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喷雾干燥法制备的甲基丙烯酸酯微/纳米颗粒:初步体外/体内研究

Methacrylate micro/nano particles prepared by spray drying: a preliminary in vitro/in vivo study.

作者信息

Muñoz Ortega Begoña, Sallam Marwa Ahmed, Marín Boscá M Teresa

机构信息

a Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy , Granada University , Granada , Spain and.

b Department of Industrial Pharmacy, Faculty of Pharmacy , Alexandria University , Alexandria , Egypt.

出版信息

Drug Deliv. 2016 Sep;23(7):2439-2444. doi: 10.3109/10717544.2015.1008154. Epub 2015 Feb 26.

Abstract

Delivery systems controlling drug release only in the colon holds great promises since they improve utilization of drug and decrease the dosing times comparison with conventional forms. The aim of the present study was to prepare polymeric microparticles on the basis of Ciprofloxacin via oral route for the treatment of inflammatory bowel disease. Ciprofloxacin was selected because of its extensive coverage for intestinal flora, relatively favorable side-effect profile and preliminary data suggesting its efficacy in the treatment of active Crohn's Disease. Microparticles were prepared using different acrylic compounds, namely Eudragit® RL (PO) and RS (PO) and a mixture of both. Spray-drying was used as a preparation method of Ciprofloxacin/Eudragit® microparticles using a Mini Spray Dryer B-290 (Büchi, Postfach, Switzerland). In vitro dissolution studies were performed to choose the best formulation and selected microparticles were characterized by size and morphology by environmental scanning electron microscopy. Yield and encapsulation efficiency were calculated and in vivo/ex vivo experiments were investigated both of which suggest that selected microparticles can be used for colon targeting of drugs increasing residence time of the drug in the affected area.

摘要

仅在结肠控制药物释放的给药系统具有很大的前景,因为与传统剂型相比,它们提高了药物的利用率并减少了给药次数。本研究的目的是通过口服途径制备基于环丙沙星的聚合物微粒,用于治疗炎症性肠病。选择环丙沙星是因为其对肠道菌群的广泛覆盖、相对良好的副作用谱以及表明其在治疗活动性克罗恩病中疗效的初步数据。使用不同的丙烯酸化合物,即尤特奇® RL(PO)和RS(PO)以及两者的混合物制备微粒。使用Mini Spray Dryer B - 290(瑞士布赫公司,邮政信箱)通过喷雾干燥法制备环丙沙星/尤特奇®微粒。进行体外溶出研究以选择最佳配方,并通过环境扫描电子显微镜对选定的微粒进行尺寸和形态表征。计算产率和包封效率,并研究体内/体外实验,两者均表明选定的微粒可用于药物的结肠靶向,增加药物在受影响区域的停留时间。

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