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疏水性和亲水性添加剂对马来酸噻吗洛尔从聚己内酯基水凝胶的溶胶-凝胶转变及释放行为的影响

Effect of hydrophobic and hydrophilic additives on sol-gel transition and release behavior of timolol maleate from polycaprolactone-based hydrogel.

作者信息

Mishra Gyan P, Tamboli Viral, Mitra Ashim K

机构信息

Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 2464 Charlotte Street, Kansas City, MO 64108-2718, USA.

出版信息

Colloid Polym Sci. 2011 Sep;289(14):1553-1562. doi: 10.1007/s00396-011-2476-y.

Abstract

The objective of this work was to delineate the effect of hydrophilic and hydrophobic polymeric additives on sol-gel transition and release profile of timolol maleate (TM) from poly (ethylene glycol)-poly (ε-caprolactone)- poly (ethylene glycol) (PEG-PCL-PEG)-based thermosensitive hydrogel. Polycaprolactone (hydrophobic additive) and polyvinyl alcohol (PVA) (hydrophilic additive) reduced critical gel concentration of PEG-PCL-PEG triblock polymer. The effect of PCL on sol-gel transition was more pronounced than PVA. However, with PCL no statistically significant difference in release profile was observed. The effect of PVA on release profile was more pronounced, which reduced the cumulative percentage release of TM from 86.4±0.8% to 73.7±1.8% over 316 h. Moreover, cytotoxicity of the hydrogel was also investigated utilizing rabbit primary corneal epithelial culture cells. No significant cytotoxicity of hydrogel alone or in presence of additives was observed. So, polymeric additive strategy serves as a valuable tool for optimizing TM release kinetics from PEG-PCL-PEG hydrogel matrix.

摘要

这项工作的目的是描述亲水性和疏水性聚合物添加剂对马来酸噻吗洛尔(TM)从聚(乙二醇)-聚(ε-己内酯)-聚(乙二醇)(PEG-PCL-PEG)基热敏水凝胶的溶胶-凝胶转变和释放曲线的影响。聚己内酯(疏水性添加剂)和聚乙烯醇(PVA)(亲水性添加剂)降低了PEG-PCL-PEG三嵌段聚合物的临界凝胶浓度。PCL对溶胶-凝胶转变的影响比PVA更明显。然而,对于PCL,在释放曲线上未观察到统计学上的显著差异。PVA对释放曲线的影响更明显,在316小时内将TM的累积释放百分比从86.4±0.8%降低到73.7±1.8%。此外,还利用兔原代角膜上皮培养细胞研究了水凝胶的细胞毒性。未观察到单独的水凝胶或在存在添加剂的情况下有明显的细胞毒性。因此,聚合物添加剂策略是优化PEG-PCL-PEG水凝胶基质中TM释放动力学的有价值工具。

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