在健康兔内耳模型中鼓膜内注射乳剂样分散体以增加辛那利嗪的用量。

IF 3.9 Nanomedicine (London, England) Pub Date : 2024-01-01 Epub Date: 2024-07-23 DOI:10.1080/17435889.2024.2373042
Abhinab Goswami, Syed Nazrin Ruhina Rahman, Srikanth Ponneganti, Vijayakumar Gangipangi, Hariprasad Vavialala, Pullapanthula Radhakrishnanand, Sudhagar Selvaraju, Srinivasa Rao Mutheneni, Shreekant Bharti, Tamilvanan Shunmugaperumal
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摘要

目的:在健康兔内耳模型中研究共晶液体乳剂样分散体用于耳内注射以增强辛那利定在圆窗膜上的通透性。方法:采用双层系统优化方法获得注射剂配方。通过超高效液相色谱-串联质谱法分析了耳周和血浆中的药物浓度。超高效液相色谱-串联质谱法分析兔子耳内注射后 30、60、90 和 120 分钟的药物浓度。结果显示在分散体中观察到了剪切稀化行为、药物的即时释放(10 分钟内释放率为 98.80%)和较高的细胞存活率(24 小时内释放率大于 97.86%)。在兔子耳内注射后 30 分钟,观察到其耳周液中的辛那利嗪水平为 8168.57 ± 1236.79 ng/ml。结论乳液状分散体可增强药物通过圆窗膜的渗透性。
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Intratympanic injections of emulsion-like dispersions to augment cinnarizine amount in a healthy rabbit inner ear model.

Aim: To investigate eutectic liquid-based emulsion-like dispersions for intratympanic injections to augment cinnarizine permeability across round window membrane in a healthy rabbit inner ear model.Methods: Two-tier systematic optimization was used to get the injection formula. The drug concentrations in perilymph and plasma were analyzed via. Ultra-performance liquid chromatography-tandem mass spectrometry method after 30-, 60-, 90- and 120-min post intratympanic injection time points in rabbits.Results: A shear-thinning behavior, immediate drug release (∼98.80%, 10 min) and higher cell viability (>97.86%, 24 h) were observed in dispersions. The cinnarizine level of 8168.57 ± 1236.79 ng/ml was observed in perilymph at 30 min post intratympanic injection in rabbits.Conclusion: The emulsion-like dispersions can augment drug permeability through round window membrane.

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