Wissing S A, Müller R H
Department of Pharmaceutics, Biopharmaceutics and Biotechnology, The Free University of Berlin, Kelchstrasse 31, D-12169 Berlin, Germany.
J Control Release. 2002 Jun 17;81(3):225-33. doi: 10.1016/s0168-3659(02)00056-1.
The aim of this study was the comparison of two different formulations (solid lipid nanoparticles (SLN) and conventional o/w emulsion) as carrier systems for the molecular sunscreen oxybenzone. The influence of the carrier on the rate of release was studied in vitro with a membrane-free model. The release rate could be decreased by up to 50% with the SLN formulation. Further in vitro measurements with static Franz diffusion cells were performed. In vivo, penetration of oxybenzone into stratum corneum on the forearm was investigated by the tape stripping method. It was shown that the rate of release is strongly dependent upon the formulation and could be decreased by 30-60% in SLN formulations. In all test models, oxybenzone was released and penetrated into human skin more quickly and to a greater extent from the emulsions. The rate of release also depends upon the total concentration of oxybenzone in the formulation. In vitro-in vivo correlations could be made qualitatively.
本研究的目的是比较两种不同的制剂（固体脂质纳米粒（SLN）和传统的水包油乳液）作为分子防晒剂二苯甲酰甲烷载体系统的情况。采用无膜模型在体外研究了载体对释放速率的影响。使用SLN制剂时，释放速率可降低多达50%。进一步使用静态弗兰兹扩散池进行了体外测量。在体内，通过胶带剥离法研究了二苯甲酰甲烷在前臂角质层中的渗透情况。结果表明，释放速率强烈依赖于制剂，SLN制剂的释放速率可降低30%-60%。在所有测试模型中，二苯甲酰甲烷从乳液中释放并更快、更大量地渗透到人体皮肤中。释放速率还取决于制剂中二苯甲酰甲烷的总浓度。可以进行定性的体外-体内相关性研究。
