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Development of Resistant Starch Film Coated Microparticles for an Oral Colon‐Specific Drug Delivery
Starch ( IF 2.6 ) Pub Date : 2020-05-04 , DOI: 10.1002/star.201900262
Anum Khan 1 , Amna Bibi 1 , Huma Ali 1 , Asim ur Rehman 2 , Maimoona Qindeel 2 , Muhammad Irfan 1 , Aamer Ali Shah 1 , Malik Badshah 1 , Fariha Hasan 1 , Samiullah Khan 1
Affiliation  

In this study, novel enzymatically modified resistant starch type III (EM‐RSIII) derived drug loaded microspheres are developed for oral colon‐specific delivery of ciprofloxacin HCl, used as a model drug. EM‐RS III is enzymatically prepared using starch hydrolyzing enzymes amylase and pullulanase. The prebiotic effect of EM‐RSIII is successfully scrutinized for promoting the growth of probiotic bacteria, for example, Lactobacillus reuteri. Drug‐loaded microspheres are synthesized from the EM‐RSIII through a single emulsion evaporation method. The pH‐sensitive drug‐loaded microspheres are characterized through scanning electron microscopy, X‐ray diffraction, and Fourier‐transform infrared spectroscopy. Release studies confirm the stability of drug‐loaded microspheres at acidic pH while sustained release is observed at pH 7.8 demonstrating a site‐specific delivery of drug to the colon. The in vitro release mechanism of drug is evaluated using various kinetic models. The study also reveals that EM‐RSIII‐derived microspheres are biodegradable and are degraded by the natural microflora of the colon, which is indicated by stimulating growth of probiotic bacteria. The microspheres are exploited as drug carriers for the colon‐specific release of ciprofloxacin HCl, and its encapsulation is further confirmed from the antibacterial activity.

中文翻译:

抗性淀粉薄膜包衣微粒用于口服结肠特定药物的开发

在这项研究中,开发了新型的经酶修饰的抗药性III型淀粉(EM-RSIII)衍生的微球,用于口服环丙沙星盐酸盐的结肠特异性递送,用作模型药物。EM‐RS III使用淀粉水解酶淀粉酶和支链淀粉酶进行酶促制备。已成功检查了EM‐RSIII的益生元作用以促进益生菌例如罗伊氏乳杆菌的生长。载有药物的微球是通过单乳液蒸发法由EM-RSIII合成的。pH敏感的载药微球通过扫描电子显微镜,X射线衍射和傅立叶变换红外光谱进行表征。释放研究证实了载药微球在酸性pH下的稳定性,而在pH 7.8观察到了缓释,表明了药物向结肠的定点递送。使用各种动力学模型评估药物的体外释放机理。该研究还揭示了EM-RSIII衍生的微球可生物降解,并被结肠的天然菌群降解,这可通过刺激益生菌的生长来表明。微球被用作药物载体,用于盐酸环丙沙​​星在结肠中的释放,
更新日期:2020-05-04
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