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<p>As the most frequent clinical problem, intervertebral disc degeneration (IVDD) and associated inflammatory pain are still a big challenge, thus there is a need for improved and more lasting therapeutic approaches. In this study, a lipidic prodrug of diclofenac, Diclofenac Lauryl Ester (L-DCF), was synthesized and formulated into nanoparticles (Nanofenac-L) using the ethanol injection method followed by microfluidization. The encapsulation efficiency of Nanofenac-L was &gt; 97% with sustained drug release, releasing around 65% of the diclofenac in 48&#xa0;h. The therapeutic potential of Nanofenac-L was evaluated in rat intervertebral disc-derived nucleus pulposus cells.&#xa0;Nanofenac-L was found to be more effective than free Diclofenac Sodium (DCF-Na) in terms of anti-inflammatory activity, which was confirmed with significant suppression of COX-2 and Substance P. Furthermore, Nanofenac-L increased the expression of antioxidant genes in cells, such as SOD1, GPX1 and PRDX1. Preventive treatment was found to have shown therapeutic value whereas the curative treatment yielded a significant therapeutic effect indicating the possibility of Nanofenac-L to alleviate inflammation as well as to slow down disease progression. Altogether, these results suggest that Nanofenac-L could represent a promising long-lasting anti-inflammatory, pain relieving and antioxidant nanotherapeutic. Comprehensive preclinical and clinical evaluation is essential to translate these findings into viable therapies.</p> Graphical Abstract <p></p>

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Scalable diclofenac lauryl ester prodrug nanoparticles: a promising strategy for reducing inflammation associated with intervertebral disc degeneration

  • 期刊论文

  • 发表日期：

    2026年6月18日

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  • Saadat Hussain,
  • Aqsa Arif,
  • Perveen Bano,
  • Rudaba Saleem,
  • Shafiqa Naeem Rajput,
  • Liangliang Zhang,
  • Irfan Khan,
  • Mujeeb-ur-Rehman

摘要

As the most frequent clinical problem, intervertebral disc degeneration (IVDD) and associated inflammatory pain are still a big challenge, thus there is a need for improved and more lasting therapeutic approaches. In this study, a lipidic prodrug of diclofenac, Diclofenac Lauryl Ester (L-DCF), was synthesized and formulated into nanoparticles (Nanofenac-L) using the ethanol injection method followed by microfluidization. The encapsulation efficiency of Nanofenac-L was > 97% with sustained drug release, releasing around 65% of the diclofenac in 48 h. The therapeutic potential of Nanofenac-L was evaluated in rat intervertebral disc-derived nucleus pulposus cells. Nanofenac-L was found to be more effective than free Diclofenac Sodium (DCF-Na) in terms of anti-inflammatory activity, which was confirmed with significant suppression of COX-2 and Substance P. Furthermore, Nanofenac-L increased the expression of antioxidant genes in cells, such as SOD1, GPX1 and PRDX1. Preventive treatment was found to have shown therapeutic value whereas the curative treatment yielded a significant therapeutic effect indicating the possibility of Nanofenac-L to alleviate inflammation as well as to slow down disease progression. Altogether, these results suggest that Nanofenac-L could represent a promising long-lasting anti-inflammatory, pain relieving and antioxidant nanotherapeutic. Comprehensive preclinical and clinical evaluation is essential to translate these findings into viable therapies.

Graphical Abstract