Formulation and Evaluation of Ion-Triggered In situ gel for Effective Ocular Delivery of Ciprofloxacin HCl and Olopatadine HCl in Combination

Q2 Pharmacology, Toxicology and Pharmaceutics Drug Delivery Letters Pub Date : 2023-12-05 DOI:10.2174/0122103031267809231128111259
D. A. Shaikh, Munira M. M. Momin
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Abstract

Ocular in situ gels (ISG) are an adequate substitute to overcome the pitfalls of conventional eye drops as they acquaintance the advantages of solutions, including accuracy, dosing frequency, and ease of administration with prolonged contact with the ocular membrane. The present investigation aims to develop the ion-triggered in situ gel (ITISG) system for the convenient administration of Ciprofloxacin HCl (CFH) and Olopatadine HCl (OLH) in combination by employing gellan gum to prolong the pre-corneal residence, optic bioavailability and declines dosing frequency. The ISG material and critical quality attributes (CQA) were identified. Quality by Design (QbD) was established to optimize the formulation. Nine experimental formulations were designed (F1-F9) and assigned to distinct physicochemical and in vitro examinations Optimized batch F2 exhibited all the findings within acceptable limits. The Ion-triggered ISG technique exhibits maximum drug release over a 240-min cycle, much more significant than conventional eyedrops (60 min), suggesting sustained drug distribution and superior corneal penetration and absorption. Comprehensive findings of the present investigation conclude that the CFH and OLH would be effectively formulated as an ion-triggered ISG system to manage several draw-backs associated with prolonged release, ocular retention, and better corneal penetration com-pared with conventional eyedrops.
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离子触发原位凝胶的制备与评估:盐酸环丙沙星和盐酸奥洛他定的有效眼部给药组合
眼原位凝胶(ISG)是克服传统滴眼液缺陷的适当替代品,因为它们了解溶液的优点,包括准确性,给药频率,易于与眼膜长时间接触。本研究旨在利用结冷胶延长环丙沙星(CFH)和奥洛帕他定(OLH)在角膜前的停留时间、光学生物利用度和降低给药频率,建立离子触发原位凝胶(ITISG)系统,方便环丙沙星(CFH)和奥洛帕他定(OLH)联合给药。确定了ISG材料和关键质量属性(CQA)。建立质量设计法(QbD),对配方进行优化。设计了9个实验配方(F1-F9),并进行了不同的理化和体外检查,优化批次F2的所有结果都在可接受的范围内。离子触发ISG技术在240分钟的周期内显示出最大的药物释放,比传统滴眼液(60分钟)显著得多,表明药物持续分布和更好的角膜渗透和吸收。本研究的综合结果表明,与传统滴眼液相比,CFH和OLH可以有效地作为离子触发的ISG系统来管理与释放时间延长、眼潴留和更好的角膜穿透有关的几个缺点。
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来源期刊
Drug Delivery Letters
Drug Delivery Letters Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.70
自引率
0.00%
发文量
30
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