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用于控释药物递送的pH响应性聚(甲基丙烯酸2-羟乙酯-共-衣康酸)微凝胶的制备与评价

PREPARATION AND EVALUATION OF pH RESPONSIVE POLY(2-HYDROXYETHYL METHACRYLATE-CO-ITACONIC ACID) MICROGELS FOR CONTROLLED DRUG DELIVERY.

作者信息

Rashid Zermina, Ranjha Nazar Muhammad, Raza Hina, Razzaq Rabia, Mehmood Asif

出版信息

Acta Pol Pharm. 2016 Jul;73(4):1045-1055.

PMID:29648731
Abstract

In this study, a series of pH sensitive microgels (MGs) were prepared by modified free radical suspension polymerization of 2-hydroxyethyl methacrylate (HEMA) and itaconic acid (IA), using ethylene glycol dimethacrylate (EGDMA) as crosslinker. Equilibrium swelling technique was employed for esomeprazole magnesium trihydrate (EMT) loading. Prepared microgels were characterized through Fourier transforms infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), dynamic light scattering technique (DLS), scanning electron microscopy (SEM), equilibrium swelling and in vitro drug release kinetics. FTIR and TGA confirmed the formation of copolymeric p(HEMA-co-IA) network. SEM and DLS revealed smooth, round and uniformly distributed microspheres with particle size up to 10 μm. Developed microgels found to be pH responsive in nature. All the formulations (HIDI - HID5) followed Higuchi model with non-Fickian diffusion mechanism of drug release. It was concluded that p(HEMA-co-IA) microgels have potential to be used as drug carriers for site specific and controlled drug delivery.

摘要

在本研究中,以乙二醇二甲基丙烯酸酯(EGDMA)为交联剂,通过甲基丙烯酸羟乙酯(HEMA)和衣康酸(IA)的改性自由基悬浮聚合制备了一系列pH敏感微凝胶(MGs)。采用平衡溶胀技术负载三水合埃索美拉唑镁(EMT)。通过傅里叶变换红外光谱(FTIR)、热重分析(TGA)、动态光散射技术(DLS)、扫描电子显微镜(SEM)、平衡溶胀和体外药物释放动力学对制备的微凝胶进行了表征。FTIR和TGA证实了共聚p(HEMA-co-IA)网络的形成。SEM和DLS显示微球表面光滑、呈圆形且分布均匀,粒径可达10μm。所制备的微凝胶在性质上具有pH响应性。所有制剂(HIDI - HID5)均遵循Higuchi模型,药物释放机制为非Fickian扩散。得出结论,p(HEMA-co-IA)微凝胶有潜力用作药物载体,实现药物的定点和控释。

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