Synthesis, characterization, properties of N-succinyl chitosan-g-poly (methacrylic acid) hydrogels and in vitro release of theophylline
Synthesis, characterization, properties of N-succinyl chitosan-g-poly (methacrylic acid) hydrogels and in vitro release of theophylline
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DOI：
10.1016/j.polymer.2016.03.045
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发表时间：
2016-06-01
期刊：
影响因子：
4.6
通讯作者：
Ramesh, K.
中科院分区：
文献类型：
--
作者：
Bashir, Shahid;Teo, Yin Yin;Ramesh, K.
近年来，生物相容性和刺激响应性高分子材料在口服给药系统中的应用引起了人们极大的兴趣。具有刺激敏感性和溶胀性的水凝胶作为一种很有前途的药物定位控释材料受到了人们的关注。在本研究中，独特的生物降解性，生物相容性，溶胀性，和pH响应性N-琥珀酰壳聚糖-g-聚（甲基丙烯酸）水凝胶制备通过自由基机制口服茶碱。该方法以过硫酸铵（APS）为引发剂，N，N '-亚甲基双丙烯酰胺（MBA）为交联剂。采用傅里叶变换红外光谱（FTIR）、X射线衍射（XRD）、差示扫描量热法（DSC）、场发射扫描电子显微镜（FESEM）和流变仪等对复合材料的物理性能进行了表征。结果清楚地证实了N-琥珀酰壳聚糖-g-聚（甲基丙烯酸）凝胶的成功形成。水凝胶的体外降解依赖于单体与交联浓度的比例。考察了单体浓度、引发剂浓度、交联剂浓度、pH值和盐离子强度对溶胀行为的影响。结果表明，这些参数的强烈影响，对溶胀性能。高浓度引发剂和低交联剂制备的水凝胶具有最大溶胀。溶胀动力学数据表明，溶胀行为符合非Fickian反常输运机理。此外，发现茶碱负载和包封率（EE %）分别为14.5-23.5%和58- 94%。然而，茶碱的体外释放曲线被发现依赖于pH、单体浓度、引发剂和交联剂。在模拟肠液（SIF）中的最大释放量为90%。药物释放数据与Ritger-Peppas模型拟合良好。此外，还考察了茶碱的化学活性，发现药物在体外释放后仍保持其化学活性。(C)2016爱思唯尔有限公司版权所有
Although there was great interest in the biocompatible and stimuli responsive polymeric materials in oral drug delivery systems in recent years. The stimuli sensitive and swellable hydrogels have got striking attention as promising materials for site specific controlled drug delivery. In the present study, unique biodegradable, biocompatible, swellable, and pH responsive N-succinyl chitosan-g-Poly (methacrylic acid) hydrogels were prepared through free radical mechanism for oral administration of theophylline. In this method, ammonium persulfate (APS) and N, N'-methylenebisacrylamide (MBA) were used as initiator and crosslinking agent, respectively. The physical properties characterization was performed by Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC), field emission scanning electron microscope (FESEM), and rheometer. The results clearly confirmed the successful formation of N-succinyl chitosan-g-Poly (methacrylic acid) gel. In vitro degradation of hydrogels was found dependent on the ratio of monomers to crosslinking concentration. The effect of concentration of monomers, initiator, and crosslinking agent, pH and ionic strength of salts on swelling behavior was investigated. The results revealed the strong influence of these parameters, on swelling properties. Hydrogel prepared with high concentration of initiator and low crosslinking agent showed maximum swelling. The swelling showed good fitting to second order rate equation and the swelling kinetics data demonstrated the swelling behavior followed non-Fickian anomalous transport mechanism. Furthermore, theophylline loading and encapsulation efficiency (EE %) were found to be 14.5-23.5% and 58-94%, respectively. However, the in vitro release profile of theophylline was found dependent on pH, concentration of monomers, initiator, and crosslinking agent. The maximum release was found to be 90% in simulated intestinal fluid (SIF). The drug release data showed good fitting to Ritger-Peppas model. Moreover, the chemical activity of theophylline was also investigated and found that the drug maintained its chemical activity after in vitro release. (C) 2016 Elsevier Ltd. All rights reserved.