Department of Chemistry, H. N. B. Garhwal University, Srinagar (Garhwal), Uttarakhand, India.
Curr Drug Deliv. 2012 May;9(3):305-14. doi: 10.2174/156720112800389070.
Biopharmaceutical properties together with potency contribute critically towards clinical efficacy of the drugs by influencing the dissolution and bioavailability. The aim of this study was to develop an amphiphilic phyto-phospholipid complex in order to enhance the delivery of poorly soluble rutin. The rutin-phospholipid complex (Ru-PLc) was prepared and investigated for various physico-chemical parameters like drug loading, infrared absorption (FTIR), differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), scanning electron microscopy (SEM), aqueous/ n-octanol solubility and dissolution study. The in vitro anti-oxidant activity was also studied. In the SEM, Ru-PLc was found fluffy and porous with rough surface morphology. FTIR, DSC and XRPD data confirmed the formation of phospholipid complex. The water/ noctanol solubility of rutin was improved from 2.88 to 45.71 μg/ ml and 68.17 to 245.18 μg/ ml, respectively in the complex. The improved dissolution was shown by the phospholipid complex at different pH buffers. The antioxidant activity indicated that, the bioactivity of rutin was maintained even after being complexed with the phospholipid. Based on the results, it can be concluded that the phospholipid complex may be considered as a promising drug delivery system for improving the overall absorption and bioavailability of the rutin molecule.
生物制药特性与效价一起通过影响药物的溶解和生物利用度，对药物的临床疗效起着至关重要的作用。本研究的目的是开发一种两亲性植物磷脂复合物，以提高难溶性芦丁的传递效率。制备了芦丁-磷脂复合物（Ru-PLc），并对其进行了各种物理化学参数的研究，如药物负载、红外吸收（FTIR）、差示扫描量热法（DSC）、X 射线粉末衍射法（XRPD）、扫描电子显微镜（SEM）、水/正辛醇溶解度和溶解研究。还研究了体外抗氧化活性。在 SEM 中，Ru-PLc 被发现具有蓬松多孔的粗糙表面形态。FTIR、DSC 和 XRPD 数据证实了磷脂复合物的形成。芦丁的水/正辛醇溶解度分别从 2.88μg/ml 和 68.17μg/ml 提高到 45.71μg/ml 和 245.18μg/ml。在不同的 pH 缓冲液中，磷脂复合物显示出了更好的溶解性能。抗氧化活性表明，即使芦丁与磷脂形成复合物，其生物活性也得以维持。基于这些结果，可以得出结论，磷脂复合物可以被认为是一种有前途的药物传递系统，以提高芦丁分子的整体吸收和生物利用度。
