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<p>Brinzolamide (BRZ) is a carbonic anhydrase inhibitor for primary open-angle glaucoma (POAG) and ocular hypertension (OH). However, it suffers from poor aqueous solubility, leading to irritation and reduced patient compliance. This study introduces a novel β-cyclodextrin (β-CD)-based micellar formulation (MCLs) to improve solubility, safety, and therapeutic performance. BRZ micellar formulations (BRZ-MCLs) were developed using Pluronic F68/F127 and β-CD to enhance solubility. Characterization included particle size, polydispersity index (PDI), entrapment efficiency (EE%), and in vitro release. Irritation was assessed via HET-CAM (Hen’s Egg Chorioallantoic Membrane) and Draize tests. Molecular docking (PDB ID: 4M2R) and TOPKAT predicted stable binding and favorable safety. The optimized BRZ-MCLs showed a particle size of 80 ± 7.7&#xa0;nm, low PDI (0.145 ± 0.06), negative ZP (− 11.8 ± 0.21), and high EE% (81.95 ± 1.62%). They achieved sustained drug release (85 ± 0.275% over 72&#xa0;h), significantly higher than the BRZ suspension (69 ± 0.202%). Molecular docking indicated stable BRZ binding with THR A: 200, PHE A:131, and PRO A:202. Toxicity assessments confirmed BRZ-MCLs were non-irritating (irritation score (IS) = 0) and non-mutagenic. This β-CD micellar system offers a novel, patient-friendly strategy for ocular BRZ delivery, addressing solubility and irritation issues while enhancing therapeutic outcomes in glaucoma management.</p> Graphical Abstract <p>Graphical representation of the development of BRZ micelles. The BRZ/β-CD inclusion complex was evaluated using a phase solubility study to optimize the micellar formulation. HET-CAM test and in vivo studies were performed to assess ocular irritation to evaluate the safety profile of the formulation.</p> <p></p>

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Enhanced ocular delivery of brinzolamide via β-cyclodextrin-based micelles for glaucoma management

  • 期刊论文

  • 发表日期：

    2025年11月24日

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  • Rashmi Maurya,
  • Akash Vikal,
  • Raj Kumar Narang,
  • Preeti Patel,
  • Balak Das Kurmi

摘要

Brinzolamide (BRZ) is a carbonic anhydrase inhibitor for primary open-angle glaucoma (POAG) and ocular hypertension (OH). However, it suffers from poor aqueous solubility, leading to irritation and reduced patient compliance. This study introduces a novel β-cyclodextrin (β-CD)-based micellar formulation (MCLs) to improve solubility, safety, and therapeutic performance. BRZ micellar formulations (BRZ-MCLs) were developed using Pluronic F68/F127 and β-CD to enhance solubility. Characterization included particle size, polydispersity index (PDI), entrapment efficiency (EE%), and in vitro release. Irritation was assessed via HET-CAM (Hen’s Egg Chorioallantoic Membrane) and Draize tests. Molecular docking (PDB ID: 4M2R) and TOPKAT predicted stable binding and favorable safety. The optimized BRZ-MCLs showed a particle size of 80 ± 7.7 nm, low PDI (0.145 ± 0.06), negative ZP (− 11.8 ± 0.21), and high EE% (81.95 ± 1.62%). They achieved sustained drug release (85 ± 0.275% over 72 h), significantly higher than the BRZ suspension (69 ± 0.202%). Molecular docking indicated stable BRZ binding with THR A: 200, PHE A:131, and PRO A:202. Toxicity assessments confirmed BRZ-MCLs were non-irritating (irritation score (IS) = 0) and non-mutagenic. This β-CD micellar system offers a novel, patient-friendly strategy for ocular BRZ delivery, addressing solubility and irritation issues while enhancing therapeutic outcomes in glaucoma management.

Graphical Abstract

Graphical representation of the development of BRZ micelles. The BRZ/β-CD inclusion complex was evaluated using a phase solubility study to optimize the micellar formulation. HET-CAM test and in vivo studies were performed to assess ocular irritation to evaluate the safety profile of the formulation.