School of Pharmacy, Department of Pharmaceutics, University of Oslo, P.O. Box 1068, Blindern, N-0316 Oslo, Norway.
Int J Pharm. 2012 Oct 15;436(1-2):454-62. doi: 10.1016/j.ijpharm.2012.07.018. Epub 2012 Jul 20.
Ethyl(hydroxyethyl) cellulose (EHEC) is known to form hydrogels in water at elevated temperatures in the presence of an ionic surfactant. In this paper, the potential use of arginine-based surfactants is explored considering the production of a low toxicity thermoresponsive hydrogel for pharmaceutical and biomedical applications. The interactions between EHEC and the monomeric surfactant N(α)-lauroyl-L-arginine methyl ester (LAM) and two gemini surfactants N(α),N(ω)-bis(N(α)-acylarginine) α,ω-dialkyl amides were evaluated by Rheo-Small Angle Light Scattering measurements. The complex viscosity of the systems was dependent on surfactant concentration and temperature. Under specific conditions, soft gels of homogeneous structure were produced. The cloud point (CP) of the EHEC-LAM system varied significantly with surfactant concentration, while only moderate CP changes were found in the presence of the gemini surfactants. Finally, the effect of the surfactants on the viability of a human cell line was evaluated. Despite the lower toxicity of LAM, the superior gel forming efficiency of the gemini surfactants at lower concentrations revealed their advantageous suitability as components of a biocompatible thermoresponsive gel system.
羟乙基纤维素(EHEC)在存在离子型表面活性剂的情况下,于高温的水中形成水凝胶。在本文中,考虑到用于药物和生物医学应用的低毒性温敏水凝胶的生产,探索了使用基于精氨酸的表面活性剂的可能性。通过流变小角光散射测量评估了 EHEC 与单体表面活性剂 N(α)-月桂酰-L-精氨酸甲酯(LAM)和两种双子表面活性剂 N(α),N(ω)-双(N(α)-酰基精氨酸)α,ω-二烷基酰胺之间的相互作用。体系的复粘度取决于表面活性剂浓度和温度。在特定条件下,生成了具有均匀结构的软凝胶。EHEC-LAM 体系的浊点(CP)随表面活性剂浓度显著变化,而在存在双子表面活性剂时仅发现 CP 适度变化。最后,评估了表面活性剂对人细胞系活力的影响。尽管 LAM 的毒性较低,但双子表面活性剂在较低浓度下形成凝胶的效率更高,表明它们作为生物相容温敏凝胶体系的组成部分具有优势适用性。