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Amelioration from the ocular irritant Capsaicin: development and assessment of a Capsazepine in situ gel system for ocular delivery.
Expert Opinion on Drug Delivery ( IF 5.0 ) Pub Date : 2020-04-24 , DOI: 10.1080/17425247.2020.1754396
Harshita Krishnatreyya 1, 2 , Hemanga Hazarika 1 , Achintya Saha 2 , Santa Mandal 1 , Nilutpal Sharma Bora 1 , Sumit Kishor 1 , Yangchen Doma Bhutia 1 , Danswrang Goyary 1 , Sanjeev Karmakar 1 , Pronobesh Chattopadhyay 1
Affiliation  

Background: Defense personnel utilize capsaicin-based ocular sprays as non-lethal agents for law implementation during instances of mob violence. This study involves the capsaicin antagonist Capsazepine and the investigation of whether Capsazepine's antagonistic approach can be favorably utilized for defense utilization to block capsaicin-initiated pain and inflammation via the ocular pathway.Research design and methods: Ocular capsazepine in situ gels were prepared with polymers Pluronic F-127 and Chitosan; optimized formulation was quantified in ocular tissues chromatographically and by in vivo live ocular imaging; anti-inflammatory efficacy was determined by eye irritation testing, corneal and retinal imaging, ocular prostaglandin estimation, and by viability and proliferation testing using human ocular cell lines, etc.Results: A physicochemically stable Capsazepine in situ gel was formulated which showed little ocular irritation, considerable transcorneal permeation; was precisely quantified in ocular tissues by gas chromatography and in vivo live ocular imaging; showed anti-inflammatory properties against capsaicin by eye imaging experiments, prostaglandin declination and showed acceptable cytocompatibility when studied using human ocular cell lines.Conclusions: The fabricated in situ Capsazepine gel system might be promising for ocular delivery as it appears a pharmacologically potent and safe development, suitable for utilization in the ocular clinical therapy, provided there is additional research to substantiate it.

中文翻译:

改善眼刺激性辣椒素:开发和评估用于眼部递送的辣椒素原位凝胶系统。

背景:国防人员在发生暴民暴力事件时,将基于辣椒素的眼用喷雾剂用作非致死剂,以执行法律。这项研究涉及辣椒素拮抗剂Capsazepine并研究了Capsazepine的拮抗方法是否可以有利地用于通过眼部途径阻断辣椒素引起的疼痛和炎症的防御利用。研究设计和方法:用聚合物Pluronic制备了眼部辣椒素原位凝胶F-127和壳聚糖;通过色谱法和体内活体眼部成像对优化后的配方进行定量。通过眼刺激测试,角膜和视网膜成像,前列腺素估计值以及使用人眼细胞系进行的活力和增殖测试等确定抗炎功效。配制了一种物理化学稳定的辣椒碱原位凝胶,该凝胶显示出很少的眼部刺激感,可观的角膜渗透性。通过气相色谱和体内活眼成像精确定量在眼组织中;通过人眼细胞系研究,通过眼部成像实验,辣椒素偏角化显示出对辣椒素的抗炎特性,并显示出可接受的细胞相容性。结论:原位制备的辣椒素凝胶系统有望在眼部递送,因为它在药理学上有效且安全地发展适用于眼科临床治疗,只要有其他研究可以证实。通过气相色谱和体内活眼成像精确定量在眼组织中;通过人眼细胞系研究,通过眼部成像实验,辣椒素偏角化显示出对辣椒素的抗炎特性,并显示出可接受的细胞相容性。结论:原位制备的辣椒素凝胶系统有望在眼部递送,因为它在药理学上有效且安全地发展适用于眼科临床治疗,只要有其他研究可以证实。通过气相色谱和体内活眼成像精确定量在眼组织中;通过人眼细胞系研究,通过眼部成像实验,辣椒素偏角化显示出对辣椒素的抗炎特性,并显示出可接受的细胞相容性。结论:原位制备的辣椒素凝胶系统有望在眼部递送,因为它在药理学上有效且安全地发展适用于眼科临床治疗,只要有其他研究可以证实。
更新日期:2020-04-24
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