a School of Biological Science and Medical Engineering, State Key Laboratory of Bioelectronics , Southeast University , Nanjing , China.
b Collaborative Innovation Center of Suzhou Nano Science and Technology , Suzhou , China.
J Microencapsul. 2017 Sep;34(6):571-581. doi: 10.1080/02652048.2017.1367852. Epub 2017 Sep 3.
This study aimed at in vitro evaluation of α-lipoic acid-loaded lipid nanocapsules for topical delivery, which was prepared by hot high-pressure homogenisation. Stable particles could be formed and particle size was 148.54 ± 2.31 nm with polydispersity index below 0.15. Encapsulation efficiency and drug loading of α-lipoic acid were 95.23 ± 0.45% and 2.81 ± 0.37%. Antioxidant study showed α-lipoic acid could be protected by lipid nanocapsules without loss of antioxidant activity. Sustained release of α-lipoic acid from lipid nanocapsules was obtained and cumulative release was 62.18 ± 1.51%. In vitro percutaneous study showed the amount of α-lipoic acid distributed in skin was 1.7-fold than permeated. Cytotoxicity assay and antioxidant activity on L929 cells indicated this formulation had low cytotoxicity and ability of protecting cells from oxidative damage within specific concentration. These studies suggested α-lipoic acid-loaded lipid nanocapsules could be potential formulation for topical delivery.
本研究旨在通过高压均质法体外评价载硫辛酸的脂质纳米囊的经皮给药。可形成稳定的粒子，粒径为 148.54 ± 2.31nm，多分散指数低于 0.15。硫辛酸的包封效率和载药量分别为 95.23 ± 0.45%和 2.81 ± 0.37%。抗氧化研究表明，脂质纳米囊可保护硫辛酸而不损失其抗氧化活性。从脂质纳米囊得到硫辛酸的持续释放，累积释放率为 62.18 ± 1.51%。体外经皮研究表明，分布在皮肤中的硫辛酸量是渗透量的 1.7 倍。对 L929 细胞的细胞毒性试验和抗氧化活性表明，该制剂在特定浓度下具有低细胞毒性和保护细胞免受氧化损伤的能力。这些研究表明，载硫辛酸的脂质纳米囊可能是一种有潜力的经皮给药制剂。
