Jain S K, Chourasia M K, Masuriha R, Soni V, Jain A, Jain Nitin K, Gupta Y
Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar, India.
Drug Deliv. 2005 Jul-Aug;12(4):207-15. doi: 10.1080/10717540590952591.
Topical application of the drugs at the pathological sites offer potential advantages of delivering the drug directly to the site of action and thus producing high tissue concentrations of the drug. The solid lipid nanoparticles (SLN) bearing flurbiprofen were prepared by microemulsion method by dispersing o/w microemulsion in a cold aqueous surfactant medium under mechanical stirring. The SLN gel was prepared by adding SLN dispersion to polyacrylamide gel prepared by using polyacrylamide (0.5%), glycerol (10%), and water (69.5%). Shape and surface morphology was determined by scanning electron microscopy that revealed fairly spherical shape of the formulation. Percent drug entrapment was higher in SLN dispersion in comparison to SLN gel formulations. In vitro drug release, determined using cellophane membrane, showed that SLN dispersion exhibited higher drug release compared with SLN gel formulations. Both the SLN dispersion and SLN-gel formulation possessed a sustained drug release over a 24-hr period, but this sustained effect was more pronounced with SLN-gel formulations. The percent inhibition of edema after 8 hr was 55.51 +/- 0.26% in case of SLN-T4-gel, whereas flurbiprofen and SLN-T4 dispersion exhibited 28.81 +/- 0.46 and 31.89 +/- 0.82 inhibition of edema. The SLN-T4-gel not only decreased the inflammation to larger magnitude, but also sustained its effect.
在病理部位局部应用药物具有将药物直接输送到作用部位的潜在优势,从而使药物在组织中达到高浓度。通过微乳液法,在机械搅拌下将油包水型微乳液分散在冷的水性表面活性剂介质中,制备了载有氟比洛芬的固体脂质纳米粒(SLN)。通过将SLN分散体添加到由聚丙烯酰胺(0.5%)、甘油(10%)和水(69.5%)制备的聚丙烯酰胺凝胶中,制备了SLN凝胶。通过扫描电子显微镜测定形状和表面形态,结果显示制剂呈相当规则的球形。与SLN凝胶制剂相比,SLN分散体中的药物包封率更高。使用玻璃纸膜测定的体外药物释放表明,与SLN凝胶制剂相比,SLN分散体表现出更高的药物释放。SLN分散体和SLN凝胶制剂在24小时内均具有持续的药物释放,但这种持续作用在SLN凝胶制剂中更为明显。在SLN - T4 - 凝胶的情况下,8小时后水肿的抑制率为55.51±0.26%,而氟比洛芬和SLN - T4分散体对水肿的抑制率分别为28.81±0.46和31.89±0.82。SLN - T4 - 凝胶不仅能更大程度地减轻炎症,还能持续发挥其作用。