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<p>Glaucoma therapy is often limited by poor ocular bioavailability and the short residence time of conventional eye drops, highlighting the need for sustained-release delivery systems. This study presents the development of a thermosensitive <i>in situ</i> hydrogel incorporating cation-exchange resin (CER) for sustained delivery of betaxolol hydrochloride (BH) in glaucoma therapy. CER microspheres were prepared using a seed swelling method, and drug loading was achieved through an ion-exchange interaction to obtain BH@CER, which was characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and scanning electron microscopy (SEM). A thermosensitive hydrogel-microspheres composite (BH@CER@P407) was formulated using optimized concentrations of poloxamer 407 (P407), exhibiting a sol-to-gel transition at approximately 34°C for easy administration and prolonged ocular retention. <i>In vitro</i> release studies indicated that BH@CER@P407 achieved sustained release (85% over 12&#xa0;h), in contrast to the pronounced burst release of commercial BH eye drops (Betoptic® S, 90% within 2&#xa0;h). <i>In vivo</i> evaluations in New Zealand rabbits revealed strong ocular adhesion and retention for up to 8&#xa0;h, correlating with sustained intraocular pressure (IOP) reduction. Ocular irritation studies confirmed excellent biocompatibility. Compared to Betoptic® S, the BH@CER@P407 offers enhanced ocular residence and prolonged therapeutic efficacy, presenting a promising strategy for improving glaucoma treatment.&#xa0;</p> Graphical Abstract <p></p>

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Controlled Release of Thermosensitive Hydrogel Incorporating Betaxolol-Loaded Resin Microspheres for Glaucoma Therapy

  • 期刊论文

  • 发表日期：

    2026年3月17日

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  • Hongfei Liu,
  • Zhen Zhang,
  • Xinyi Tang,
  • Yingshu Feng,
  • Caleb Kesse Firempong,
  • Haibing He,
  • Guoqing Zhang

摘要

Glaucoma therapy is often limited by poor ocular bioavailability and the short residence time of conventional eye drops, highlighting the need for sustained-release delivery systems. This study presents the development of a thermosensitive in situ hydrogel incorporating cation-exchange resin (CER) for sustained delivery of betaxolol hydrochloride (BH) in glaucoma therapy. CER microspheres were prepared using a seed swelling method, and drug loading was achieved through an ion-exchange interaction to obtain BH@CER, which was characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and scanning electron microscopy (SEM). A thermosensitive hydrogel-microspheres composite (BH@CER@P407) was formulated using optimized concentrations of poloxamer 407 (P407), exhibiting a sol-to-gel transition at approximately 34°C for easy administration and prolonged ocular retention. In vitro release studies indicated that BH@CER@P407 achieved sustained release (85% over 12 h), in contrast to the pronounced burst release of commercial BH eye drops (Betoptic® S, 90% within 2 h). In vivo evaluations in New Zealand rabbits revealed strong ocular adhesion and retention for up to 8 h, correlating with sustained intraocular pressure (IOP) reduction. Ocular irritation studies confirmed excellent biocompatibility. Compared to Betoptic® S, the BH@CER@P407 offers enhanced ocular residence and prolonged therapeutic efficacy, presenting a promising strategy for improving glaucoma treatment. 

Graphical Abstract