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<p>Glaucoma, a leading cause of irreversible blindness, is driven by elevated intraocular pressure (IOP) and oxidative retinal damage. Resveratrol (RES), a polyphenolic antioxidant with neuroprotective activity, offers therapeutic potential but suffers from poor aqueous solubility and low ocular bioavailability. This study developed and evaluated a cationic phyto-microemulsion to enhance ocular delivery of RES. RES-loaded phyto-microemulsion (RES-ME) were formulated using isopropyl myristate, Tween 80, and propylene glycol, with stearylamine (SA) imparting positive surface charge. Optimized uncoated phyto-microemulsion (RTPG) and SA-coated phyto-microemulsion (SRTPG) were characterized for physicochemical properties, mucoadhesive strength, <i>in vitro</i> drug release, <i>ex vivo</i> goat corneal permeation, antioxidant activity, ocular irritation, and IOP-lowering efficacy in a dexamethasone-induced rat glaucoma model. SRTPG exhibited a globule size of 186.2 ± 6.24&#xa0;nm, PDI 0.147 ± 0.04, and zeta potential + 28 ± 4.56&#xa0;mV. Drug release was sustained (70–75% over 8&#xa0;h) and best fitted the Higuchi model (R2 &gt; 0.98). SRTPG achieved markedly higher corneal permeation (750.3&#xa0;µg/cm2) versus RTPG. HET-CAM and histology confirmed minimal irritancy and preserved corneal architecture. <i>In vivo</i>, SRTPG produced a maximal IOP reduction of 23.88% at 4&#xa0;h and prolonged efficacy (AUC₀–₈<sub>h</sub> = 114.28), comparable to dorzolamide. The enhanced performance is attributed to cationic surface charge–mediated mucoadhesion and lipidic microemulsion–facilitated transcorneal transport. SRTPG offer safe, sustained, and penetration-enhanced ocular delivery, with dual IOP-lowering and antioxidant effects, representing a promising nanocarrier platform for glaucoma management.</p> Graphical Abstract <p></p>

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Stearylamine-Coated Cationic Phyto-Microemulsions Enhance Resveratrol Ocular Delivery for Glaucoma Therapy: Experimental and Preclinical Insights

  • 期刊论文

  • 发表日期：

    2026年3月4日

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  • Jothimani Rajeswari,
  • Karthikeyan Kesavan,
  • Alpana Ram

摘要

Glaucoma, a leading cause of irreversible blindness, is driven by elevated intraocular pressure (IOP) and oxidative retinal damage. Resveratrol (RES), a polyphenolic antioxidant with neuroprotective activity, offers therapeutic potential but suffers from poor aqueous solubility and low ocular bioavailability. This study developed and evaluated a cationic phyto-microemulsion to enhance ocular delivery of RES. RES-loaded phyto-microemulsion (RES-ME) were formulated using isopropyl myristate, Tween 80, and propylene glycol, with stearylamine (SA) imparting positive surface charge. Optimized uncoated phyto-microemulsion (RTPG) and SA-coated phyto-microemulsion (SRTPG) were characterized for physicochemical properties, mucoadhesive strength, in vitro drug release, ex vivo goat corneal permeation, antioxidant activity, ocular irritation, and IOP-lowering efficacy in a dexamethasone-induced rat glaucoma model. SRTPG exhibited a globule size of 186.2 ± 6.24 nm, PDI 0.147 ± 0.04, and zeta potential + 28 ± 4.56 mV. Drug release was sustained (70–75% over 8 h) and best fitted the Higuchi model (R2 > 0.98). SRTPG achieved markedly higher corneal permeation (750.3 µg/cm2) versus RTPG. HET-CAM and histology confirmed minimal irritancy and preserved corneal architecture. In vivo, SRTPG produced a maximal IOP reduction of 23.88% at 4 h and prolonged efficacy (AUC₀–₈h = 114.28), comparable to dorzolamide. The enhanced performance is attributed to cationic surface charge–mediated mucoadhesion and lipidic microemulsion–facilitated transcorneal transport. SRTPG offer safe, sustained, and penetration-enhanced ocular delivery, with dual IOP-lowering and antioxidant effects, representing a promising nanocarrier platform for glaucoma management.

Graphical Abstract