Department of Environmental Biotechnology, Bharathidasan University, Tiruchirappalli, Tamil Nadu, India.
IET Nanobiotechnol. 2021 Feb;15(1):90-99. doi: 10.1049/nbt2.12010. Epub 2021 Feb 2.
This investigation is to find a prolonged or delayed drug release system, exclusively for the treatment of hepatitis-B to reduce the side effects, which arise when conventional solid dose forms are administered. To pursue this goal, lamivudine-loaded Eudragit-coated pectin microspheres have been formulated employing water/oil (W/O) emulsion evaporation strategy. The formulation was optimised using a 3 factorial design. A drug to polymer ratio of 1:2, the surfactant of 1 ml, the volume of 50 ml of processing medium with a stirring speed of 2500 rpm were found to be the optimal parameters to obtain the lamivudine-loaded Eudragit-coated pectin microspheres formulation with a high drug entrapment efficiency of 89.44% ± 1.44%. The in vitro release kinetics of lamivudine was a suitable fit to the Higuchi model, indicating a diffusion-controlled release with anomalous transport. The obtained microspheres were then subjected to different characterisation studies, including scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). The results of this study clearly indicate that Eudragit-coated pectin microspheres could be the promising controlled release carriers for colon-specific delivery of lamivudine in the presence of rat cecal content.
本研究旨在开发一种用于治疗乙型肝炎的缓释或迟释药物系统，以减少常规固体制剂给药时产生的副作用。为了实现这一目标，采用水/油（W/O）乳液蒸发策略，制备了载拉米夫定的 Eudragit 包被果胶微球。采用 3 因素设计对制剂进行优化。结果发现，药物与聚合物的比例为 1:2、表面活性剂为 1ml、加工介质的体积为 50ml、搅拌速度为 2500rpm 时，可获得载拉米夫定的 Eudragit 包被果胶微球制剂，药物包封率高达 89.44%±1.44%。拉米夫定的体外释放动力学符合 Higuchi 模型，表明其释放为扩散控制，伴有异常传递。然后对所得微球进行了不同的特性研究，包括扫描电子显微镜（SEM）、傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和 X 射线衍射（XRD）。研究结果清楚地表明，在大鼠盲肠内容物存在的情况下，Eudragit 包被果胶微球可作为拉米夫定结肠定位释放的有前途的控释载体。
