Dimitrijevic D, Lamandin C, Uchegbu I F, Shaw A J, Florence A T
Centre for Drug Delivery Research, School of Pharmacy, University of London, UK.
J Pharm Pharmacol. 1997 Jun;49(6):611-6. doi: 10.1111/j.2042-7158.1997.tb06854.x.
Measurements of transepithelial electrical resistance (TEER), the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) test and monitoring of poly(ethylene glycol) (PEG) transport have been used to study the effects of the non-ionic surfactants Solulan C24 and Solulan 16, either free in solution or as an integral part of niosome bi-layers, on intestinal epithelial cells from man (Caco-2 cell monolayers). The effects on epithelial integrity and on the transport of the hydrophilic drug metformin depend on the concentration of the surfactants. At concentrations above 1% the effect on TEER of the surfactant in niosomal form and free in solution were equivalent whereas cell viability was preserved to a higher concentration of Solulans when the Solulans were present in the niosomal form. It was concluded that the toxic effect of niosomes arises from free surfactant present in the niosome suspension.
已采用跨上皮电阻(TEER)测量、MTT(3-(4,5-二甲基噻唑-2-基)-2,5-二苯基-2H-溴化四唑)试验以及聚乙二醇(PEG)转运监测,来研究非离子表面活性剂Solulan C24和Solulan 16(以游离于溶液中或作为脂质体双层的组成部分的形式)对人肠上皮细胞(Caco-2细胞单层)的影响。对上皮完整性和亲水性药物二甲双胍转运的影响取决于表面活性剂的浓度。浓度高于1%时,脂质体形式和游离于溶液中的表面活性剂对TEER的影响相当,而当Solulan以脂质体形式存在时,细胞活力在更高的Solulan浓度下仍能得以保持。得出的结论是,脂质体的毒性作用源自脂质体悬浮液中存在的游离表面活性剂。