Bendas Ehab R, Abdelbary Aly A
Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Kasr El-Ainy Street, Cairo 11562, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Kasr El-Ainy Street, Cairo 11562, Egypt.
Int J Pharm. 2014 Jul 1;468(1-2):97-104. doi: 10.1016/j.ijpharm.2014.04.030. Epub 2014 Apr 16.
Recently, great attention has been paid to nanocapsules. The interest of these structures is due to their promising applications as drug delivery systems. The objective of this study was to develop novel enteric coating technique based on instantaneous encapsulation of the acid-labile drug, omeprazole in innovative enteric nanocapsules. Omeprazole enteric nanocapsules were formulated by varying the type and amount of the enteric polymer. The particle size (PS), polydispersity index (PDI), zeta potential (ZP) and encapsulation efficiency (EE) values of the prepared enteric nanocapsules were determined. A full 2(1)×3(1) factorial design was used for planning and analysis of the experimental trials to select the optimized formulation. The highest desirability value was 0.7463 for formula E3 (containing 200mg hydroxypropyl methylcellulose phthalate (HPMCP)). The stability of omeprazole was reflected by the absence of the exothermal peak when the drug was encapsulated as detected by differential scanning calorimetry (DSC) thermograms. In vitro drug release study confirmed the USP specifications required to meet the key formulation characteristics of gastro-resistance. In vivo pharmacological assessment showed that the optimized nanocapsules were able to protect rat stomach against ulcer formation compared to the aqueous suspension of the drug which showed less significant protection.
最近，纳米胶囊受到了极大的关注。这些结构之所以令人感兴趣，是因为它们作为药物递送系统具有广阔的应用前景。本研究的目的是基于将酸不稳定药物奥美拉唑瞬间包封在创新型肠溶纳米胶囊中，开发一种新型肠溶包衣技术。通过改变肠溶聚合物的类型和用量来制备奥美拉唑肠溶纳米胶囊。测定了所制备的肠溶纳米胶囊的粒径（PS）、多分散指数（PDI）、zeta电位（ZP）和包封率（EE）值。采用全2(1)×3(1)析因设计对实验进行规划和分析，以选择优化的配方。配方E3（含有200mg邻苯二甲酸羟丙基甲基纤维素（HPMCP））的最高可取性值为0.7463。差示扫描量热法（DSC）热谱图检测显示，当药物被包封时，没有放热峰，这反映了奥美拉唑的稳定性。体外药物释放研究证实了符合胃抗性关键配方特征所需的美国药典规范。体内药理学评估表明，与药物水悬浮液相比，优化后的纳米胶囊能够保护大鼠胃免受溃疡形成，而药物水悬浮液的保护作用不太显著。
