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Development of Smart Polymer Microparticles through Suspension Polymerization for Treatment of Schistosomiasis
Macromolecular Reaction Engineering ( IF 1.5 ) Pub Date : 2019-11-07 , DOI: 10.1002/mren.201900028
Thamiris Franckini Paiva 1 , Jéssica Bentes Alves 2 , Príamo Albuquerque Melo 1 , José Carlos Pinto 1
Affiliation  

Schistosomiasis is a parasitic disease that affects millions of people, especially low‐income people, and is considered a major public health problem in underdeveloped countries. The drug used most often for the treatment of the disease is praziquantel (PZQ), which has a strong and characteristic bitter taste that makes treatment of children inconvenient. For this reason, the present work investigates the development of smart pH‐sensitive polymer microparticles produced through suspension polymerizations to be used as vehicles for the controlled release of praziquantel in the body. The microparticles are produced through copolymerization of methyl methacrylate and the cationic comonomers diethylaminoethyl methacrylate or dimethylaminoethyl methacrylate. The obtained results indicate that microparticles with sizes in the range of 10–1100 µm can be formed successfully, allowing high PZQ encapsulation efficiencies (>80%). Zeta potential analyses and drug release assays confirm the pH‐sensitive responses of the cationic copolymers, leading to effective release of PZQ (around 80% in pH 1.2) in acidic media that simulate the organic fluids present in the stomach.

中文翻译:

悬浮聚合制备智能聚合物微粒治疗血吸虫病

血吸虫病是一种寄生虫病,影响到数百万人,尤其是低收入人群,在不发达国家被认为是主要的公共卫生问题。最常用于治疗该疾病的药物是吡喹酮(PZQ),其苦味浓郁且具有特征性,给儿童的治疗带来不便。因此,本工作研究了悬浮聚合生产的智能pH敏感聚合物微粒的发展,该微粒可用作控制吡喹酮在体内释放的载体。通过甲基丙烯酸甲酯和阳离子共聚单体甲基丙烯酸二乙基氨基乙基酯或甲基丙烯酸二甲基氨基乙基酯的共聚生产微粒。获得的结果表明,可以成功形成尺寸在10–1100 µm范围内的微粒,从而实现了较高的PZQ封装效率(> 80%)。Zeta电位分析和药物释放分析证实了阳离子共聚物的pH敏感响应,从而导致PZQ(在pH 1.2时约为80%)在模拟胃中存在的有机液体的酸性介质中有效释放。
更新日期:2019-11-07
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