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<p>Rheumatoid arthritis (RA) is a chronic autoimmune disease that leads to generalised joint damage and, ultimately leads to disability. Although existing treatment options, such as nonsteroidal anti-inflammatory drugs (NSAIDs) and disease-modifying antirheumatic drugs (DMARDs), show some improvement, these are often accompanied by adverse effects and limited effectiveness. Tofacitinib, a Janus kinase (JAK) inhibitor, promises well in RA treatment. However, its low solubility has limited its therapeutic potential because of its poor bioavailability. This is a study aimed at optimising the liposomal formulation of tofacitinib to enhance its bioavailability and eliminate side effects associated with oral administration. The liposomal formulation was produced by thin-film hydration, in which phosphatidylcholine, cholesterol and PEGylated lipids were incorporated to provide maximum encapsulation and improved stability. In addition, an analytical procedure for quantification of tofacitinib using RP-HPLC was established and validated. The method showed extraordinary precision, accuracy and linearity, correlation coefficient (R²) of 0.999. The particles were characterised for particle size, zeta potential and entrapment efficiency (EE). The ideal composition displayed a particle size of 164 ± 28.06&#xa0;nm; a polydispersity index (PDI) of 0.16, and EE of 92%. In vitro release studies demonstrated a prolonged release profile for the drug, with 92.8% of the drug released at 24&#xa0;h. These data indicate that the liposomal formulation of tofacitinib can potentially increase its therapeutic effect significantly due to enhancement of bioavailability and diminishing systemic side-effects; thus, it would be a promising line for RA therapy development.</p>

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RP-HPLC Analytical Method Development for Estimation of Tofacitinib in Pure Form and Liposome Formulation

  • 期刊论文

  • 发表日期：

    2025年10月30日

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  • Shivani Pannu,
  • Inderjeet Verma

摘要

Rheumatoid arthritis (RA) is a chronic autoimmune disease that leads to generalised joint damage and, ultimately leads to disability. Although existing treatment options, such as nonsteroidal anti-inflammatory drugs (NSAIDs) and disease-modifying antirheumatic drugs (DMARDs), show some improvement, these are often accompanied by adverse effects and limited effectiveness. Tofacitinib, a Janus kinase (JAK) inhibitor, promises well in RA treatment. However, its low solubility has limited its therapeutic potential because of its poor bioavailability. This is a study aimed at optimising the liposomal formulation of tofacitinib to enhance its bioavailability and eliminate side effects associated with oral administration. The liposomal formulation was produced by thin-film hydration, in which phosphatidylcholine, cholesterol and PEGylated lipids were incorporated to provide maximum encapsulation and improved stability. In addition, an analytical procedure for quantification of tofacitinib using RP-HPLC was established and validated. The method showed extraordinary precision, accuracy and linearity, correlation coefficient (R²) of 0.999. The particles were characterised for particle size, zeta potential and entrapment efficiency (EE). The ideal composition displayed a particle size of 164 ± 28.06 nm; a polydispersity index (PDI) of 0.16, and EE of 92%. In vitro release studies demonstrated a prolonged release profile for the drug, with 92.8% of the drug released at 24 h. These data indicate that the liposomal formulation of tofacitinib can potentially increase its therapeutic effect significantly due to enhancement of bioavailability and diminishing systemic side-effects; thus, it would be a promising line for RA therapy development.