包油（o/w）乳液溶剂蒸发方法将PX封装在PCL纳米粒子（尺寸102.7±19.37 nm，封装效率92.83±0.4410）中。然后对纳米颗粒的包封效率、产率百分比、粒度分析、形态特征和体外药物释放曲线进行表征。最终，用胶原合成的纳米粒子被缀合，从而使用交联剂将纳米粒子捕获在胶原海绵中。最后，生物相容性测试表明，本研究制作的抗炎剂对细胞没有毒性作用。根据这些结果，负载 PX 的 PCL 纳米颗粒与胶原蛋白 (PPCLnp-Coll) 似乎有望用于基于颗粒药物递送的 IA 给药，以治疗关节炎。