Department of Physical Chemistry, Faculty of Pharmacy, University of Barcelona, Barcelona, Spain.
Colloids Surf B Biointerfaces. 2011 Nov 1;88(1):150-7. doi: 10.1016/j.colsurfb.2011.06.025. Epub 2011 Jun 25.
Triamcinolone acetonide (TA) is a corticosteroid drug currently administered by intravitreal injection for a broad spectrum of inflammatory, edematous and angiogenic ocular diseases. To increase the drug's bioavailability by ocular instillation, TA was encapsulated in nanostructured lipid carriers (NLC), previously optimized by our group using a factorial design approach. In the present paper, nanometric (∼200 nm), unimodal and negatively charged NLC loaded with the fluorescent lipid marker Nile red (NR-NLC) and drug (TA-NLC) were produced by high pressure homogenization. Based on the selected formulations, in vivo tests were carried out by eye-drop instillation of NR-NLC in mice, revealing the systems' ability of delivering lipophilic actives to the posterior segment of the eye via the corneal and non-corneal pathways. Short and long-term stability of TA-NLC was assessed by high performance stability analysis using the Turbiscan®. The results showed a backscattering of less than 1.5% and during a period of 6 months, anticipated the low tendency of these particles for aggregation during shelf life when stored at room temperature.
曲安奈德（TA）是一种皮质类固醇药物，目前通过玻璃体内注射用于治疗广泛的炎症、水肿和血管生成性眼病。为了通过眼部滴注提高药物的生物利用度，我们小组先前使用析因设计方法对 TA 进行了纳米结构脂质载体（NLC）包封。在本文中，通过高压匀质法制备了纳米级（∼200nm）、单峰和带负电荷的负载荧光脂质标记尼罗红（NR-NLC）和药物（TA-NLC）的 NLC。基于所选配方，通过在小鼠中滴眼滴注 NR-NLC 进行了体内测试，结果表明该系统能够通过角膜和非角膜途径将亲脂性活性剂递送至眼部后段。使用 Turbiscan®进行高性能稳定性分析评估了 TA-NLC 的短期和长期稳定性。结果表明，背散射小于 1.5%，在 6 个月的时间内，预计这些颗粒在室温下储存时在保质期内聚集的趋势较低。
