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电解质和泊洛沙姆 188 对固体脂质纳米粒(SLNs)聚集动力学的影响。

Influence of electrolyte and poloxamer 188 on the aggregation kinetics of solid lipid nanoparticles (SLNs).

机构信息

Department of Pharmaceutical Engineering, School of Chemical Engineering, Tianjin University, Tianjin, PR China.

出版信息

Drug Dev Ind Pharm. 2012 Sep;38(9):1084-9. doi: 10.3109/03639045.2011.640331. Epub 2011 Dec 19.

DOI:10.3109/03639045.2011.640331
PMID:22181005
Abstract

Solid lipid nanoparticles (SLNs) have attracted increasing attention as colloidal drug carriers due to theirs advantages including low toxicity, drug targeting and modified release. However, undesired particle aggregation in aqueous dispersions would limit the applicability of SLNs for drug delivery. The purpose of the present article is to investigate the aggregation behavior of the SLNs and quantitatively evaluate how the concentration of NaCl and F68 affect the stability of the SLNs. The early stage aggregation kinetics of the SLNs was investigated over a wide range of NaCl concentrations by employing dynamic light scattering (DLS). In the presence of the NaCl, aggregation kinetics of the SLNs exhibited reaction-limited (slow) and diffusion-limited (fast) regimes. These results indicated that the aggregation behavior of these new nanoparticles can be well explained by the classical Derjaguin-Landau-Verwey-Overbeek (DLVO) theory. The critical coagulation concentration (CCC) of SLNs containing 0.0%, 0.1%, 0.5%, 2.0%, and 4.0% of Poloxamer 188 (F68) was 416, 328, 519, 607, and 602 mM, respectively, suggesting that the F68 influences the aggregation behavior of the SLNs. F68 made the SLNs more sensitive to the electrolyte when its concentration is low (0.1%), the bush of the polymer F68 has a bridging effect that accelerated the aggregation process of the SLNs. However, at the high concentration, F68 can provide the steric repulsion to the nanoparticles, which effectively stabilized the SLNs dispersions.

摘要

固体脂质纳米粒(SLNs)由于其低毒性、药物靶向和缓释等优点,作为胶体药物载体受到越来越多的关注。然而,在水相中,不希望出现的颗粒聚集会限制 SLNs 在药物传递中的适用性。本文旨在研究 SLNs 的聚集行为,并定量评估 NaCl 和 F68 的浓度如何影响 SLNs 的稳定性。通过动态光散射(DLS)研究了 SLNs 在宽 NaCl 浓度范围内的早期聚集动力学。在 NaCl 的存在下,SLNs 的聚集动力学表现出反应限制(缓慢)和扩散限制(快速)两个阶段。这些结果表明,这些新纳米颗粒的聚集行为可以很好地用经典的德加古因-兰德劳-弗韦尔-奥弗贝克(DLVO)理论来解释。含有 0.0%、0.1%、0.5%、2.0%和 4.0%的泊洛沙姆 188(F68)的 SLNs 的临界聚沉浓度(CCC)分别为 416、328、519、607 和 602mM,表明 F68 影响 SLNs 的聚集行为。当 F68 的浓度较低(0.1%)时,F68 使 SLNs 对电解质更加敏感,聚合物 F68 的支链具有桥接作用,加速了 SLNs 的聚集过程。然而,在高浓度下,F68 可以为纳米颗粒提供空间排斥,有效地稳定了 SLNs 分散体。

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