Müller R H, Radtke M, Wissing S A
PharmaSol GmbH, Blohmstrasse 66a, 12307, Berlin, Germany.
Adv Drug Deliv Rev. 2002 Nov 1;54 Suppl 1:S131-55. doi: 10.1016/s0169-409x(02)00118-7.
Solid lipid nanoparticles (SLN) were developed at the beginning of the 1990 s as an alternative carrier system to emulsions, liposomes and polymeric nanoparticles. The paper reviews advantages-also potential limitations-of SLN for the use in topical cosmetic and pharmaceutical formulations. Features discussed include stabilisation of incorporated compounds, controlled release, occlusivity, film formation on skin including in vivo effects on the skin. As a novel type of lipid nanoparticles with solid matrix, the nanostructured lipid carriers (NLC) are presented, the structural specialties described and improvements discussed, for example, increase in loading capacity, physical and chemical long-term stability, triggered release and potentially supersaturated topical formulations. For both SLN and NLC, the technologies to produce the final topical formulation are described, especially the production of highly concentrated lipid nanoparticle dispersions >30-80% lipid content. Production issues also include clinical batch production, large scale production and regulatory aspects (e. g. status of excipients or proof of physical stability).
固体脂质纳米粒(SLN)于20世纪90年代初被开发出来,作为乳液、脂质体和聚合物纳米粒的替代载体系统。本文综述了SLN用于局部化妆品和药物制剂的优势以及潜在局限性。讨论的特性包括包封化合物的稳定性、控释、封闭性、在皮肤上形成薄膜以及对皮肤的体内效应。作为一种具有固体基质的新型脂质纳米粒,本文介绍了纳米结构脂质载体(NLC),描述了其结构特点并讨论了改进之处,例如载药量增加、物理和化学长期稳定性、触发释放以及潜在的过饱和局部制剂。对于SLN和NLC,均描述了制备最终局部制剂的技术,特别是脂质含量>30 - 80%的高浓度脂质纳米粒分散体的制备。生产问题还包括临床批量生产、大规模生产和监管方面(例如辅料状态或物理稳定性证明)。