Sustained release of brimonidine from conjunctival sac insert to reduce intraocular pressure for glaucoma treatment

被引：0
作者：
Zhang, Zhutian [1 ,2 ,3 ,4 ]
Ma, Qian [5 ]
Dai, Zhaoxing [6 ]
Hong, Jiaxu [1 ,2 ,3 ,4 ,7 ,8 ]
Gu, Jifeng [9 ]
Shi, Rong [10 ]
Xu, Jianjiang [1 ,2 ,3 ,4 ,7 ,8 ]
Ma, Yaling [5 ]
Sun, Xinghuai [1 ,2 ,3 ,4 ,7 ,8 ]
Sun, Jianguo [1 ,2 ,3 ,4 ,7 ,8 ]
机构：
[1] Fudan Univ, Eye & ENT Hosp, Eye Inst, Shanghai Med Coll, Shanghai, Peoples R China
[2] Fudan Univ, NHC Key Lab Myopia, Shanghai, Peoples R China
[3] Chinese Acad Med Sci, Key Lab Myopia, Shanghai, Peoples R China
[4] Shanghai Key Lab Visual Impairment & Restorat, Shanghai, Peoples R China
[5] Ningxia Med Univ, Gen Hosp, Dept Ophthalmol, Yinchuan, Ningxia, Peoples R China
[6] Shanghai Haohai Biol Technol Co Ltd, Shanghai, Peoples R China
[7] Fudan Univ, State Key Lab Med Neurobiol, Shanghai, Peoples R China
[8] Fudan Univ, Inst Brain Sci, MOE Frontiers Ctr Brain Sci, Shanghai, Peoples R China
[9] Fudan Univ, Eye & ENT Hosp, Dept Pharm, Shanghai Key Lab Bioact Small Mol, Shanghai, Peoples R China
[10] Shanghai Univ Tradit Chinese Med, Sci & Technol Expt Ctr, Shanghai, Peoples R China
来源：
EXPERT OPINION ON DRUG DELIVERY | 2024年 / 21卷 / 06期
基金：
中国国家自然科学基金; 上海市自然科学基金;
关键词：
Sustained release; conjunctival sac insert; brimonidine; intraocular pressure; glaucoma; BLOOD-BRAIN-BARRIER; STEM-CELL TRANSPLANTATION; TARGETED-DRUG-DELIVERY; FUSION PROTEIN; MONOCLONAL-ANTIBODY; PARKINSONS-DISEASE; ALZHEIMERS-DISEASE; TRANSPORT; CONJUGATE; GLYCOSOAMINOGLYCANS;
D O I：
10.1080/17425247.2024.2378082
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
BackgroundGlaucoma is one of the major irreversible blinding eye diseases in the world. Reducing intraocular pressure (IOP) is the primary treatment option, and taking eye drops daily is the common method. However, short drug duration and poor bioavailability of eye drops may lead to unsatisfied therapeutic effects and inadequate patient compliance.MethodsA brimonidine-loaded silicone rubber insert (BRI@SR@PT) was prepared by loading brimonidine into a surface-modified silicone rubber ring, followed by polydopamine/thermoplastic polyurethane coatings. The physical properties, in vitro cytocompatibility and drug release of BRI@SR@PT were investigated. The BRI@SR@PT was administrated in the conjunctival sac of rabbit eyes, and its in vivo drug release, IOP-lowering efficacy and biosafety were assessed.ResultsThe BRI@SR@PT presented great thermal stability and excellent elasticity. The BRI@SR@PT was able to release BRI sustainably for 28 days with little toxicity in vitro. Compared to BRI eye drops, the BRI@SR@PT effectively lowered IOP for 21 days based on the sustained BRI release with great biosafety when administrated in conjunctival sac of rabbit eyes in a noninvasive fashion.ConclusionsThe conjunctival sac insert (BRI@SR@PT), as a promising drug-delivery platform, may provide a sustained IOP-lowering treatment for patients with ocular hypertension or glaucoma, without the need for invasive procedures.
引用
收藏
页码：975 / 986
页数：12
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