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<p>The aim of the study is to develop and optimize lifitegrast-loaded oleogels for enhanced ocular delivery with improved residence time and bioavailability for dry eye disease management. Oleogels containing lifitegrast were developed using both apricot kernel oil and Phospholipon 90G. Formulations were optimized using a 3<sup>2</sup> factorial design with Phospholipon 90G concentration (5–15%) and processing temperature (60–80&#xa0;°C) as independent variables. The new formula was carefully tested for physicochemical properties, ex vivo corneal penetration, stability and irritation when used in the eye in animal experiments. The quadratic model effectively described variable-response relationships (<i>R</i><sup>2</sup> &gt; 0.98). Phospholipon 90G concentration exhibited dominant influence on both responses (<i>F</i>-values 1971.20 and 4216.35). The optimized formulation (F6: 15% Phospholipon, 70&#xa0;°C) demonstrated superior oil binding capacity (96.91 ± 1.24%), appropriate viscosity (297.00 ± 7.82&#xa0;mPa·s), and physiological pH (7.2 ± 0.13). Ex vivo studies revealed significant corneal permeation (64.91 ± 3.67&#xa0;mg/cm<sup>2</sup> at 5&#xa0;h), representing a 13-fold improvement over conventional formulations. Accelerated stability testing confirmed robust integrity over 6&#xa0;months with minimal parameter changes. In vivo studies showed no ocular irritation, confirming excellent biocompatibility. Oleogels have promising effects on improving ocular drug delivery, as it ensures more stable retention and constant release of the drug to the eye. Preliminary results suggest potential for reduced dosing frequency and improved patient compliance, pending clinical validation. Further in vivo pharmacokinetic and clinical studies are warranted to establish translational potential.</p>

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Development and fabrication of apricot kernel oil-based oleogels for enhanced ocular delivery of lifitegrast in dry eye management

  • 期刊论文

  • 发表日期：

    2026年2月23日

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  • Someshwar Mankar,
  • Saurabh Argade,
  • Suhas Siddheshwar,
  • Shubham Mhaske,
  • Achal Andhale

摘要

The aim of the study is to develop and optimize lifitegrast-loaded oleogels for enhanced ocular delivery with improved residence time and bioavailability for dry eye disease management. Oleogels containing lifitegrast were developed using both apricot kernel oil and Phospholipon 90G. Formulations were optimized using a 32 factorial design with Phospholipon 90G concentration (5–15%) and processing temperature (60–80 °C) as independent variables. The new formula was carefully tested for physicochemical properties, ex vivo corneal penetration, stability and irritation when used in the eye in animal experiments. The quadratic model effectively described variable-response relationships (R2 > 0.98). Phospholipon 90G concentration exhibited dominant influence on both responses (F-values 1971.20 and 4216.35). The optimized formulation (F6: 15% Phospholipon, 70 °C) demonstrated superior oil binding capacity (96.91 ± 1.24%), appropriate viscosity (297.00 ± 7.82 mPa·s), and physiological pH (7.2 ± 0.13). Ex vivo studies revealed significant corneal permeation (64.91 ± 3.67 mg/cm2 at 5 h), representing a 13-fold improvement over conventional formulations. Accelerated stability testing confirmed robust integrity over 6 months with minimal parameter changes. In vivo studies showed no ocular irritation, confirming excellent biocompatibility. Oleogels have promising effects on improving ocular drug delivery, as it ensures more stable retention and constant release of the drug to the eye. Preliminary results suggest potential for reduced dosing frequency and improved patient compliance, pending clinical validation. Further in vivo pharmacokinetic and clinical studies are warranted to establish translational potential.