Preparation of controlled release ophthalmic drops, for glaucoma therapy using thermosensitive poly-N-isopropylacrylamide
Preparation of controlled release ophthalmic drops, for glaucoma therapy using thermosensitive poly-N-isopropylacrylamide
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DOI：
10.1016/s0142-9612(01)00127-2
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发表时间：
2002-01-01
期刊：
影响因子：
14
通讯作者：
Yang, IK
中科院分区：
文献类型：
--
作者：
Hsiue, GH;Hsu, SH;Yang, IK
本研究基于聚N-异丙基丙烯酰胺（PNIPAAm）的温敏性，开发了用于青光眼治疗的眼用控释剂。已知PNIPAAm的澄清溶液在温度从室温升高至约32 ℃时经历相转变。在室温下，药物包埋在缠结的聚合物链中或包封在交联的聚合物水凝胶内，并在局部施用后逐渐释放（即，在更高的温度下）。制备了含有肾上腺素的线性PNIPAAm和交联PNIAAm纳米粒。体外释药及细胞毒性试验。将基于线性PNIPAAm或线性PNIPAAm和交联PNIPAAm纳米颗粒的混合物的眼用制剂施用于兔，并评价眼内压（IOP）降低效果。基于线性PNIPAAm的制剂的降低的压力响应持续时间比常规滴眼剂长6倍。此外，对于基于线性PNIPAAm和交联纳米颗粒的混合物的制剂，降压效果持续了8倍长。这些结果表明，使用热敏聚合物溶液或水凝胶是潜在的控制释放抗青光眼眼科药物。(C)2001爱思唯尔科技有限公司版权所有。
In this study, controlled release ophthalmic agents for glaucoma therapy were developed based on the thermosensitivity of poly-N-isopropylacrylamide (PNIPAAm). The clear solution of PNIPAAm was known to undergo phase transition when the temperature was raised from the room temperature to about 32 degreesC. The drug was entrapped in the tangled polymer chains or encapsulated within the crosslinked polymer hydrogel at room temperature, and released progressively after topical application (i.e., at a higher temperature). Linear PNIPAAm and crosslinked PNIAAm nanoparticles containing epinephrine were prepared. The drug release rate and cytotoxicity were investigated in vitro. Ophthalmic formulations based on either linear PNIPAAm or the mixture of linear PNIPAAm and crosslinked PNIPAAm nanoparticles were administered to rabbits and the intraocular pressure (IOP)lowering effect was evaluated. The decreased pressure response of the formulation based on linear PNIPAAm lasted six-fold longer than that of the conventional eye drop. Furthermore, for formulation based on the mixture of linear PNIPAAm and crosslinked nanoparticles, the pressure-lowering effect lasted eight times longer. These results suggest the use of thermosensitive polymer solutions or hydrogels is potential in controlled release antiglaucoma ophthalmic drugs. (C) 2001 Elsevier Science Ltd. All rights reserved.