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<p>Chronic lymphocytic leukemia is a malignancy of B-cells. Ibrutinib (IBR) forms the enzymatic activity of Bruton tyrosine kinase (BTK) by creating a covalent connection with the cysteine residue in the enzyme’s active region. In this study, we wanted to create a unique formulation of IBR-loaded chitosan-coated liposomes, or IBR chitosomes. Low-molecular weight chitosan was placed on top of IBR liposomes that had been made utilizing the thin film technique. After optimizing IBR chitosomes with a Box-Behnken design, the mean particle size was measured at 314.2 ± 4.35&#xa0;nm, the polydispersity index was found to be 0.246 ± 0.18, and the zeta potential was found to be + 32.1 ± 0.22&#xa0;mV. IBR chitosomes were shown to have a drug encapsulation efficiency of 70.90 ± 2.21. Ibrutinib release from liposomes at pH 1.2 was shown to be reduced by chitosan coating, according to in vitro release tests The chitosan coating improves oral bioavailability by mucoadhesion,&#xa0;extended&#xa0;gastrointestinal residence time, and absorption enhancing effects. It&#xa0;also&#xa0;provides&#xa0;protection against gastric degradation,&#xa0;with&#xa0;more intact drug&#xa0;arriving&#xa0;at&#xa0;the absorption site. IBR chitosomes exhibited a 3.472-fold and 2.07-fold increase in AUC(0-t) and Cmax, respectively, in the in-vivo pharmacokinetic evaluation compared to free IBR suspension. Furthermore, IBR chitosomes have a 3.47-fold better oral bioavailability than IBR solution alone, according to in vivo pharmacokinetic investigations. As such, the synthesized IBR chitosomes serve as an advantageous drug delivery mechanism, augmenting IBR’s solubility and oral bioavailability.</p> Graphical Abstract <p></p>

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Development, Optimization, and Characterization of Ibrutinib-Loaded Chitosomes Using Box-Behnken Design: In Vitro Evaluation and In Vivo Pharmacokinetic Studies

  • 期刊论文

  • 发表日期：

    2025年5月30日

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  • Pragathi Devanand Bangera,
  • Kiran Noel Lobo,
  • Mahesha Keerikkadu,
  • Divya Dhatri Kara,
  • Vamshi Krishna Tippavajhala,
  • Mahalaxmi Rathnanand

摘要

Chronic lymphocytic leukemia is a malignancy of B-cells. Ibrutinib (IBR) forms the enzymatic activity of Bruton tyrosine kinase (BTK) by creating a covalent connection with the cysteine residue in the enzyme’s active region. In this study, we wanted to create a unique formulation of IBR-loaded chitosan-coated liposomes, or IBR chitosomes. Low-molecular weight chitosan was placed on top of IBR liposomes that had been made utilizing the thin film technique. After optimizing IBR chitosomes with a Box-Behnken design, the mean particle size was measured at 314.2 ± 4.35 nm, the polydispersity index was found to be 0.246 ± 0.18, and the zeta potential was found to be + 32.1 ± 0.22 mV. IBR chitosomes were shown to have a drug encapsulation efficiency of 70.90 ± 2.21. Ibrutinib release from liposomes at pH 1.2 was shown to be reduced by chitosan coating, according to in vitro release tests The chitosan coating improves oral bioavailability by mucoadhesion, extended gastrointestinal residence time, and absorption enhancing effects. It also provides protection against gastric degradation, with more intact drug arriving at the absorption site. IBR chitosomes exhibited a 3.472-fold and 2.07-fold increase in AUC(0-t) and Cmax, respectively, in the in-vivo pharmacokinetic evaluation compared to free IBR suspension. Furthermore, IBR chitosomes have a 3.47-fold better oral bioavailability than IBR solution alone, according to in vivo pharmacokinetic investigations. As such, the synthesized IBR chitosomes serve as an advantageous drug delivery mechanism, augmenting IBR’s solubility and oral bioavailability.

Graphical Abstract