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Purpose <p>Posaconazole is widely utilized as a salvage therapy, for the treatment of ocular mucormycosis in the patients who are intolerant to Amphotericin B, and also effective for the treatment of immunocompromised patient. Despite its therapeutic potential, oral administration of Posaconazole is hindered by erratic gastrointestinal absorption and variable systemic bioavailability, which may compromise treatment efficacy. Ocular administration of drug facilitates site specific drug delivery and reduced adverse effect associated with systemic administration. The present study focuses on the development and evaluation of Posaconazole loaded pH responsive ocular <i>in situ</i> gel, for the effective treatment of Mucormycosis by enhancing corneal drug retention. </p> Method <p>This dosage form was prepared by using the polymers; Carbopol 934 and HPMC K4M, which transit from solution to gel form upon contact with tear fluid. A 3² full factorial design was used for optimization and optimized formulation was evaluated for various physicochemical and performance parameters to determine its suitability for ocular administration. </p> Result <p>Optimized formulation exhibited sufficient gelling strength, only in 2-3 sec. The optimized batch PCZ05 exhibited the Viscosity 601 ± 12 cps and%drug release at 6 hr was found to be 90.87 ± 0.35. Texture analysis confirmed the physical characteristics for ocular application. Isotonicity study and sterility study established the compatibility and microbiological safety of developed preparation. The optimized formulation showed satisfactory antifungal activity; against<i>Candida albicans</i>. <i>Ex vivo</i> corneal retention study indicated localization of drug in cornea for 6 h. HET- CAM study (<i>In vitro</i> ocular irritation study) evidenced no ocular irritation of optimized formulation and well tolerated by eye. </p> Conclusion <p>The optimized Posaconazole loaded <i>in situ</i> gel formulation exhibited desirable physicochemical property, suitable for ocular administration. Further, <i>in vivo</i> studies and microbiological testing against Mucorales are required to establish its therapeutic potential.</p>

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Investigation of the Efficacy of A pH-Responsive Ocular in Situ Gel of Posaconazole: In Vitro and Ex Vivo Insights

  • 期刊论文

  • 发表日期：

    2026年2月16日

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  • Dipti Gohil,
  • Subham Jayswal,
  • Nirmal Shah,
  • Pranav Shah,
  • Meenakshi Patel

摘要

Purpose

Posaconazole is widely utilized as a salvage therapy, for the treatment of ocular mucormycosis in the patients who are intolerant to Amphotericin B, and also effective for the treatment of immunocompromised patient. Despite its therapeutic potential, oral administration of Posaconazole is hindered by erratic gastrointestinal absorption and variable systemic bioavailability, which may compromise treatment efficacy. Ocular administration of drug facilitates site specific drug delivery and reduced adverse effect associated with systemic administration. The present study focuses on the development and evaluation of Posaconazole loaded pH responsive ocular in situ gel, for the effective treatment of Mucormycosis by enhancing corneal drug retention.

Method

This dosage form was prepared by using the polymers; Carbopol 934 and HPMC K4M, which transit from solution to gel form upon contact with tear fluid. A 3² full factorial design was used for optimization and optimized formulation was evaluated for various physicochemical and performance parameters to determine its suitability for ocular administration.

Result

Optimized formulation exhibited sufficient gelling strength, only in 2-3 sec. The optimized batch PCZ05 exhibited the Viscosity 601 ± 12 cps and%drug release at 6 hr was found to be 90.87 ± 0.35. Texture analysis confirmed the physical characteristics for ocular application. Isotonicity study and sterility study established the compatibility and microbiological safety of developed preparation. The optimized formulation showed satisfactory antifungal activity; againstCandida albicans. Ex vivo corneal retention study indicated localization of drug in cornea for 6 h. HET- CAM study (In vitro ocular irritation study) evidenced no ocular irritation of optimized formulation and well tolerated by eye.

Conclusion

The optimized Posaconazole loaded in situ gel formulation exhibited desirable physicochemical property, suitable for ocular administration. Further, in vivo studies and microbiological testing against Mucorales are required to establish its therapeutic potential.