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局部用他克莫司前体药物纳米囊泡作为实验性干眼症综合征的一种潜在治疗方法。

Topical Tacrolimus Progylcosomes Nano-Vesicles As a Potential Therapy for Experimental Dry Eye Syndrome.

作者信息

Garg Vaidehi, Nirmal Jayabalan, Warsi Musarrat H, Pandita Deepti, Kesharwani Prashant, Jain Gaurav Kumar

机构信息

Department of Pharmaceutics, School of Pharmaceutical Education & Research, Jamia Hamdard, Hamdard Nagar, New Delhi 110062, India.

Translational Pharmaceutics Research Laboratory, Department of Pharmacy, BITS Pilani, Hyderabad 500078, India.

出版信息

J Pharm Sci. 2022 Feb;111(2):479-484. doi: 10.1016/j.xphs.2021.09.038. Epub 2021 Sep 29.

Abstract

The present work aimed to evaluate the efficacy of topical tacrolimus (0.01%) loaded propylene glycol (PG) modified nano-vesicles (Proglycosomes Nano-vesicles, PNVs) for the treatment of experimental dry eye syndrome (DES) in rabbits. DES was induced by topical application of atropine (1.0%) and benzalkonium chloride (0.1%) aqueous solution. PNVs treatment (PNV group) was compared with tacrolimus solution 0.01% (TAC group) and untreated group and healthy group were used as controls. PNV treated animals showed improved clinical performance with marked increase in tear production and tear break-up time (TBUT). Further, PNVs also subside ocular inflammation as evident from absence of matrix metalloprotenaise-9 and normal ocular surface temperature (32.3 ± 0.34 °C). Additionally, PNVs have positive effect on ocular and epithelial damage observed through low ocular surface staining score and improved globlet cell density. The PNV treatment was found to more effectively compared to TAC solution and most of the parameters were close to those of healthy animals. In conclusion, tacrolimus PNV formulation (0.01%) could be a potential therapy for treatment of dry eye syndrome.

摘要

本研究旨在评估负载0.01%他克莫司的丙二醇(PG)修饰纳米囊泡(Proglycosomes纳米囊泡,PNVs)治疗兔实验性干眼综合征(DES)的疗效。通过局部应用1.0%阿托品和0.1%苯扎氯铵水溶液诱导DES。将PNVs治疗组(PNV组)与0.01%他克莫司溶液组(TAC组)进行比较,未治疗组和健康组作为对照。接受PNVs治疗的动物临床症状改善,泪液分泌显著增加,泪膜破裂时间(TBUT)延长。此外,PNVs还能减轻眼部炎症,这从基质金属蛋白酶-9的缺失和正常眼表温度(32.3±0.34℃)可以明显看出。此外,通过低眼表染色评分和改善杯状细胞密度可以观察到PNVs对眼表和上皮损伤有积极作用。发现PNV治疗比TAC溶液更有效,大多数参数接近健康动物。总之,0.01%他克莫司PNV制剂可能是治疗干眼综合征的一种潜在疗法。

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