Doijad R C, Manvi F V, Godhwani D M, Joseph R, Deshmukh N V
Department of Pharmaceutics, K. L. E. S's College of Pharmacy, JNMC Campus, Nehru Nagar, Belguam-590 010, India.
Indian J Pharm Sci. 2008 Mar-Apr;70(2):203-7. doi: 10.4103/0250-474X.41456.
The present study is aimed at the overall improvement in the efficacy, reduced toxicity and enhancement of therapeutic index of cisplatin. Solid lipid nanoparticulate delivery system of cisplatin has been developed by microemulsification method by using stearic acid, soy lecithin 95% and sodium glycolate. The formulations were then characterized with respect to size and its surface morphology, zeta potential, entrapment efficiency, in vitro drug release profile, in vivo drug targeting studies and its stability under specific conditions. The formulated solid lipid nanoparticles were oval with a diameter ranging from 250 nm to 500 nm. The lowest entrapment efficiency was found to be 47.59% and highest was found to be 74.53%. The zeta potential was in the range of -9.8 to -11.2 mv. In vitro release study was analyzed using various mathematical models. Highest cumulative percent drug release was observed with F-1 (97.22 %) and lowest with F-4 (78.43%) in 16 h. The in vivo result of formulated solid lipid nanoparticles of cisplatin reveals that the drug is preferentially targeting to liver followed by brain and lungs.
本研究旨在全面提高顺铂的疗效、降低毒性并提高治疗指数。通过微乳化法，使用硬脂酸、95%大豆卵磷脂和乙醇酸钠开发了顺铂的固体脂质纳米颗粒递送系统。然后对制剂进行了粒径及其表面形态、zeta电位、包封率、体外药物释放曲线、体内药物靶向研究以及在特定条件下的稳定性等方面的表征。所制备的固体脂质纳米颗粒呈椭圆形，直径范围为250nm至500nm。最低包封率为47.59%，最高为74.53%。zeta电位在-9.8至-11.2mv范围内。使用各种数学模型对体外释放研究进行了分析。在16小时内，F-1的药物累积释放百分比最高（97.22%），F-4最低（78.43%）。顺铂固体脂质纳米颗粒的体内结果表明，药物优先靶向肝脏，其次是脑和肺。
