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关于含有双分隔油滴的阳离子眼用乳剂以共同递送环孢素 A 和依托度酸的研究。

Studies on cationic ocular emulsions containing bipartitioned oil droplets to codeliver cyclosporin A and etodolac.

机构信息

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Guwahati, Assam, 781101, India.

Suria Eye Products Pvt. Ltd, BIO-NEST Incubation Centre, National Institute of Pharmaceutical Education and Research (NIPER), Guwahati, Assam, 781101, India.

出版信息

Nanomedicine (Lond). 2024;19(12):1035-1050. doi: 10.2217/nnm-2023-0364. Epub 2024 Apr 30.

Abstract

To prepare ocular emulsions containing bipartitioned oil droplets to entrap cyclosporin A (0.05% w/w) and etodolac (0.2% w/w) by using castor, olive and silicon oils. The physicochemical characterizations of prepared emulsions were performed. The drug's biodistribution profiles and pharmacokinetic parameters from emulsions were checked using the ultraperformance liquid chromatography-tandem mass spectrometry method in the ocular tissues of the healthy rabbit eye model. The emulsions displayed 365.13 ± 7.21 nm size and 26.45 ± 2.09 mV zeta potential. The ferrying of two drugs after releasing from emulsions occurred across corneal/conjunctival tissues to enter the vitreous and sclera following a single drop administration into the rabbit's eyes. The dual drug-loaded emulsions were more likely to produce synergistic anti-inflammatory activity for managing moderate-to-severe dry eye disease.

摘要

制备含有双分割油滴的眼部乳液,以包封环孢素 A(0.05%w/w)和依托度酸(0.2%w/w),使用蓖麻油、橄榄油和硅油。对制备的乳液进行理化特性分析。采用超高效液相色谱-串联质谱法检测健康兔眼模型眼部组织中药物的分布特征和药代动力学参数。乳液的粒径为 365.13±7.21nm,zeta 电位为 26.45±2.09mV。两种药物从乳液中释放后,通过角膜/结膜组织转运,滴注入兔眼后进入玻璃体和巩膜。双载药乳液更有可能产生协同抗炎活性,用于治疗中重度干眼疾病。

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