Cytotoxicity of solid lipid nanoparticles as a function of the lipid matrix and the surfactant
Cytotoxicity of solid lipid nanoparticles as a function of the lipid matrix and the surfactant
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DOI：
10.1023/a:1012043315093
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发表时间：
1997-04-01
影响因子：
3.7
通讯作者：
Mehnert, W
中科院分区：
文献类型：
--
作者：
Muller, RH;Ruhl, D;Mehnert, W
目的.评估固体脂质纳米粒（SLN）的体外细胞毒性，作为脂质基质（Dynasan 114，Compritol ATO 888）和稳定表面活性剂（泊洛沙姆，吐温80，大豆卵磷脂和十二烷基硫酸钠）的函数。与其他胶体载体的比较，应确定其潜在的用途在clinic.Methods，SLNs产生高压匀浆。通过测量与SLN孵育后HL 60细胞和人粒细胞的活力来评估细胞毒性。通过化学发光测量对颗粒内化进行定量。脂质的性质对生存能力没有影响;发现表面活性剂存在明显差异。与SLN表面的结合显著降低了表面活性剂的细胞毒性作用，对于泊洛沙姆184高达65倍。永久性HL 60细胞系-从具有粒细胞特征的细胞分化而来，通过视黄酸处理-产生与新鲜分离的人粒细胞相同的结果。总体而言，SLN的细胞毒性低于聚氰基丙烯酸烷基酯和聚乳酸/乙醇酸（PLA/GA）纳米颗粒。由于使用人粒细胞时结果相同，因此分化的HL 60细胞可用作静脉注射SLN制剂的易于获得的体外试验系统。SLN似乎适合作为药物载体系统的潜在静脉内使用，由于其在体外的细胞毒性非常低。
Purpose. Assessment of the in vitro cytotoxicity of solid lipid nanoparticles (SLNs) as a function of lipid matrix (Dynasan 114, Compritol ATO 888), and stabilizing surfactant (poloxamers, Tween 80, soya lecithin, and sodium dodecyl sulphate). Comparison with other colloidal carriers should determine their potential use in the clinic.Methods, SLNs were produced by high pressure homogenisation. Cytotoxicity was assessed by measuring the viability of HL60 cells and human granulocytes after incubation with SLNs. Particle internalisation was quantified by chemiluminescence measurements.Results. The nature of the lipid had no effect on viability; distinct differences were found for the surfactants. Binding to the SLN surface reduced markedly the cytotoxic effect of the surfactants, e.g., up to a factor of 65 for poloxamer 184. The permanent HL60 cell line-differentiated from cells with granulocyte characteristics by retinoic acid treatment-yielded results identical to freshly isolated human granulocytes. In general, the SLNs showed a lower cytotoxicity compared to polyalkylcyanoacrylate and polylactic/glycolic acid (PLA/GA) nanoparticles.Conclusions. Because the results are identical when using human granulocytes, differentiated HL60 cells can be used as an easily accessible in vitro test system for i.v. injectable SLN formulations. The SLNs appear suitable as a drug carrier system for potential intravenous use due to their very low cytotoxicity in vitro.