Mahran Alaa, Ismail Sayed, Allam Ayat A
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, Sphinx University, New Assiut City, Assiut 71515, Egypt.
Pharmaceutics. 2021 Mar 25;13(4):444. doi: 10.3390/pharmaceutics13040444.
Treatment of uveitis (i.e., inflammation of the uvea) is challenging due to lack of convenient ophthalmic dosage forms. This work is aimed to determine the efficiency of triamcinolone acetonide (TA)-loaded microemulsion as an ophthalmic delivery system for the treatment of uveitis. Water titration method was used to construct different pseudo-ternary phase diagrams. Twelve microemulsion formulations were prepared using oleic acid, Cremophor EL, and propylene glycol. Among all tested formulations, Formulation F3, composed of oil: surfactant-co-surfactant (1:1): water (15:35:50% , respectively), was found to be stable and showed acceptable pH, viscosity, conductivity, droplet size (211 ± 1.4 nm), and zeta potential (-25 ± 1.7 mV) and almost complete in vitro drug release within 24 h. The in vivo performance of the optimized formulation was evaluated in experimentally uveitis-induced rabbit model and compared with a commercial TA suspension (i.e., Kenacort-A) either topically or by subconjunctival injection. Ocular inflammation was evaluated by clinical examination, white blood cell count, protein content measurement, and histopathological examination. The developed TA-loaded microemulsion showed superior therapeutic efficiency in the treatment of uveitis with high patient compliance compared to commercial suspension. Hence, it could be considered as a potential ocular treatment option in controlling of uveitis.
由于缺乏方便的眼科剂型,葡萄膜炎(即葡萄膜炎症)的治疗具有挑战性。这项工作旨在确定载有曲安奈德(TA)的微乳剂作为治疗葡萄膜炎的眼科给药系统的有效性。采用水滴定法构建不同的伪三元相图。使用油酸、聚氧乙烯蓖麻油(Cremophor EL)和丙二醇制备了12种微乳剂配方。在所有测试配方中,由油:表面活性剂-助表面活性剂(1:1):水(分别为15:35:50%)组成的F3配方被发现是稳定的,并且显示出可接受的pH值、粘度、电导率、液滴大小(211±1.4nm)和zeta电位(-25±1.7mV),并且在24小时内几乎完全体外药物释放。在实验性葡萄膜炎诱导的兔模型中评估了优化配方的体内性能,并与市售TA混悬液(即Kenacort-A)进行了局部或结膜下注射比较。通过临床检查、白细胞计数、蛋白质含量测量和组织病理学检查评估眼部炎症。与市售混悬液相比,所开发的载TA微乳剂在治疗葡萄膜炎方面显示出更高的治疗效率和患者依从性。因此,它可被视为控制葡萄膜炎的一种潜在眼部治疗选择。