Freie Universität Berlin, Institute of Pharmacy, Germany.
Philipps-Universität Marburg, Department of Pharmaceutics and Biopharmaceutics, Germany.
Int J Pharm. 2019 May 1;562:293-302. doi: 10.1016/j.ijpharm.2019.03.016. Epub 2019 Mar 8.
smartPearls are a novel dermal delivery system based on mesoporous (pores 2-50 nm) particles, developed in 2014. Their pores can be loaded with active which is long-term stabilized in its amorphous state. The increased saturation solubility by the amorphous state leads to an increased dermal bioavailability of poorly soluble actives. To avoid sedimentation of the porous particles (3-50 µm) in dermal formulations, viscoelastic gels were developed using ι-carrageenan, polyacrylate and the viscoelastic Kühne salad dressing as a reference from food industry. Silica particles (company Grace/US, 50 and 150 µm) were loaded into the gels and long-term stability was assessed by a VIS sedimentation test. Furthermore, the gels were characterized by analytical centrifugation (LUMiSizer) to assess the critical rpm/g values, allowing to order them after their absolute viscoelastic stabilizing ability. Characterization was complemented by rotation rheology, amplitude sweep and a frequency sweep analysis for the determination of elastic and viscous moduli G' and G'' at varying conditions. Based on the throughout characterization, polymers can be selected to sufficiently stabilize dermal formulations even with large sized smartPearls - the prerequisite for using this delivery system in dermal products.
智能珍珠是一种新型的基于中孔（孔 2-50nm）颗粒的透皮给药系统，于 2014 年开发。其孔可以装载活性物质，该活性物质在无定形状态下长期稳定。无定形状态下的增加的饱和溶解度导致较差溶性活性物质的透皮生物利用度增加。为了避免多孔颗粒（3-50µm）在透皮制剂中的沉淀，使用 ι-卡拉胶、聚丙烯酸和食品工业中作为参考的粘弹性 Kühne 沙拉酱开发了粘弹性凝胶。将硅胶颗粒（Grace/US 公司，50 和 150µm）装入凝胶中，并通过 VIS 沉降试验评估长期稳定性。此外，通过分析离心（LUMiSizer）对凝胶进行了表征，以评估允许根据其绝对粘弹性稳定能力对其进行排序的临界 rpm/g 值。通过旋转流变学、振幅扫描和频率扫描分析进行了补充，以确定在不同条件下弹性和粘性模量 G'和 G''。基于全面的表征，可以选择聚合物来充分稳定透皮制剂，即使使用大尺寸的智能珍珠也是如此——这是在透皮产品中使用这种给药系统的前提条件。
