Ahmad Mohammad Zaki, Akhter Sohail, Anwar Mohammed, Kumar Atul, Rahman Mahfoozur, Talasaz Azita Hajhossein, Ahmad Farhan Jalees
Department of Pharmaceutics, Dreamz College of Pharmacy , Khilra-Meramesit, Sundernagar, Mandi, Himachal Pradesh , India.
Drug Dev Ind Pharm. 2013 Dec;39(12):1936-43. doi: 10.3109/03639045.2012.719906. Epub 2012 Sep 27.
The purpose of this investigation was to evaluate the colon-targeted Irinotecan Hydrochloride (ITC-HCl) loaded microspheres by pharmacokinetic and biochemical studies. The microspheres were prepared by double emulsion solvent evaporation method with natural polymer Assam Bora rice starch. The microspheres were characterized for their micromeritics properties, incorporation efficiency, in vitro and in vivo drug release studies. The release study confirmed the insignificant release of ITC-HCl in physiological condition of stomach and small intestine and major drug release in the caecal content. In vivo release study of the optimized microsphere was compared with immediate release (IR) ITC-HCl. ITC-HCl was distributed predominantly in the upper GI tract from the IR, whereas ITC-HCl was distributed primarily to the lower part of GI tract from the microspheres formulation. Enhanced levels of liver enzymes were found in animals given IR ITC-HCl as well as augmented levels of serum albumin, creatinine, leucocytopenia and thrombocytopenia was also observed. In summary, Assam Bora rice starch microspheres exhibit slow and extended release of ITC-HCl over longer periods of time with reduced systemic side-effects.
本研究的目的是通过药代动力学和生化研究评估结肠靶向载盐酸伊立替康（ITC-HCl）微球。采用双乳液溶剂蒸发法，以天然聚合物阿萨姆博拉大米淀粉制备微球。对微球的微观性质、包封率、体外和体内药物释放研究进行了表征。释放研究证实，ITC-HCl在胃和小肠的生理条件下释放量极少，主要在盲肠内容物中释放药物。将优化后的微球的体内释放研究与速释（IR）ITC-HCl进行了比较。IR ITC-HCl使ITC-HCl主要分布在上消化道，而微球制剂使ITC-HCl主要分布在胃肠道下部。给予IR ITC-HCl的动物肝脏酶水平升高，同时还观察到血清白蛋白水平升高、肌酐升高、白细胞减少和血小板减少。总之，阿萨姆博拉大米淀粉微球在较长时间内呈现出ITC-HCl的缓慢和持续释放，且全身副作用减少。
