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<p>Glaucoma, a leading cause of blindness, is caused by elevated intraocular pressure (IOP) that damages retinal ganglion cells. Current treatments, such as bimatoprost (BIM) eye drops, are limited by poor ocular bioavailability and rapid precorneal clearance. This study proposes a novel approach using BIM-loaded surfactant-based bilosomes (SBB) and lipid-based bilosomes (LBB) incorporated into an in situ gel (ISG) to enhance ocular drug delivery and therapeutic efficacy. Optimized formulations were obtained utilizing a 3<sup>3</sup>-Box Behnken Design (BBD). SBB showed a particle size of 165.3 ± 5.32&#xa0;nm, a zeta potential of -23.8 ± 5.32 mV, and an encapsulation efficiency of 83.92 ± 2.76%, while LBB exhibited a particle size of 155.23 ± 1.35&#xa0;nm, zeta potential of -25.83 ± 1.26 mV, and encapsulation efficiency of 86.71 ± 2.41%, maintaining excellent refrigerated stability over 90 days. Both formulations exhibited sustained in vitro release and enhanced ex vivo corneal permeation. In vivo studies conducted on New Zealand rabbits showed that BIM-SBB-ISG and BIM-LBB-ISG exhibited a 37.66% (15.77 ± 0.61 mmHg) and 36.57% (16.22 ± 1.37 mmHg) reduction in IOP, respectively, at 24&#xa0;h. Pharmacokinetic analysis showed extended half-lives and AUC values compared to Lumigan<sup>®</sup>. In albino Wistar rats with corticosteroid-induced glaucoma, BIM-SBB-ISG lowered IOP from 38.24 ± 0.61 to 17.34 ± 0.98 mmHg (2.21-fold reduction), while BIM-LBB-ISG decreased IOP from 38.78 ± 2.57 to 18.46 ± 0.61 mmHg (2.10-fold reduction) over 24&#xa0;h. These results highlight the potential of BIM-SBB-ISG and BIM-LBB-ISG as promising alternatives for improved glaucoma management.</p> Graphical Abstract <p></p>

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Enhanced Ocular Delivery of Bimatoprost Using Surfactant and Lipid-Based Bilosomes in Situ Gel in Rabbits and Glaucoma-Induced Wistar Rats

  • 期刊论文

  • 发表日期：

    2026年1月8日

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  • Devansh Singhal,
  • Harsh P. Nijhawan,
  • Khushwant S. Yadav

摘要

Glaucoma, a leading cause of blindness, is caused by elevated intraocular pressure (IOP) that damages retinal ganglion cells. Current treatments, such as bimatoprost (BIM) eye drops, are limited by poor ocular bioavailability and rapid precorneal clearance. This study proposes a novel approach using BIM-loaded surfactant-based bilosomes (SBB) and lipid-based bilosomes (LBB) incorporated into an in situ gel (ISG) to enhance ocular drug delivery and therapeutic efficacy. Optimized formulations were obtained utilizing a 33-Box Behnken Design (BBD). SBB showed a particle size of 165.3 ± 5.32 nm, a zeta potential of -23.8 ± 5.32 mV, and an encapsulation efficiency of 83.92 ± 2.76%, while LBB exhibited a particle size of 155.23 ± 1.35 nm, zeta potential of -25.83 ± 1.26 mV, and encapsulation efficiency of 86.71 ± 2.41%, maintaining excellent refrigerated stability over 90 days. Both formulations exhibited sustained in vitro release and enhanced ex vivo corneal permeation. In vivo studies conducted on New Zealand rabbits showed that BIM-SBB-ISG and BIM-LBB-ISG exhibited a 37.66% (15.77 ± 0.61 mmHg) and 36.57% (16.22 ± 1.37 mmHg) reduction in IOP, respectively, at 24 h. Pharmacokinetic analysis showed extended half-lives and AUC values compared to Lumigan®. In albino Wistar rats with corticosteroid-induced glaucoma, BIM-SBB-ISG lowered IOP from 38.24 ± 0.61 to 17.34 ± 0.98 mmHg (2.21-fold reduction), while BIM-LBB-ISG decreased IOP from 38.78 ± 2.57 to 18.46 ± 0.61 mmHg (2.10-fold reduction) over 24 h. These results highlight the potential of BIM-SBB-ISG and BIM-LBB-ISG as promising alternatives for improved glaucoma management.

Graphical Abstract