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使用溶胶-凝胶介孔二氧化硅作为控释系统的单次结膜下注射制剂,用于白内障手术后无需滴眼护理。

Single subconjunctival injection formulation using sol-gel mesoporous silica as a controlled release system for drop-free post-cataract surgery care.

作者信息

Sun Yaoyao, Huffman Kristyn, Freeman William R, Cheng Lingyun

机构信息

From the Department of Ophthalmology, Jacobs Retina Center at Shiley Eye Institute, University of California San Diego, La Jolla, California, USA. Y. Sun is now at the Department of Ophthalmology, Ophthalmology & Optometry Center, Peking University People's Hospital, Beijing, China.

出版信息

J Cataract Refract Surg. 2020 Nov;46(11):1548-1553. doi: 10.1097/j.jcrs.0000000000000366.

Abstract

PURPOSE

To develop a mesoporous silica drug delivery system and target drop-free care after cataract surgery with a single subconjunctival injection.

SETTING

Laboratory.

DESIGN

Experimental animal study.

METHODS

Ketorolac was infiltration-loaded into sol-gel mesoporous silica particles encapsulated with poly(allylamine hydrochloride) and poly(sodium 4-styrenesulfonate) using a layer-by-layer adsorption technique (SG-Ket-LBL). The formulation was subjected to an in vitro and in vivo drug release study in addition to ocular toxicology evaluation.

RESULTS

Thermogravimetric analysis revealed that the drug loading efficiency was 4.4% for the SG-Ket-LBL particles. The in vivo safety study demonstrated that the formulation was well tolerated after subconjunctival injection and aqueous humor pharmacokinetics showed sustained therapeutic drug release for the targeted time window of 6 to 8 weeks.

CONCLUSIONS

Findings indicated that sol-gel mesoporous silica could be used as a drug carrier for subconjunctival administration. The tested formulation, SG-Ket-LBL, provided therapeutic ketorolac for 6 to 8 weeks, which might be used for a single subconjunctival injection to replace nonsteroidal anti-inflammatory drug eyedrops after cataract surgery.

摘要

目的

开发一种介孔二氧化硅药物递送系统,通过单次结膜下注射实现白内障手术后无滴剂护理。

设置

实验室。

设计

实验动物研究。

方法

使用逐层吸附技术(SG-Ket-LBL)将酮咯酸渗透加载到包裹有聚(烯丙胺盐酸盐)和聚(4-苯乙烯磺酸钠)的溶胶-凝胶介孔二氧化硅颗粒中。除了眼毒理学评估外,还对该制剂进行了体外和体内药物释放研究。

结果

热重分析显示,SG-Ket-LBL颗粒的载药效率为4.4%。体内安全性研究表明,结膜下注射后该制剂耐受性良好,房水药代动力学显示在6至8周的目标时间窗口内药物持续释放。

结论

研究结果表明,溶胶-凝胶介孔二氧化硅可作为结膜下给药的药物载体。测试的制剂SG-Ket-LBL可提供6至8周的治疗性酮咯酸,可用于单次结膜下注射以替代白内障手术后的非甾体抗炎眼药水。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b2eb/7644604/2a0491c25752/nihms-1615583-f0001.jpg

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