School of Chemical Engineering, University of Campinas (UNICAMP), Campinas, São Paulo, Brazil.
Pharm Dev Technol. 2013 May-Jun;18(3):577-81. doi: 10.3109/10837450.2011.614250. Epub 2011 Sep 29.
The aim of the present work was to load mitotane, an effective drug for adrenocortical carcinoma treatment, in solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC). The SLN and NLC were successfully prepared by high shear homogenization followed by hot high pressure homogenization. Formulations were composed of cetyl palmitate as the solid lipid for SLN, whereas for NLC PEGylated stearic acid was selected as solid lipid and medium chain triacylglycerols as the liquid lipid. Tween® 80 and Span® 85 were used as surfactants for all formulations. The particle size, zeta potential, polydispersity index (PI), encapsulation efficiency (EE), and loading capacity (LC) were evaluated. The SLN showed a mean particle size of 150 nm, PI of 0.20, and surface charge -10 mV, and the EE and LC could reach up to 92.26% and 0.92%, respectively. The NLC were obtained with a mean particle size of 250 nm, PI of 0.30, zeta potential -15 mV and 84.50% EE, and 0.84% LC, respectively. Hydrophilic coating of SLN with chitosan or benzalkonium chloride was effective in changing zeta potential from negative to positive values. The results suggest that mitotane was efficiently loaded in SLN and in NLC, being potential delivery systems for improving mitotane LC and controlled drug release.
本工作旨在将米托坦（一种治疗肾上腺皮质癌的有效药物）载入固体脂质纳米粒（SLN）和纳米结构脂质载体（NLC）中。通过高剪切匀化随后进行热高压匀化成功制备了 SLN 和 NLC。配方由十六烷棕榈酸酯组成，作为 SLN 的固体脂质，而对于 NLC，选择了聚乙二醇化硬脂酸作为固体脂质，中链三酰基甘油作为液体脂质。Tween®80 和 Span®85 被用作所有制剂的表面活性剂。评估了粒径、Zeta 电位、多分散指数（PI）、包封效率（EE）和载药量（LC）。SLN 的平均粒径为 150nm，PI 为 0.20，表面电荷为-10mV，EE 和 LC 可分别达到 92.26%和 0.92%。NLC 的平均粒径为 250nm，PI 为 0.30，Zeta 电位为-15mV，EE 为 84.50%，LC 为 0.84%。用壳聚糖或苯扎氯铵对 SLN 进行亲水性包被可有效将 Zeta 电位从负值变为正值。结果表明，米托坦可有效地载入 SLN 和 NLC 中，这两种载体均具有提高米托坦 LC 和控制药物释放的潜力。
