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<p>In the present study, brinzolamide&#xa0;(BRZ)&#xa0;—an anti-glaucoma drug was formulated into microsponge-loaded in situ gel for improved ophthalmic delivery. Microsponges were developed using solvent emulsion diffusion method comprising Eudragit RL-100. Further, microsponges integrated into in situ gel to provide longer residence into eyes. Various formulation and process parameters affecting microsponge characteristics were optimized. Amongst different formulations, S14 formulation with 2:1 drug-polymer ratio showed highest entrapment efficiency (93%), smallest particle size 10.3&#xa0;μm and polydispersity index 0.22, useful for ocular delivery. Further, S14 batch was embedded into in situ gel comprising poloxamer 407 and poloxamer 188 in combination (ISG I) and poloxamer 407 alone (ISG II). In situ gel was assessed for various physicochemical and rheological properties. Biological tests like HET-CAM assay, corneal irritation test and in vivo efficacy study were performed to assess suitability for ocular delivery. In vivo studies revealed that both ISG I and ISG II exhibited superior therapeutic efficacy (achieved grater reduction in intraocular pressure) and were non-irritant to rabbit eyes. The sustained drug release and improved ocular properties reflect that ISG I and ISG II have the capability to improve glaucoma treatment. To conclude, BRZ microsponge-loaded in situ gel puts forward possible, effective alternate delivery system for effective glaucoma management.</p> Graphical Abstract <p></p>

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Brinzolamide microsponge-loaded in situ gel for sustained ocular delivery: design, characterization and in vivo evaluation

  • 期刊论文

  • 发表日期：

    2026年4月21日

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  • Babita Agarwal,
  • Shivshankar Chandapure,
  • Aditya Kakad,
  • Namdev More,
  • Prabhakar Panzade,
  • Pavan Rathi,
  • Pravin Patil,
  • Sachin Jagdale

摘要

In the present study, brinzolamide (BRZ) —an anti-glaucoma drug was formulated into microsponge-loaded in situ gel for improved ophthalmic delivery. Microsponges were developed using solvent emulsion diffusion method comprising Eudragit RL-100. Further, microsponges integrated into in situ gel to provide longer residence into eyes. Various formulation and process parameters affecting microsponge characteristics were optimized. Amongst different formulations, S14 formulation with 2:1 drug-polymer ratio showed highest entrapment efficiency (93%), smallest particle size 10.3 μm and polydispersity index 0.22, useful for ocular delivery. Further, S14 batch was embedded into in situ gel comprising poloxamer 407 and poloxamer 188 in combination (ISG I) and poloxamer 407 alone (ISG II). In situ gel was assessed for various physicochemical and rheological properties. Biological tests like HET-CAM assay, corneal irritation test and in vivo efficacy study were performed to assess suitability for ocular delivery. In vivo studies revealed that both ISG I and ISG II exhibited superior therapeutic efficacy (achieved grater reduction in intraocular pressure) and were non-irritant to rabbit eyes. The sustained drug release and improved ocular properties reflect that ISG I and ISG II have the capability to improve glaucoma treatment. To conclude, BRZ microsponge-loaded in situ gel puts forward possible, effective alternate delivery system for effective glaucoma management.

Graphical Abstract