School of Pharmaceutical Sciences, IFTM University, Moradabad 244001, Uttar Pradesh, India.
Colloids Surf B Biointerfaces. 2013 Dec 1;112:483-91. doi: 10.1016/j.colsurfb.2013.07.054. Epub 2013 Aug 8.
Gellan gum (GG) microbeads containing tranexamic acid (TA), an anti-fibrinolytic drug were prepared by a classic sol-gel transition induced by ionic crosslinking technique using aluminum chloride (AlCl3) as cross-linking agent. The influence of different formulation variables on in vitro physico-chemical parameters and drug release studies were performed systematically. The microbeads were evaluated by scanning electron microscopy (SEM), Fourier transform infra-red (FTIR) spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and high performance liquid chromatographic (HPLC) analysis. Particle size and swelling behavior of microbeads were also investigated. Microbeads showed improved drug encapsulation efficiency along with enhanced drug release. The in vivo studies exhibited sustained drug release in rabbits over a prolonged period after oral administration of these newly developed TA loaded GG microbeads. Based on the results of in vitro and in vivo studies in experimental animal model it was concluded that these microbeads provided intestinal specific controlled release of TA.
以海藻酸钙(GG)微球为载体,采用离子交联技术,通过经典的溶胶-凝胶转变,制备载氨甲环酸(TA)的 GG 微球。使用三氯化铝(AlCl3)作为交联剂,系统研究了不同制剂变量对体外物理化学参数和药物释放的影响。通过扫描电子显微镜(SEM)、傅里叶变换红外(FTIR)光谱、X 射线衍射(XRD)、差示扫描量热法(DSC)和高效液相色谱(HPLC)分析对微球进行了评估。还研究了微球的粒径和溶胀行为。微球显示出改善的药物包封效率以及增强的药物释放。在兔体内研究中,这些新开发的 TA 负载 GG 微球经口服给药后,在较长时间内表现出持续的药物释放。基于实验动物模型的体外和体内研究结果,得出结论,这些微球提供了 TA 的肠道特异性控制释放。