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<p>Nintedanib (NIN) is a US FDA-approved tyrosine kinase inhibitor for effectively treating idiopathic pulmonary fibrosis (IPF). This work aims to develop long-circulating polymeric micelles of nintedanib to treat immobile patients with IPF. Nintedanib polymeric micelles were prepared using the polymer Pluronic F127 <i>via</i> the thin film hydration method. Further, Pluronic F127 was surface modified by thiolation with thioglycolic acid (-SH group) and thiolated nintedanib micelles (NIN-TA-micelles) were prepared with modified Pluronic F127. ATR-FTIR, <sup>1</sup>H NMR, and <sup>13</sup>C NMR confirmed structural characteristics of thiolated Pluronic F127. The thiolated micelles showed a vesicle size of 350 ± 15&#xa0;nm, PDI of 0.499 ± 0.07 and zeta potential of -32.9 ± 0.64 mV. The micelles were spherical when observed under a transmission electron microscope. NIN-TA-micelles showed an extended drug release profile of 83.65 ± 2.1% in 120&#xa0;h in a 6.8 pH buffer compared to 92.8 ± 8.4% of NIN-micelles within 48&#xa0;h. The MTT assay of NIN-micelles and NIN-TA-micelles on A549 cells showed the IC50 value of 138.81&#xa0;µg/mL and 82.61&#xa0;µg/mL, respectively. Intracellular hydroxyproline test showed that NIN-TA-micelles are approximately 1.51 times more effective than NIN-micelles at 40&#xa0;µg and approximately 1.36 times more effective at 80&#xa0;µg. The sustained-release properties and enhanced therapeutic efficacy of NIN-TA-micelles suggest their potential to prolong patient survival in patients with IPF.</p> Graphical abstract <p></p>

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Long-circulating thiolated Pluronic-based micelles of nintedanib for lung fibrosis: development, in vitro characterization and cell line studies for antifibrotic effect

  • 期刊论文

  • 发表日期：

    2026年6月19日

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  • Dhruti Thakkar,
  • Kunal Gokhale,
  • Sarika Wairkar

摘要

Nintedanib (NIN) is a US FDA-approved tyrosine kinase inhibitor for effectively treating idiopathic pulmonary fibrosis (IPF). This work aims to develop long-circulating polymeric micelles of nintedanib to treat immobile patients with IPF. Nintedanib polymeric micelles were prepared using the polymer Pluronic F127 via the thin film hydration method. Further, Pluronic F127 was surface modified by thiolation with thioglycolic acid (-SH group) and thiolated nintedanib micelles (NIN-TA-micelles) were prepared with modified Pluronic F127. ATR-FTIR, 1H NMR, and 13C NMR confirmed structural characteristics of thiolated Pluronic F127. The thiolated micelles showed a vesicle size of 350 ± 15 nm, PDI of 0.499 ± 0.07 and zeta potential of -32.9 ± 0.64 mV. The micelles were spherical when observed under a transmission electron microscope. NIN-TA-micelles showed an extended drug release profile of 83.65 ± 2.1% in 120 h in a 6.8 pH buffer compared to 92.8 ± 8.4% of NIN-micelles within 48 h. The MTT assay of NIN-micelles and NIN-TA-micelles on A549 cells showed the IC50 value of 138.81 µg/mL and 82.61 µg/mL, respectively. Intracellular hydroxyproline test showed that NIN-TA-micelles are approximately 1.51 times more effective than NIN-micelles at 40 µg and approximately 1.36 times more effective at 80 µg. The sustained-release properties and enhanced therapeutic efficacy of NIN-TA-micelles suggest their potential to prolong patient survival in patients with IPF.

Graphical abstract