Nirbhavane Pradip, Moksha Laxmi, Sharma Gajanand, Velpandian Thirumurthy, Singh Bhupinder, Katare O P
UGC-Centre of Advanced Study, Division of Pharmaceutics, University Institute of Pharmaceutical Sciences (UIPS), Panjab University, Chandigarh 160014, India.
Dr. Rajendra Prasad Centre for Ophthalmic Sciences, Ocular Pharmacology and Pharmacy Division, All India Institute of Medical Sciences, New Delhi 110029, India.
Life (Basel). 2023 Apr 20;13(4):1057. doi: 10.3390/life13041057.
The current study was undertaken to evaluate the efficacy of a novel nano-lipoidal eye drop formulation of triamcinolone acetonide (TA) for the topical treatment of uveitis. The triamcinolone acetonide-loaded nanostructured lipid carriers (cTA-NLC) were developed by employing 'hot microemulsion method' using biocompatible lipids, which exhibited a sustained release nature and enhanced efficacy when evaluated in vitro. The in vivo efficacy of this developed formulation was tested on Wistar rats, and a single-dose pharmacokinetic study was conducted in rabbits. The eyes of animals were examined for any signs of inflammation using the 'Slit-lamp microscopic' method. The aqueous humor collected from the sacrificed rats was tested for total protein count and cell count. The total protein count was determined using BSA assay method, while the total cell count was determined by Neubaur's hemocytometer method. The results showed that the cTA-NLC formulation had negligible signs of inflammation, with a clinical score of uveitis 0.82 ± 0.166, which is much less than control/untreated (3.80 ± 0.3) and free drug suspension (2.66 ± 0.405). The total cell count was also found to be significantly low for cTA-NLC (8.73 ± 1.79 × 10) as compared to control (52.4 ± 7.71 × 10) and free drug suspension (30.13 ± 3.021 × 10). Conclusively, the animal studies conducted showed that our developed formulation holds the potential for effective management of uveitis.
本研究旨在评估一种新型曲安奈德纳米脂质滴眼剂用于葡萄膜炎局部治疗的疗效。采用“热微乳法”，使用生物相容性脂质制备了载曲安奈德的纳米结构脂质载体（cTA-NLC），体外评估显示其具有缓释特性且疗效增强。在Wistar大鼠上测试了该制剂的体内疗效，并在兔身上进行了单剂量药代动力学研究。使用“裂隙灯显微镜”方法检查动物眼睛是否有炎症迹象。对处死大鼠收集的房水进行总蛋白计数和细胞计数检测。总蛋白计数采用牛血清白蛋白（BSA）测定法，总细胞计数采用Neubauer血细胞计数板法测定。结果显示，cTA-NLC制剂的炎症迹象可忽略不计，葡萄膜炎临床评分为0.82±0.166，远低于对照组/未治疗组（3.80±0.3）和游离药物混悬液组（2.66±0.405）。与对照组（52.4±7.71×10）和游离药物混悬液组（30.13±3.021×10）相比，cTA-NLC的总细胞计数也显著较低（8.73±1.79×10）。总之，所进行的动物研究表明，我们开发的制剂具有有效治疗葡萄膜炎的潜力。
