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<p>Gallic acid (GA), a polyphenol, shows promise in treating chronic myeloid leukemia (CML), a severe condition affecting all ages. While tyrosine kinase inhibitors (TKIs) have improved CML management, resistance necessitates alternative therapies. GA nanosponges (GA-NS) were developed using emulsion solvent diffusion&#xa0;method and optimized through a Box-Behnken design with 15 experimental runs. Independent variables included ethylated cellulose (X1), polyviol (X2), and dimethyl carbonate (X3), while dependent variables were particle size (PS) (Y1), entrapment efficiency (%EE) (Y2), and zeta potential (ZP) (Y3). A validated RP-HPLC method with a mobile phase of water (0.1% formic acid) and methanol (80:20 v/v), a 1&#xa0;mL/min flow rate, and a column temperature of 30&#xa0;°C ensured precise GA quantification. Surface morphology was assessed via TEM, and <i>in-vitro</i> cytotoxicity using the K-562 leukemia cell line. Optimized GA-NS exhibited a PS of 318.9&#xa0;nm, 88.74% EE, and ZP of -23.94&#xa0;mV. Drug content was 86.3%, with release kinetics aligning with a korsmeyer-peppas model (R<sup>2</sup> = 0.9591). GA analysis showed a retention time of 4.834&#xa0;min, a tailing factor of 1.75, and 3935.25 theoretical plates. Validation displayed linearity (R<sup>2</sup> = 0.9997) over 2–12&#xa0;µg/mL, with LOD and LOQ of 0.257&#xa0;µg/mL and 0.781&#xa0;µg/mL. TEM confirmed spherical nanosponges, and cytotoxicity testing demonstrated an IC50 of 358.13&#xa0;µg/mL against imatinib. GA-NS, optimized via a QbD approach, and the validated HPLC method support GA’s application as a stable, effective CML therapy.</p> Graphical Abstract <p></p>

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Quality-by-Design Optimization of Gallic Acid Loaded Nanosponges for Enhancing its Drug Delivery: RP-HPLC Quantification and In-vitro Anti-leukemic Activity

  • 期刊论文

  • 发表日期：

    2025年6月23日

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  • Vineeth Bharadwaj. P,
  • Vinayak Mastiholimath,
  • Atith Muppayyanamath,
  • Rahul Koli

摘要

Gallic acid (GA), a polyphenol, shows promise in treating chronic myeloid leukemia (CML), a severe condition affecting all ages. While tyrosine kinase inhibitors (TKIs) have improved CML management, resistance necessitates alternative therapies. GA nanosponges (GA-NS) were developed using emulsion solvent diffusion method and optimized through a Box-Behnken design with 15 experimental runs. Independent variables included ethylated cellulose (X1), polyviol (X2), and dimethyl carbonate (X3), while dependent variables were particle size (PS) (Y1), entrapment efficiency (%EE) (Y2), and zeta potential (ZP) (Y3). A validated RP-HPLC method with a mobile phase of water (0.1% formic acid) and methanol (80:20 v/v), a 1 mL/min flow rate, and a column temperature of 30 °C ensured precise GA quantification. Surface morphology was assessed via TEM, and in-vitro cytotoxicity using the K-562 leukemia cell line. Optimized GA-NS exhibited a PS of 318.9 nm, 88.74% EE, and ZP of -23.94 mV. Drug content was 86.3%, with release kinetics aligning with a korsmeyer-peppas model (R2 = 0.9591). GA analysis showed a retention time of 4.834 min, a tailing factor of 1.75, and 3935.25 theoretical plates. Validation displayed linearity (R2 = 0.9997) over 2–12 µg/mL, with LOD and LOQ of 0.257 µg/mL and 0.781 µg/mL. TEM confirmed spherical nanosponges, and cytotoxicity testing demonstrated an IC50 of 358.13 µg/mL against imatinib. GA-NS, optimized via a QbD approach, and the validated HPLC method support GA’s application as a stable, effective CML therapy.

Graphical Abstract