Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil.
Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul, PBox 15003, Porto Alegre, 91501-970, RS, Brazil.
Int J Pharm. 2012 Apr 15;426(1-2):271-279. doi: 10.1016/j.ijpharm.2012.01.051. Epub 2012 Feb 1.
The hemocompatibility of nanoparticles is of critical importance for their systemic administration as drug delivery systems. Formulations of lipid-core nanocapsules, stabilized with polysorbate 80-lecithin and uncoated or coated with chitosan (LNC and LNC-CS), were prepared and characterized by laser diffraction (D[4,3]: 129 and 134 nm), dynamic light scattering (119 nm and 133 nm), nanoparticle tracking (D50: 124 and 139 nm) and particle mobility (zeta potential: -15.1 mV and +9.3 mV) analysis. In vitro hemocompatibility studies were carried out with mixtures of nanocapsule suspensions in human blood at 2% and 10% (v/v). The prothrombin time showed no significant change independently of the nanocapsule surface potential or its concentration in plasma. Regarding the activated partial thromboplastin time, both suspensions at 2% (v/v) in plasma did not influence the clotting time. Even though suspensions at 10% (v/v) in plasma decreased the clotting times (p<0.05), the values were within the normal range. The ability of plasma to activate the coagulation system was maintained after the addition of the formulations. Suspensions at 2% (v/v) in blood showed no significant hemolysis or platelet aggregation. In conclusion, the lipid-core nanocapsules uncoated or coated with chitosan are hemocompatible representing a potential innovative nanotechnological formulation for intravenous administration.
纳米颗粒的血液相容性对于它们作为药物递送系统的全身给药至关重要。用聚山梨酯 80-卵磷脂稳定的脂质核纳米胶囊制剂，以及未涂层或用壳聚糖（LNC 和 LNC-CS）涂层的制剂，通过激光衍射（D[4,3]：129 和 134nm）、动态光散射（119nm 和 133nm）、纳米颗粒跟踪（D50：124 和 139nm）和颗粒迁移率（zeta 电位：-15.1mV 和+9.3mV）分析进行了表征。在 2%和 10%（v/v）的人血纳米胶囊混悬液混合物中进行了体外血液相容性研究。无论纳米胶囊表面电位或其在血浆中的浓度如何，凝血酶原时间均无显著变化。关于活化部分凝血活酶时间，两种浓度（2%v/v）的混悬液在血浆中均不影响凝血时间。尽管在血浆中的混悬液浓度为 10%（v/v）时会降低凝血时间（p<0.05），但这些值仍在正常范围内。添加制剂后，血浆激活凝血系统的能力得以维持。在血液中的混悬液浓度为 2%（v/v）时，没有明显的溶血或血小板聚集。综上所述，未涂层或用壳聚糖涂层的脂质核纳米胶囊具有血液相容性，代表了一种潜在的用于静脉内给药的创新纳米技术制剂。
