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<p>In this research, hyaluronic acid (HA) was selected as a targeting agent for targeting overexpressed CD44 receptors in the leukemia. Ibrutinib (IBR) loaded liposomes (IBR-LPs) were fabricated by thin film hydration method, and HA was conjugated to IBR-LPs (HA-IBR-LPs) using carbodiimide chemistry. The IBR-LPs and HA-IBR-LPs showed particle size 88.34 ± 4.08&#xa0;nm and 113.3 ± 3.7&#xa0;nm, respectively. The zeta potential of HA-IBR-LPs was − 16.5 ± 3.50&#xa0;mV, and IBR-LPs was − 7.68 ± 2.24&#xa0;mV. The entrapment efficiency of IBR-LPs and HA-IBR-LPs was found to be 75.58 ± 2.38% and 72.05 ± 3.50%, respectively. The IBR was converted in the amorphous form after encapsulation into LPs. The IBR-LPs and HA-IBR-LPs exhibited spherical shape and were hemocompatible. The release of IBR-LPs and HA-IBR-LPs was 95.39 ± 1.50% in 28&#xa0;h and 93.89 ± 2.81% in 34&#xa0;h, respectively. The HA-IBR-LPs (IC50 0.3&#xa0;μM) were more cytotoxic as compared to IBR-LPs (IC50 0.7&#xa0;μM) and free IBR (IC50 1&#xa0;μM) across HL-60 cell line. The high internalization of fluorescein isothiocyanate loaded HA liposomes was observed across HL-60 cells. The HA-IBR-LPs increased blood circulation time as that of free IBR in rats. Hence, it can be said that HA-IBR-LPs could be a propitious nanocarrier for targeted delivery for CD44 receptors in leukemia.</p> Graphical Abstract <p></p>

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Hyaluronic Acid Conjugated Liposomes for Targeted Delivery of Ibrutinib: In Vitro, Cell Line, and In Vivo Assessment

  • 期刊论文

  • 发表日期：

    2025年2月18日

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  • Mitali Patel,
  • Puja Patel,
  • Bhavin Vyas

摘要

In this research, hyaluronic acid (HA) was selected as a targeting agent for targeting overexpressed CD44 receptors in the leukemia. Ibrutinib (IBR) loaded liposomes (IBR-LPs) were fabricated by thin film hydration method, and HA was conjugated to IBR-LPs (HA-IBR-LPs) using carbodiimide chemistry. The IBR-LPs and HA-IBR-LPs showed particle size 88.34 ± 4.08 nm and 113.3 ± 3.7 nm, respectively. The zeta potential of HA-IBR-LPs was − 16.5 ± 3.50 mV, and IBR-LPs was − 7.68 ± 2.24 mV. The entrapment efficiency of IBR-LPs and HA-IBR-LPs was found to be 75.58 ± 2.38% and 72.05 ± 3.50%, respectively. The IBR was converted in the amorphous form after encapsulation into LPs. The IBR-LPs and HA-IBR-LPs exhibited spherical shape and were hemocompatible. The release of IBR-LPs and HA-IBR-LPs was 95.39 ± 1.50% in 28 h and 93.89 ± 2.81% in 34 h, respectively. The HA-IBR-LPs (IC50 0.3 μM) were more cytotoxic as compared to IBR-LPs (IC50 0.7 μM) and free IBR (IC50 1 μM) across HL-60 cell line. The high internalization of fluorescein isothiocyanate loaded HA liposomes was observed across HL-60 cells. The HA-IBR-LPs increased blood circulation time as that of free IBR in rats. Hence, it can be said that HA-IBR-LPs could be a propitious nanocarrier for targeted delivery for CD44 receptors in leukemia.

Graphical Abstract