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用于向眼后段进行接力给药的环糊精复合物@层状双氢氧化物多功能纳米复合眼药水。

Multifunctional nanocomposite eye drops of cyclodextrin complex@layered double hydroxides for relay drug delivery to the posterior segment of the eye.

作者信息

Xu Chen, Lu Jinhui, Zhou Li, Liang Jie, Fang Lei, Cao Feng

机构信息

Department of Pharmaceutical, School of Pharmacy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing, 210009, China; WuXi Clinical Development Services Co., Ltd, 666 Gaoxin Road, Wuhan, 430075, China.

Department of Pharmaceutical, School of Pharmacy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing, 210009, China.

出版信息

Carbohydr Polym. 2021 May 15;260:117800. doi: 10.1016/j.carbpol.2021.117800. Epub 2021 Feb 13.

Abstract

Topical drug delivery system to the posterior segment of the eye is facing many challenges, such as rapid drug elimination, low permeability, and low concentration at the targeted sites. To overcome these challenges, Multifunctional nanocomposite eye drops of dexamethasone-carboxymethyl-β-cyclodextrin@layered double hydroxides-glycylsarcosine (DEX-CM-β-CD@LDH-GS) were developed for relay drug delivery. Herein, our studies demonstrated that DEX-CM-β-CD@LDH-GS could penetrate through human conjunctival epithelial cells with an intact structure and exhibited integrity in the sclera of rabbits' eyes with in vivo fluorescence resonance energy transfer imaging. Consequently, tissue distribution indicated that DEX-CM-β-CD@LDH-GS nanocomposite eye drops could maintain the effective therapeutic concentration of DEX in choroid-retina within 3 h. As a relay drug delivery system, drug-CD@LDH nanocomposites offer an efficient strategy for drug delivery from ocular surface to the posterior segment.

摘要

眼部后段的局部给药系统面临着诸多挑战,如药物快速消除、低渗透性以及靶点部位的低浓度等问题。为克服这些挑战,研发了用于接力给药的地塞米松 - 羧甲基 -β-环糊精@层状双氢氧化物 - 甘氨酰肌氨酸(DEX - CM -β- CD@LDH - GS)多功能纳米复合眼药水。在此,我们的研究表明,DEX - CM -β- CD@LDH - GS能够完整地穿透人结膜上皮细胞,并通过体内荧光共振能量转移成像在兔眼巩膜中保持完整性。因此,组织分布表明DEX - CM -β- CD@LDH - GS纳米复合眼药水能够在3小时内维持脉络膜 - 视网膜中DEX的有效治疗浓度。作为一种接力给药系统,药物 - CD@LDH纳米复合材料为从眼表到眼后段的药物递送提供了一种有效的策略。

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