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采用微波辐射接枝共聚反应设计、开发并验证了基于瓜尔胶的 pH 敏感药物传递载体。

Design, development and validation of guar gum based pH sensitive drug delivery carrier via graft copolymerization reaction using microwave irradiations.

机构信息

Department of Chemistry, Birla Institute of Technology, Mesra, Ranchi, Jharkhand 835215, India.

Department of Chemistry, Birla Institute of Technology, Mesra, Ranchi, Jharkhand 835215, India.

出版信息

Int J Biol Macromol. 2019 Oct 1;138:278-291. doi: 10.1016/j.ijbiomac.2019.07.063. Epub 2019 Jul 13.

DOI:10.1016/j.ijbiomac.2019.07.063
PMID:31310787
Abstract

A natural polysaccharide exudate guar gum was modified via graft copolymerization reaction aided by microwave irradiation. The graft copolymerization was carried out by using 2-hydroxyl ethyl methacrylate (PHEMA) as monomer and ceric ammonium nitrate (CAN) as a free radical initiator under microwave irradiation. Different grades of graft copolymers of (GG-g-P(HEMA)) were designed by varying the initiator and monomer concentrations and the best grade was developed with maximum percentage of grafting. The validation of synthesis was done by different characterization techniques such as C NMR, FTIR, SEM, CHNSO and TGA. These grades were applied as pH sensitive drug delivery carrier with pH variations in simulation with environment of gastrointestinal tract. The swelling study of GG-g-P(HEMA) based tablets was recorded as a function of varied pH and temperature to suit its application in GI tract. The equilibrium swelling percentage was found to be low at pH 1.2 whereas it was high at alkaline pH 7.4 condition. This swelling behavior makes this material quite suitable to be used as drug delivery carrier. The release mechanism of drug 5 - amino salicylic acid (5-ASA) was studied by different mathematical kinetics models. 5-ASA is a therapeutic drug to cure mild to moderate inflammatory bowel disease.

摘要

一种天然多糖渗出物瓜尔胶通过微波辐射辅助接枝共聚反应进行了修饰。接枝共聚反应是在微波辐射下,以 2-羟乙基甲基丙烯酸酯(PHEMA)为单体,硝酸铈铵(CAN)为自由基引发剂进行的。通过改变引发剂和单体浓度设计了不同等级的(GG-g-P(HEMA))接枝共聚物,最佳等级的接枝率最高。通过 C NMR、FTIR、SEM、CHNSO 和 TGA 等不同的表征技术验证了合成。这些等级被用作 pH 敏感的药物输送载体,模拟胃肠道环境中的 pH 变化。记录了基于 GG-g-P(HEMA)的片剂在不同 pH 和温度下的溶胀研究,以适应其在胃肠道中的应用。在 pH 1.2 时平衡溶胀率较低,而在碱性 pH 7.4 条件下较高。这种溶胀行为使这种材料非常适合用作药物输送载体。通过不同的数学动力学模型研究了 5-氨基水杨酸(5-ASA)药物的释放机制。5-ASA 是一种治疗轻度至中度炎症性肠病的治疗药物。

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