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<p>Nilotinib, is used to treat chronic myeloid leukemia (CML) a second-generation tyrosine kinase inhibitor, has poor solubility and low oral bioavailability, limiting its therapeutic potential. This study aimed to develop and optimize a solid lipid nanosuspension (SLN) of nilotinib to enhance its solubility, dissolution rate, and intestinal permeability.&#xa0;A Nilotinib–soya lecithin–PVP K30 complex was formulated into a nanosuspension using the solvent–antisolvent precipitation method with Polysorbate 80 as the stabilizer. A central composite design evaluated the effect of surfactant concentration and homogenization speed on critical quality attributes such as drug release, particle size, and permeability.&#xa0;The optimized SLN exhibited nanosized, spherical particles with enhanced solubility, dissolution, and permeability compared to pure drug and conventional nanosuspension. Thermal and X-ray analyses confirmed partial amorphization, contributing to improved solubility and dissolution. In vitro dissolution studies demonstrated &gt; 90% drug release from SLN versus &lt; 50% from API. Ex vivo studies using goat intestine showed a 1.9-fold increase in permeability with SLN. The saturation solubility has increased by nearly 7-fold in SLN compared to the API.&#xa0;This study showed an effective lipid-based nanosuspensions that overcome the biopharmaceutical limitations of BCS Class IV drugs. The developed SLN system offers a promising oral delivery strategy for nilotinib, and further in vivo pharmacokinetic investigations.</p>

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Design and Optimization of a Lecithin-Loaded Solid Lipid Nanosuspension for Enhancing Permeability and Oral Bioavailability of Nilotinib

  • 期刊论文

  • 发表日期：

    2026年1月16日

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  • Komal Parmar,
  • Mehul Patel,
  • Tejal Soni

摘要

Nilotinib, is used to treat chronic myeloid leukemia (CML) a second-generation tyrosine kinase inhibitor, has poor solubility and low oral bioavailability, limiting its therapeutic potential. This study aimed to develop and optimize a solid lipid nanosuspension (SLN) of nilotinib to enhance its solubility, dissolution rate, and intestinal permeability. A Nilotinib–soya lecithin–PVP K30 complex was formulated into a nanosuspension using the solvent–antisolvent precipitation method with Polysorbate 80 as the stabilizer. A central composite design evaluated the effect of surfactant concentration and homogenization speed on critical quality attributes such as drug release, particle size, and permeability. The optimized SLN exhibited nanosized, spherical particles with enhanced solubility, dissolution, and permeability compared to pure drug and conventional nanosuspension. Thermal and X-ray analyses confirmed partial amorphization, contributing to improved solubility and dissolution. In vitro dissolution studies demonstrated > 90% drug release from SLN versus < 50% from API. Ex vivo studies using goat intestine showed a 1.9-fold increase in permeability with SLN. The saturation solubility has increased by nearly 7-fold in SLN compared to the API. This study showed an effective lipid-based nanosuspensions that overcome the biopharmaceutical limitations of BCS Class IV drugs. The developed SLN system offers a promising oral delivery strategy for nilotinib, and further in vivo pharmacokinetic investigations.