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Purpose <p>Osteoarthritis is a degenerative joint disease that causes painful inflammation with&#xa0;cartilaginous damage that highly impacts geriatric health, demanding advanced therapy with limited complications on treatment. Conventional therapies&#xa0;focused on associated pain only, thus failing to treat the root cause of inflammatory degenerative cartilaginous tissue of the joints. To overcome the related issues, a holistic approach is the combinatorial therapy of Oxaprozin (OXA) and Apricot kernel oil (AKO) which encompasses the excellent analgesic and&#xa0;restoration of lipid-balance activities.</p> Method <p>The scalable targeted transcutaneous delivery of OXA-loaded Apricot oil-based nanoemulgel (OXA-NEG)&#xa0;was&#xa0;optimized and evaluated. Further, preclinical studies aligned with better therapeutic outcomes.</p> Result <p>The GC–MS study of the AKO identified potential components, including vitamins, fatty acids, and antioxidants. The optimized nanoemulsion with an average globule size of 208.5 ± 5.97&#xa0;nm, PDI 0.2502 ± 0.045, and zeta potential of -16.33 ± 0.241&#xa0;mV, revealed promising&#xa0;delivery. The OXA-NEG&#xa0;exhibited good spreadability and extrudability in texture analysis. The <i>in-vitro</i> and <i>ex-vivo</i> studies demonstrated sustained release with high permeation flux&#xa0;compared to conventional gel. The&#xa0;therapeutic potential was assessed&#xa0;on an osteoarthritis-induced animal&#xa0;model, where radiographic examination revealed that the OXA-NEG&#xa0;group of rats showed prominent recovery of the swollen joint cartilage in contrast to the control group. The plasma TNF-α and IL-6 levels also showed substantial variation (<i>p</i> &lt; 0.001) compared to the control group.</p> Conclusion <p>It is concluded that the proposed&#xa0;formulation has promising dual therapeutic potential for transcutaneous delivery, meeting safety aspects and could be aligned with better clinical acceptance.</p> Graphical Abstract <p></p>

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Transcutaneous Delivery of Dual-Approach Oxaprozin and Apricot Kernel Oil Through a QbD Driven Nanoemulgel: Therapeutic Potential Against Osteoarthritis-Induced Animal Model

  • 期刊论文

  • 发表日期：

    2026年1月5日

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  • Ahsan Ali,
  • Uzma Farooq,
  • Ayesha Siddiqui,
  • Vijay Kumar,
  • Chaudhary Abdur Rahman Hamidullah,
  • Zeenat Iqbal,
  • Mohd Aamir Mirza

摘要

Purpose

Osteoarthritis is a degenerative joint disease that causes painful inflammation with cartilaginous damage that highly impacts geriatric health, demanding advanced therapy with limited complications on treatment. Conventional therapies focused on associated pain only, thus failing to treat the root cause of inflammatory degenerative cartilaginous tissue of the joints. To overcome the related issues, a holistic approach is the combinatorial therapy of Oxaprozin (OXA) and Apricot kernel oil (AKO) which encompasses the excellent analgesic and restoration of lipid-balance activities.

Method

The scalable targeted transcutaneous delivery of OXA-loaded Apricot oil-based nanoemulgel (OXA-NEG) was optimized and evaluated. Further, preclinical studies aligned with better therapeutic outcomes.

Result

The GC–MS study of the AKO identified potential components, including vitamins, fatty acids, and antioxidants. The optimized nanoemulsion with an average globule size of 208.5 ± 5.97 nm, PDI 0.2502 ± 0.045, and zeta potential of -16.33 ± 0.241 mV, revealed promising delivery. The OXA-NEG exhibited good spreadability and extrudability in texture analysis. The in-vitro and ex-vivo studies demonstrated sustained release with high permeation flux compared to conventional gel. The therapeutic potential was assessed on an osteoarthritis-induced animal model, where radiographic examination revealed that the OXA-NEG group of rats showed prominent recovery of the swollen joint cartilage in contrast to the control group. The plasma TNF-α and IL-6 levels also showed substantial variation (p < 0.001) compared to the control group.

Conclusion

It is concluded that the proposed formulation has promising dual therapeutic potential for transcutaneous delivery, meeting safety aspects and could be aligned with better clinical acceptance.

Graphical Abstract