Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Cairo-Assuit Agriculture Road, Minia, 61519, Egypt.
AAPS PharmSciTech. 2019 Jun 26;20(6):237. doi: 10.1208/s12249-019-1453-5.
Nanoparticles for colon-drug delivery were designed and evaluated to solve many discrepancy issues as insufficient drug amount at diseased regions, high adverse effects of released drugs, and unintentionally premature drug release to noninflamed gastrointestinal regions. Herein, the prepared budesonide-loaded Eudragit S 100/Capryol 90 nanocapsules for the treatment of inflammatory bowel disease. Nanocapsules were prepared efficiently by nanoprecipitation technique and composed mainly of the pH-sensitive Eudragit S 100 polymeric coat with a semisynthetic Capryol 90 oily core. Full 3 × 2 factorial design was applied to obtain optimized nanocapsules. Optimal nanocapsules showed mean particle size of 171 nm with lower polydispersity index indicating the production of monodispersed system and negative zeta-potential of - 37.6 mV. Optimized nanocapsules showed high encapsulation efficiency of 83.4% with lower initial rapid release of 10% for first 2 h and higher rapid cumulative release of 72% after 6 h. The therapeutic activity of the prepared budesonide-loaded nanocapsules was evaluated using a rat colitis model. Disease activity score, macroscopical examination, blood glucose level, and histopathological assessment showed marked improvements over that free drug suspension. Obtained results demonstrate that the budesonide-loaded Eudragit S 100 nanocapsules are an effective colon-targeting nanosystem for the treatment of inflammatory bowel disease. Capryol 90 was found to be a successful, and even preferred, alternative to benzyl benzoate, which is commonly employed as the oil core of such nanocapsules.
用于结肠递药的纳米粒子被设计和评估，以解决许多差异问题，如病变部位药物含量不足、释放药物的高不良反应、以及药物意外过早释放到非炎症胃肠道部位。本文制备了负载布地奈德的 Eudragit S 100/Capryol 90 纳米囊用于治疗炎症性肠病。纳米囊通过纳米沉淀技术高效制备，主要由 pH 敏感的 Eudragit S 100 聚合物包衣和半合成的 Capryol 90 油芯组成。应用完全 3×2 析因设计获得优化的纳米囊。优化的纳米囊的平均粒径为 171nm，较低的多分散指数表明其产生了单分散体系，并且具有-37.6mV 的负 zeta 电位。优化的纳米囊具有 83.4%的高包封效率，在前 2 小时内快速释放 10%，6 小时后快速累积释放 72%。通过大鼠结肠炎模型评估了所制备的负载布地奈德的纳米囊的治疗活性。疾病活动评分、宏观检查、血糖水平和组织病理学评估显示，与游离药物混悬剂相比，有显著改善。获得的结果表明，负载布地奈德的 Eudragit S 100 纳米囊是一种有效的结肠靶向纳米系统，用于治疗炎症性肠病。Capryol 90 被发现是苯甲醇苯甲酸酯的成功替代品，甚至是首选替代品，苯甲醇苯甲酸酯通常被用作此类纳米囊的油芯。
