Department of Pharmaceutical Engineering, School of Chemical Engineering and Technology, Tianjin University, Education Ministry Key Laboratory of Systems Bioengineering, People's Republic of China.
AAPS PharmSciTech. 2012 Mar;13(1):276-83. doi: 10.1208/s12249-011-9746-3. Epub 2012 Jan 11.
Idebenone (IDB) is a synthetic antioxidant and analog of coenzyme Q10. The percutaneous permeation of IDB was investigated in guinea pig skin after application of different formulations. The enhancing effects of various formulations [nanostructured lipid carriers (NLCs), nanoemulsion (NE), or oil solution] on the permeation of IDB were evaluated using ex vivo guinea pig skins. Furthermore, stability of different formulations and in which chemical stability of IDB was determined during storage. Permeation experiments revealed that formulations varied in their ability to enhance the skin permeation of IDB. For NLC formulation, the cumulative amount of IDB in the epidermis, dermis, and acceptor medium of diffusion cells was approximately threefold more than NE or oil solution at the end of 24-h experiment. No significant difference between NE and oil solution was observed in the enhancement of penetration efficacy of IDB. Different formulations resulted in stability with different properties. NLC formulation revealed preferentially more stable than NE. The residual percentage of IDB loaded in NLCs, NE, and oil solution was 90.1%, 65.4%, and 51.3%, respectively, when stored at 40°C under 75% RH and 3,000 lx light conditions for 180 days. The results obtained here demonstrated that the abilities of NLCs to improve the chemical stability of IDB and enhance the skin permeation are much better than NE and oil solution. These suggest that NLCs containing IDB have significant potential use for skin care as an alternative topical formulation.
依地酸二钠(IDB)是一种合成抗氧化剂,也是辅酶 Q10 的类似物。本研究考察了不同制剂经皮给药后 IDB 在豚鼠皮肤中的渗透情况。采用离体豚鼠皮肤,评价了不同制剂(纳米结构脂质载体(NLC)、纳米乳(NE)或油溶液)对 IDB 渗透的促进作用。此外,还考察了不同制剂的稳定性,包括 IDB 在储存过程中的化学稳定性。渗透实验结果表明,不同制剂对 IDB 经皮渗透的促进作用存在差异。与 NE 或油溶液相比,NLC 制剂在 24 小时实验结束时,IDB 在表皮、真皮和扩散池接受介质中的累积量约增加了三倍。在提高 IDB 渗透功效方面,NE 和油溶液之间没有显著差异。不同制剂的稳定性存在差异。NLC 制剂比 NE 更稳定。当在 40°C、75%相对湿度和 3000 lx 光照条件下储存 180 天时,IDB 负载于 NLCs、NE 和油溶液中的残余百分比分别为 90.1%、65.4%和 51.3%。结果表明,NLCs 能够提高 IDB 的化学稳定性并增强皮肤渗透,其能力明显优于 NE 和油溶液。这表明,含 IDB 的 NLC 具有作为替代局部制剂用于皮肤护理的巨大潜力。