Department of Pharmaceutical Sciences, H. N. B. Garhwal University, Srinagar Garhwal, India.
Acta Pharm. 2009 Sep;59(3):335-44. doi: 10.2478/v10007-009-0023-x.
Pharmacosomes are amphiphilic lipid vesicular systems that have shown their potential in improving the bioavailability of poorly water soluble as well as poorly lipophilic drugs. Diclofenac is a poorly water soluble drug and also causes gastrointestinal toxicity. To improve the water solublity of diclofenac, its pharmacosomes (phospholipid complex) have been prepared and evaluated for physicochemical analysis. Diclofenac was complexed with phosphatidylcholine (80%) in equimolar ratio, in the presence of dichloromethane, by the conventional solvent evaporation technique. Pharmacosomes thus prepared were evaluated for drug solubility, drug content, surface morphology (by scanning electron microscopy), phase transition behaviour (by differential scanning calorimetry), crystallinity (by X-ray powder diffraction) and in vitro dissolution. Pharmacosomes of diclofenac were found to be irregular or disc shaped with rough surfaces in SEM. Drug content was found to be 96.2 +/- 1.1%. DSC thermograms and XRPD data confirmed the formation of the phospholipid complex. Water solubility of the prepared complex was found to be 22.1 microg mL-1 as compared to 10.5 microg mL-1 of diclofenac. This improvement in water solubility in prepared pharmacosomes may result in improved dissolution and lower gastrointestinal toxicity. Pharmacosomes showed 87.8% while the free diclofenac acid showed a total of only 60.4% drug release at the end of 10 h of dissolution study.
脂质体是两亲性的脂质囊泡系统，已显示出在提高疏水性和疏脂性差的药物的生物利用度方面的潜力。双氯芬酸是一种疏水性差的药物，也会引起胃肠道毒性。为了提高双氯芬酸的水溶性，已制备并评估了其脂质体（磷脂复合物）的理化分析。在二氯甲烷存在下，以等摩尔比将双氯芬酸与磷脂酰胆碱（80％）络合，通过常规溶剂蒸发技术。对由此制备的脂质体进行了药物溶解度，药物含量，表面形态（通过扫描电子显微镜观察），相变行为（通过差示扫描量热法观察），结晶度（通过 X 射线粉末衍射观察）和体外溶解度的评估。通过扫描电子显微镜观察到双氯芬酸的脂质体呈不规则或盘状，表面粗糙。药物含量为 96.2±1.1％。DSC 图谱和 XRPD 数据证实了磷脂复合物的形成。所制备的复合物的水溶解度为 22.1μgmL-1，而双氯芬酸的水溶解度为 10.5μgmL-1。这种在制备的脂质体中提高的水溶性可能导致溶解度提高和胃肠道毒性降低。在 10 小时的溶解研究结束时，脂质体显示出 87.8％的释放，而游离双氯芬酸酸仅显示出总共 60.4％的药物释放。
