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Purpose <p>Apigenin (APG) offers promising therapeutic benefits for osteoarthritis, but its clinical use is limited due to its poor water solubility, rapid metabolism, and low oral bioavailability, which prevent adequate drug levels from reaching the affected joints. In addition, APG does not easily pass through the skin, making conventional transdermal delivery approaches ineffective. These drawbacks highlight the necessity for an improved delivery strategy that can enhance skin penetration and provide sustained drug availability at the target site. To address this challenge, the present study developed and optimized APG-loaded transniosomes using a Box–Behnken design and incorporated the optimized formulation into a dissolving microneedle (MN) patch to enhance transdermal delivery.</p> Methods <p>Transniosomes (TNs) were prepared using the thin-film hydration method. Pre-clinical evaluation was carried out through in vitro drug release, ex vivo rat skin permeation, and in vivo pharmacodynamic studies using a Wistar albino rat osteoarthritis model.</p> Results <p>Opt-APG TNs shows vesicles size 177.1 ± 1.81 nm, PDI 0.27 ± 0.001, zeta potential − 33.49 mV and EE 91.0 ± 0.97%. TEM image of Opt-APG TNs revealed that the prepared vesicles exhibited a well-defined, sealed structure and were spherical in shape. Opt-APG TNs exhibited better drug released 75.60 ± 0.07% than control formulation. The CLSM image shows that the Rhodamine B-loaded Opt-APG TNs penetrated the skin much deeper than the normal Rhodamine B solution. Over 24 h, the percentage of cumulative APG release from the Opt-APG TNs loaded patch was 87.83 ± 3.28% with a flux value 5.49 μg/cm<sup>2</sup>/h. Pre-clinical pharmacodynamic results demonstrated that the Opt-APG TNs-loaded MN group was most effective in reducing knee joint inflammation.</p> Conclusion <p>APG TNs were successfully prepared and optimized by Box Behnken design. MN-loaded APG transniosomal system developed holds significant potential for osteoarthritis management.</p>

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Microneedle Mediated Transdermal Delivery of Apigenin-Loaded Transniosomes for Osteoarthritis Therapy

  • 期刊论文

  • 发表日期：

    2026年4月7日

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  • Farzat Farha,
  • Niha Sultana,
  • Asad Ali,
  • Nasr A Emad,
  • Nazreen Tabassum,
  • Bushra Jabi,
  • Abdul Ahad,
  • Yasmin Sultana,
  • Mohd. Aqil

摘要

Purpose

Apigenin (APG) offers promising therapeutic benefits for osteoarthritis, but its clinical use is limited due to its poor water solubility, rapid metabolism, and low oral bioavailability, which prevent adequate drug levels from reaching the affected joints. In addition, APG does not easily pass through the skin, making conventional transdermal delivery approaches ineffective. These drawbacks highlight the necessity for an improved delivery strategy that can enhance skin penetration and provide sustained drug availability at the target site. To address this challenge, the present study developed and optimized APG-loaded transniosomes using a Box–Behnken design and incorporated the optimized formulation into a dissolving microneedle (MN) patch to enhance transdermal delivery.

Methods

Transniosomes (TNs) were prepared using the thin-film hydration method. Pre-clinical evaluation was carried out through in vitro drug release, ex vivo rat skin permeation, and in vivo pharmacodynamic studies using a Wistar albino rat osteoarthritis model.

Results

Opt-APG TNs shows vesicles size 177.1 ± 1.81 nm, PDI 0.27 ± 0.001, zeta potential − 33.49 mV and EE 91.0 ± 0.97%. TEM image of Opt-APG TNs revealed that the prepared vesicles exhibited a well-defined, sealed structure and were spherical in shape. Opt-APG TNs exhibited better drug released 75.60 ± 0.07% than control formulation. The CLSM image shows that the Rhodamine B-loaded Opt-APG TNs penetrated the skin much deeper than the normal Rhodamine B solution. Over 24 h, the percentage of cumulative APG release from the Opt-APG TNs loaded patch was 87.83 ± 3.28% with a flux value 5.49 μg/cm2/h. Pre-clinical pharmacodynamic results demonstrated that the Opt-APG TNs-loaded MN group was most effective in reducing knee joint inflammation.

Conclusion

APG TNs were successfully prepared and optimized by Box Behnken design. MN-loaded APG transniosomal system developed holds significant potential for osteoarthritis management.