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<p>Limited contact time and low permeation of ophthalmic preparations due to lacrimal flow remained challenging and should be addressed by modification of therapeutic agents or addition of excipient for improving absorption across corneal epithelium.&#xa0;After phase solubility studies of Cur in different concentrations of PEG-6000, optimized Cur to PEG ratio (1:3) was selected for SD-Cur complex. Ophthalmic ointments of Cur and SD-Cur were successfully prepared by fusion method and characterized by content uniformity, pH and FTIR studies. Corneal membrane permeation, mucus permeability and antibacterial effects were also studied for evaluation of electrostatic bridging of benzalkonium chloride (BKC) with sialic acid.&#xa0;Results revealed that 20 folds increase in solubility of SD-Cur, up to 50% increase in diffusion through corneal epithelium may be due to hydrogen bonding of BKC with sialic acid, presence of PEG-6000 in SD-Cur and BKC in ointment also improved three folds permeation of Cur. Interestingly, maximum zone of inhibition (ZOI) of optimized SD-Cur-3-B was 95 ± 0.234 and 76 ± 0.543% against “<i>Staphylococcus aureus”</i> and “<i>Pseudomonas aeruginosa”</i> respectively confirmed its antibacterial behavior.&#xa0;In conclusion, SD-Cur and presence of sialic acid on corneal epithelium through electrostatic linkage with BKC of optimized ointment not only improve corneal contact time but also enhance the adequate epithelial permeability.</p> Graphical abstract <p></p>

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Improved corneal permeability of solidly dispersed curcumin by electrostatic bridging of benzalkonium chloride-sialic acid: in-vitro and ex-vivo approaches

  • 期刊论文

  • 发表日期：

    2026年5月26日

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  • Nabeela Ameer,
  • Hina Batool,
  • Muhammad Azeem,
  • Shahid Shah,
  • Fazal Rahman Sajid Chughtai,
  • Muhammad Hanif,
  • Khalid Mahmood,
  • Asad Majeed Khan,
  • Asma Aslam

摘要

Limited contact time and low permeation of ophthalmic preparations due to lacrimal flow remained challenging and should be addressed by modification of therapeutic agents or addition of excipient for improving absorption across corneal epithelium. After phase solubility studies of Cur in different concentrations of PEG-6000, optimized Cur to PEG ratio (1:3) was selected for SD-Cur complex. Ophthalmic ointments of Cur and SD-Cur were successfully prepared by fusion method and characterized by content uniformity, pH and FTIR studies. Corneal membrane permeation, mucus permeability and antibacterial effects were also studied for evaluation of electrostatic bridging of benzalkonium chloride (BKC) with sialic acid. Results revealed that 20 folds increase in solubility of SD-Cur, up to 50% increase in diffusion through corneal epithelium may be due to hydrogen bonding of BKC with sialic acid, presence of PEG-6000 in SD-Cur and BKC in ointment also improved three folds permeation of Cur. Interestingly, maximum zone of inhibition (ZOI) of optimized SD-Cur-3-B was 95 ± 0.234 and 76 ± 0.543% against “Staphylococcus aureus” and “Pseudomonas aeruginosa” respectively confirmed its antibacterial behavior. In conclusion, SD-Cur and presence of sialic acid on corneal epithelium through electrostatic linkage with BKC of optimized ointment not only improve corneal contact time but also enhance the adequate epithelial permeability.

Graphical abstract