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Purpose <p>Apigenin (API), a bioactive plant-derived flavonoid, is a potent antiarthritic and anti-inflammatory agent. However, its translational potential is hindered by its extremely low aqueous solubility and poor bioavailability. This study aimed to prepare apigenin-β-cyclodextrin (API-βCD)-loaded liposomes (API-βCD-L) coated with hyaluronic acid (HA) for improved therapeutic activity.</p> Methods <p>The thin-film hydration method was used to prepare API-βCD-L. The formulation was statistically optimized using the Design-Expert Box–Behnken design and subsequently coated with HA. Dynamic light scattering, powder X-ray diffraction, and transmission electron microscopy were used for physicochemical characterization, followed by release behavior and pharmacokinetic (PK) evaluation. Complete Freund’s adjuvant (CFA)-induced arthritis model was used to investigate the antiarthritic efficacy.</p> Results <p>The optimized API-βCD-L demonstrated a mean particle size (PS) of 198.3 ± 1.83 nm, zeta potential of 29.26 ± 2.5 mV, and %EE of 95.39% ± 0.61%. Successful surface modification with HA was evident from the surface reversal (−8.68±0.51 mV) and increase in PS to 242.2 ± 8.4 nm. Both API-βCD-L and HA-API-βCD-L improved and sustained API release compared to the suspension; however, HA-API-βCD-L demonstrated prolonged release. Significant enhancement in systemic exposure was revealed by PK analysis, including 35.9-, 10.4-, 9.6-, and 5.9 -fold increases in AUC, T<sub>1/2,</sub> C<sub>max,</sub> and mean residence time, respectively. Marked reductions in paw edema, inflammatory cytokines, and joint destruction, supported by radiological and histopathological findings, were evident from in vivo evaluation in the CFA-induced arthritis model.</p> Conclusion <p>The sustained release, enhanced bioavailability, and superior antiarthritic efficacy of HA-API-βCD-L highlight its potential as a promising nanotherapeutic agent for managing rheumatoid arthritis.</p>

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Hyaluronic acid-functionalized liposomes as a nanoplatform for enhanced pharmacokinetics and therapeutic efficacy in arthritis

  • 期刊论文

  • 发表日期：

    2026年5月8日

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  • Zakir Ali,
  • Muhammad Junaid,
  • Sibgha Batool,
  • Sidra Aslam,
  • Tofeeq ur Rehman,
  • Ali H. Alamri,
  • Adel Al Fatease,
  • Nabil K. Alruwaili,
  • Majed A Alghamdi,
  • Han-Gon Choi,
  • Fakhar ud Din

摘要

Purpose

Apigenin (API), a bioactive plant-derived flavonoid, is a potent antiarthritic and anti-inflammatory agent. However, its translational potential is hindered by its extremely low aqueous solubility and poor bioavailability. This study aimed to prepare apigenin-β-cyclodextrin (API-βCD)-loaded liposomes (API-βCD-L) coated with hyaluronic acid (HA) for improved therapeutic activity.

Methods

The thin-film hydration method was used to prepare API-βCD-L. The formulation was statistically optimized using the Design-Expert Box–Behnken design and subsequently coated with HA. Dynamic light scattering, powder X-ray diffraction, and transmission electron microscopy were used for physicochemical characterization, followed by release behavior and pharmacokinetic (PK) evaluation. Complete Freund’s adjuvant (CFA)-induced arthritis model was used to investigate the antiarthritic efficacy.

Results

The optimized API-βCD-L demonstrated a mean particle size (PS) of 198.3 ± 1.83 nm, zeta potential of 29.26 ± 2.5 mV, and %EE of 95.39% ± 0.61%. Successful surface modification with HA was evident from the surface reversal (−8.68±0.51 mV) and increase in PS to 242.2 ± 8.4 nm. Both API-βCD-L and HA-API-βCD-L improved and sustained API release compared to the suspension; however, HA-API-βCD-L demonstrated prolonged release. Significant enhancement in systemic exposure was revealed by PK analysis, including 35.9-, 10.4-, 9.6-, and 5.9 -fold increases in AUC, T1/2, Cmax, and mean residence time, respectively. Marked reductions in paw edema, inflammatory cytokines, and joint destruction, supported by radiological and histopathological findings, were evident from in vivo evaluation in the CFA-induced arthritis model.

Conclusion

The sustained release, enhanced bioavailability, and superior antiarthritic efficacy of HA-API-βCD-L highlight its potential as a promising nanotherapeutic agent for managing rheumatoid arthritis.