Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Int J Pharm. 2020 Apr 30;580:119183. doi: 10.1016/j.ijpharm.2020.119183. Epub 2020 Feb 26.
Niosomes are novel carriers that show superior transdermal permeation enhancement but require the addition of charged stabilizers. In this study, niosomes were prepared using Span 40, cholesterol, and sodium dodecyl sulfate (SDS) as stabilizers for transdermal delivery of salidroside. At concentrations of 0.05-0.40% (w/v), SDS significantly increased the zeta potential of the nanovesicles from -18.5 ± 3.2 to -157.0 ± 5.2 mV and improved the stability of the niosomal formulations. Niosomes prepared with a Span 40:cholesterol molar ratio of 4:3 and 0.1% SDS showed good stability and the highest transdermal drug delivery among all tested formulations, with 2.75-fold higher transdermal flux of 20.26 ± 1.05 μg/(cm·h) than that of aqueous salidroside solution. However, excess SDS increased the negative charge on the vesicle surface and hence repulsion with skin cells, leading to reduced drug entrapment efficiency and cellular uptake of niosomes. Although SDS in the niosomes dose-dependently increased the in vitro cytotoxicity of the formulation in skin cells, HaCaT and CCC-ESF-1 cell viability was ≥ 80% for formulations containing ≤0.1% SDS. No significant irritation was observed on rat skin with once-a-day topical application of the niosomal formulations for 7 consecutive days. Thus, SDS is a promising stabilizer for nanomedicines, including niosomes, for transdermal administration.
囊泡是一种新型载体，具有优异的经皮渗透增强作用，但需要添加带电稳定剂。在这项研究中，使用 Span 40、胆固醇和十二烷基硫酸钠 (SDS) 作为稳定剂，制备了用于透皮递送红景天苷的囊泡。在 0.05-0.40%（w/v）浓度下，SDS 显著增加了纳米囊泡的 ζ 电位从-18.5 ± 3.2 mV 增加到-157.0 ± 5.2 mV，并提高了囊泡制剂的稳定性。用 Span 40:胆固醇摩尔比为 4:3 和 0.1% SDS 制备的囊泡显示出良好的稳定性和所有测试制剂中最高的经皮药物递送，其 20.26 ± 1.05 μg/（cm·h）的透皮通量比水性红景天苷溶液高 2.75 倍。然而，过量的 SDS 增加了囊泡表面的负电荷，从而与皮肤细胞产生排斥，导致药物包封效率降低和囊泡的细胞摄取减少。尽管 SDS 使囊泡中的制剂在皮肤细胞中的体外细胞毒性呈剂量依赖性增加，但含有 ≤0.1% SDS 的制剂的 HaCaT 和 CCC-ESF-1 细胞活力≥80%。在连续 7 天每天一次局部应用囊泡制剂后，大鼠皮肤未见明显刺激。因此，SDS 是一种有前途的纳米药物稳定剂，包括用于经皮给药的囊泡。
