Pharmacy Department, The Maharaja Sayajirao University of Baroda, Fatehgunj, Vadodara, India.
Division of Phytotherapeutics and Metabolic Endocrinology, Department of Zoology, The Maharaja Sayajirao University of Baroda, Vadodara, India.
Pharm Dev Technol. 2023 Jul;28(6):535-546. doi: 10.1080/10837450.2023.2216784. Epub 2023 May 25.
In this work, novel carriers- nanoemulsomes (NE) of ganciclovir (GCV) and a fluorescent marker sodium fluorescein (SF) were developed and evaluated for posterior ocular delivery topical route. GCV loaded emulsomes (GCV NE) were optimized by a factorial design and various characterization parameters were performed on the optimized batch. The optimized batch had particle size of 131.04 ± 1.87 nm, % entrapment efficiency of 36.42 ± 3.09% and its TEM image showed discrete spherical structures below 200 nm. Ocular irritation potential of excipients and formulation were evaluated by cell line based tests on SIRC cell line, results confirmed the safety of excipients for ocular use. Precorneal retention and pharmacokinetic studies of GCV NE were performed in rabbit eyes which showed significant retention of GCV NE in the cul-de-sac. The ocular distribution study of SF-loaded nanoemulsomes (SF NE) were performed in mice eyes by confocal microscopy, images showed fluorescence in the various internal layers of retina, suggesting efficacy of emulsomes in delivering agents to the back of eye topical administration.
在这项工作中，我们开发并评估了新型载体——更昔洛韦（GCV）的纳米乳剂（NE）和荧光标记物荧光素钠（SF），用于眼部后段的局部给药途径。通过析因设计对载有更昔洛韦的乳剂（GCV NE）进行了优化，并对优化批次进行了各种特性参数的评估。优化批次的粒径为 131.04±1.87nm，包封率为 36.42±3.09%，其 TEM 图像显示出低于 200nm 的离散球形结构。通过基于细胞系的 SIRC 细胞系测试评估了辅料和制剂的眼部刺激性，结果证实了辅料用于眼部的安全性。在兔眼进行了 GCV NE 的角膜前滞留和药代动力学研究，结果表明 GCV NE 在结膜囊中有明显的滞留。通过共聚焦显微镜对 SF 载纳米乳剂（SF NE）在小鼠眼部的分布进行了研究，图像显示荧光分布在视网膜的各个内层，表明乳剂在通过局部给药将药物递送至眼后段方面的有效性。
