Polyamidoamine dendrimer hydrogel for enhanced delivery of antiglaucoma drugs
Polyamidoamine dendrimer hydrogel for enhanced delivery of antiglaucoma drugs
复制标题
DOI：
10.1016/j.nano.2011.08.018
复制
发表时间：
2012-07-01
影响因子：
5.4
通讯作者：
Yang, Hu
中科院分区：
文献类型：
--
作者：
Holden, Christopher A.;Tyagi, Puneet;Yang, Hu
树枝状聚合物水凝胶（DH）由紫外光固化的聚酰胺-胺树枝状聚合物G3.0与三个聚乙二醇（PEG，12，000 Da）-丙烯酸酯链（8.1%w/v）在pH 7.4的磷酸盐缓冲盐水（PBS）中制成，研究了两种抗青光眼药物溴莫尼定（0.1%w/v）和马来酸噻吗洛尔（0.5%w/v）的递送。发现DH对粘蛋白颗粒具有粘膜粘附性，并且对人角膜上皮细胞无毒。DH使溴莫尼定的PBS溶解度增加77.6%，并使两种药物的体外释放持续56-72小时。与滴眼剂制剂（PBS-药物溶液）相比，DH显著提高了人角膜上皮细胞的摄取，并显著增加了两种药物的牛角膜转运。DH使牛角膜上皮、基质和内皮的马来酸噻吗洛尔摄取增加0.4- 4.6倍。本工作表明，DH可以在多个方面增强抗青光眼药物的递送，代表了眼部药物递送的新平台。(C)2011 Elsevier Inc. All rights reserved.
Dendrimer hydrogel (DH), made from ultraviolet-cured polyamidoamine dendrimer G3.0 tethered with three polyethylene glycol (PEG, 12,000 Da)-acrylate chains (8.1% w/v) in pH 7.4 phosphate buffered saline (PBS), was studied for the delivery of brimonidine (0.1% w/v) and timolol maleate (0.5% w/v), two antiglaucoma drugs. DH was found to be mucoadhesive to mucin particles and nontoxic to human corneal epithelial cells. DH increased the PBS solubility of brimonidine by 77.6% and sustained the in vitro release of both drugs over 56-72 hours. As compared to eye drop formulations (PBS-drug solutions), DH brought about substantially higher human corneal epithelial cells uptake and significantly increased bovine corneal transport for both drugs. DH increased timolol maleate uptake in bovine corneal epithelium, stroma, and endothelium by 0.4- to 4.6-fold. This work demonstrated that DH can enhance the delivery of antiglaucoma drugs in multiple aspects and represents a novel platform for ocular drug delivery. (C) 2011 Elsevier Inc. All rights reserved.