Sahoo S K, Sahoo S K, Behera A, Patil S V, Panda S K
Department of Pharmaceutics, University Department of Pharmaceutical Sciences, Utkal University, Bhubaneswar, Orissa, India.
Acta Pol Pharm. 2013 Jan-Feb;70(1):123-7.
5-Fluorouracil loaded calcium-zinc-gellan and calcium-zinc-gellan-ethyl cellulose microbeads were successfully prepared by simple ionotropic gelation and oil in water ionotropic gelation technique, respectively. Prepared microbeads were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy and evaluated for particle size, drug content, encapsulation efficiency, drug release and cell cytotoxicity study. Microbeads formed were spherical with rough surface. As concentration of gellan and ethyl cellulose has increased encapsulation efficiency, particle size and sustained drug release effect also increased. The release of 5-fluorouracil from microbeads has followed Hixson Crowell model suggesting the mechanism of drug release as dissolution controlled. Cytotoxicity analysis on HT-29 human colon cancer cell lines indicated that 5-FU loaded gellan gum/gellan in combination with ethyl cellulose microbeads leads to sustained releases of drug and thus delayed apoptosis over a long period of time. The formulation with drug:gellan:ethyl cellulose ratio 2.5:7.5:1 was found to be more effectual in terms of sustained drug release activity in addition to anti-cancer activity.
分别通过简单的离子凝胶法和水包油离子凝胶技术成功制备了负载5-氟尿嘧啶的钙-锌-结冷胶微珠和钙-锌-结冷胶-乙基纤维素微珠。通过扫描电子显微镜、傅里叶变换红外光谱对制备的微珠进行表征,并对其粒径、药物含量、包封率、药物释放和细胞毒性进行研究。形成的微珠呈球形,表面粗糙。随着结冷胶和乙基纤维素浓度的增加,包封率、粒径和药物缓释效果也增加。5-氟尿嘧啶从微珠中的释放遵循希克森-克劳威尔模型,表明药物释放机制为溶出控制。对HT-29人结肠癌细胞系的细胞毒性分析表明,负载5-氟尿嘧啶的结冷胶/结冷胶与乙基纤维素微珠组合导致药物持续释放,从而在很长一段时间内延迟细胞凋亡。发现药物:结冷胶:乙基纤维素比例为2.5:7.5:1的制剂除具有抗癌活性外,在药物持续释放活性方面更有效。