Scholarlink

Background: The delivery of medicament to eye faces difficulties due to the complex structure and presence of different static and dynamic barriers of eye. Aim: The present investigates improvement of the aqueous solubility of a poorly soluble itraconazole as solid dispersion with soluplus and to study the effect of different preservatives and application of iontophoresis on transcorneal permeation. Methods: Itraconazole solid dispersion was prepared and characterized by FTIR spectroscopy, differential scanning calorimetry and X-ray powder diffraction. Then aqueous isotonic ophthalmic solution of itraconazole (pH 7.2) 0.03% W/V containing different preservatives were developed and in vitro permeation, corneal hydration and antifungal activity were studied. Results: FTIR study revealed absence of any significant interactions between Itraconazole and soluplus. The drug was in an amorphous state or as a solid solution in the prepared solid dispersion supported by DSC thermograms and P-XRD study. The aqueous solubility of Itraconazole was found as 386.02 ± 9.4 μg/ml from solid dispersion of drug to soluplus ratio 1:10. In-vitro transcorneal permeation showed maximum percentage permeation of itraconazole from the formulation containing BA (10.93 ± 0.14) followed by formulation containing MP + PP (7.94 ± 0.26) and BKC + EDTA (6.81 ± 0.19) after 2 h. In iontophoretic study, increase in current intensity from 0.5 to 1.5 mA and iontophoresis time duration from 5 min to 15 min resulted in increased in drug permeation. Corneal hydration level was studied to assess the possible corneal damage due to electric treatment. The antifungal activity of the formulations against Aspergillus flavus determined by disk diffusion method suggested formulation containing BKC + EDTA showed the maximum zone of inhibition (14.33 ± 0.58 mm) compared to other formulations. Conclusion: Hence combinational effect of iontophoresis and BKC + EDTA as preservative has significant role enhancing the corneal permeation and antifungal activity that will potentially enhance the bioavailability of itraconazole to eye.

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Combination of Solid Dispersion and Potential Iontophoresis for Improving Transcorneal In Vitro Permeation of Itraconazole

  • 会议论文

  • 发表日期：

    2026年

查看全文
  • Swagatika Das,
  • Biswaranjan Mohanty,
  • Bibaswan Mishra,
  • Bhabani Shankar Nayak

摘要

Background: The delivery of medicament to eye faces difficulties due to the complex structure and presence of different static and dynamic barriers of eye. Aim: The present investigates improvement of the aqueous solubility of a poorly soluble itraconazole as solid dispersion with soluplus and to study the effect of different preservatives and application of iontophoresis on transcorneal permeation. Methods: Itraconazole solid dispersion was prepared and characterized by FTIR spectroscopy, differential scanning calorimetry and X-ray powder diffraction. Then aqueous isotonic ophthalmic solution of itraconazole (pH 7.2) 0.03% W/V containing different preservatives were developed and in vitro permeation, corneal hydration and antifungal activity were studied. Results: FTIR study revealed absence of any significant interactions between Itraconazole and soluplus. The drug was in an amorphous state or as a solid solution in the prepared solid dispersion supported by DSC thermograms and P-XRD study. The aqueous solubility of Itraconazole was found as 386.02 ± 9.4 μg/ml from solid dispersion of drug to soluplus ratio 1:10. In-vitro transcorneal permeation showed maximum percentage permeation of itraconazole from the formulation containing BA (10.93 ± 0.14) followed by formulation containing MP + PP (7.94 ± 0.26) and BKC + EDTA (6.81 ± 0.19) after 2 h. In iontophoretic study, increase in current intensity from 0.5 to 1.5 mA and iontophoresis time duration from 5 min to 15 min resulted in increased in drug permeation. Corneal hydration level was studied to assess the possible corneal damage due to electric treatment. The antifungal activity of the formulations against Aspergillus flavus determined by disk diffusion method suggested formulation containing BKC + EDTA showed the maximum zone of inhibition (14.33 ± 0.58 mm) compared to other formulations. Conclusion: Hence combinational effect of iontophoresis and BKC + EDTA as preservative has significant role enhancing the corneal permeation and antifungal activity that will potentially enhance the bioavailability of itraconazole to eye.