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<p>Topical ocular drug delivery is greatly hindered by the fast tear turnover rate, blinking, and low corneal permeability, leading to poor bioavailability of conventional eye drops. The current study was designed to develop and optimize a new azithromycin-loaded spanlastic-laden in-situ gel (AZM-SL-ISG) to improve ocular dwell time, corneal permeability, and therapeutic outcomes. Ultra-deformable spanlastic vesicles were successfully formulated with Span 60 and Tween 80 using the thin-film hydration technique and optimized by 3² full factorial design. The optimized formulation showed a nanoscale vesicle size (~ 175&#xa0;nm), high entrapment efficiency (~ 88%), and satisfactory colloidal stability. The optimized spanlastics were then loaded into a pH-triggered Carbopol 940 in-situ gel, which underwent rapid sol-to-gel transition at the physiological ocular pH. In-vitro release studies established a sustained release profile compared to plain spanlastics. The formulation exhibited excellent ocular tolerance without any indication of irritation in rabbit eyes. In-vivo precorneal residence and ocular pharmacokinetic evaluations indicated a significantly prolonged residence time and improved aqueous humor bioavailability compared to commercial azithromycin eye drops. In conclusion, the complementary approach of elastic spanlastic vesicles and a mucoadhesive in-situ gel system provides a promising and patient-friendly approach for the enhanced ocular delivery of azithromycin in the treatment of bacterial eye infections.</p> Graphical abstract <p></p>

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Quality-by-Design Optimization of Azithromycin-Loaded Spanlastic-Based pH-Triggered In-Situ Gel for Enhanced Ocular Bioavailability

  • 期刊论文

  • 发表日期：

    2026年7月16日

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  • Hitesh Kumar Dewangan,
  • Bharat Bhushan,
  • Mohamed Rahamathulla,
  • Lamyaa M. kassem,
  • Mohammed Muqtader Ahmed

摘要

Topical ocular drug delivery is greatly hindered by the fast tear turnover rate, blinking, and low corneal permeability, leading to poor bioavailability of conventional eye drops. The current study was designed to develop and optimize a new azithromycin-loaded spanlastic-laden in-situ gel (AZM-SL-ISG) to improve ocular dwell time, corneal permeability, and therapeutic outcomes. Ultra-deformable spanlastic vesicles were successfully formulated with Span 60 and Tween 80 using the thin-film hydration technique and optimized by 3² full factorial design. The optimized formulation showed a nanoscale vesicle size (~ 175 nm), high entrapment efficiency (~ 88%), and satisfactory colloidal stability. The optimized spanlastics were then loaded into a pH-triggered Carbopol 940 in-situ gel, which underwent rapid sol-to-gel transition at the physiological ocular pH. In-vitro release studies established a sustained release profile compared to plain spanlastics. The formulation exhibited excellent ocular tolerance without any indication of irritation in rabbit eyes. In-vivo precorneal residence and ocular pharmacokinetic evaluations indicated a significantly prolonged residence time and improved aqueous humor bioavailability compared to commercial azithromycin eye drops. In conclusion, the complementary approach of elastic spanlastic vesicles and a mucoadhesive in-situ gel system provides a promising and patient-friendly approach for the enhanced ocular delivery of azithromycin in the treatment of bacterial eye infections.

Graphical abstract