Department of Pharmacology, Soniya Education Trust's College of Pharmacy, Sangolli Rayanna Nagar, Dharwad 580002, Karnataka, India.
J Microencapsul. 2013;30(4):356-68. doi: 10.3109/02652048.2012.735263. Epub 2012 Oct 18.
Pharmacokinetics, biodistribution and antitumour activity of 5-fluorouracil (5-FU)-loaded polyhydroxybutyrate (PHB) and cellulose acetate phthalate (CAP) blend microspheres were investigated in chemically induced colorectal cancer in albino male Wistar rats and compared with pristine 5-FU given as a suspension. The microspheres were characterised for particle size, encapsulation efficiency, in vitro release and in vitro cytotoxicity on human HT-29 colon cancer cell line. Spherical particles with a mean size of 44 ± 11 µm were obtained that showed sustained release of 5-FU. A high concentration of 5-FU was achieved in colonic tissues and significant reduction in tumour volume and multiplicity were observed in animals treated with 5-FU-loaded microspheres. The decreased levels of plasma albumin, creatinine, leucocytopenia and thrombocytopenia were observed in animals for 5-FU microspheres compared to the standard 5-FU formulation. The results suggest the extended release of 5-FU from the PHB-CAP blend microspheres in colonic region to enhance the antitumour efficacy.
聚羟基丁酸酯（PHB）和邻苯二甲酸醋酸纤维素（CAP）混合微球载 5-氟尿嘧啶（5-FU）的药代动力学、生物分布和抗肿瘤活性在白化雄性 Wistar 大鼠化学诱导的结直肠癌中进行了研究，并与作为混悬剂给予的原始 5-FU 进行了比较。对微球进行了粒径、包封效率、体外释放和对人 HT-29 结肠癌细胞系的体外细胞毒性进行了表征。获得了平均粒径为 44±11μm 的球形颗粒，其显示出 5-FU 的持续释放。在接受载有 5-FU 的微球治疗的动物中，结肠组织中达到了高浓度的 5-FU，并且观察到肿瘤体积和多发性显著减少。与标准 5-FU 制剂相比，在接受 5-FU 微球治疗的动物中观察到血浆白蛋白、肌酐、白细胞减少和血小板减少水平降低。结果表明，PHB-CAP 混合微球在结肠区域中释放 5-FU 时间延长，从而增强了抗肿瘤疗效。
