Departamento de Farmacia, Facultad de Química Y de Farmacia, Pontificia Universidad Católica de Chile, Vicuña Mackena 4860, 7820436, Macul, Santiago, CP, Chile.
Centro de Investigación en Nanotecnología Y Materiales Avanzados "CIEN-UC", Pontificia Universidad Católica de Chile, Santiago, Chile.
Drug Deliv Transl Res. 2022 Nov;12(11):2740-2750. doi: 10.1007/s13346-022-01134-5. Epub 2022 Mar 13.
Two pegylated lipid nanocapsules for triamcinolone transdermal delivery were designed. Both present a size close to 50 nm and a single monomodal distribution in particle size (PI < 0.2), with a zeta potential of - 20 ± 2 and + 18 ± 1, respectively. The triamcinolone encapsulation efficacy varied between 68 and 80%. They proved to be stable under storage conditions (4 °C) for at least 6 months and at a physiological temperature, using different media, for 48 h. Also, they were shown not to affect cell viability at the concentrations used. For ex vivo transdermal experiments, newborn pig skin was used. With respect to the triamcinolone transdermal penetration, the nanocapsules were demonstrated to have an absorption promoting effect, both when the drug nanocapsules were in solution or loaded into the hydrogel, quantifying between 2 and 15 times more absorbed drug than the control. In addition, regarding the triamcinolone retained in the skin, it is observed that lipid nanocapsules act as triamcinolone promoters when the nanosystems were in solution and when they were included in the hydrogel. This vehicle showed a greater triamcinolone reservoir effect in comparison to the nanocapsules, proving to be a good vehicle to formulate triamcinolone transdermal delivery.
设计了两种用于曲安奈德经皮传递的聚乙二醇化脂质纳米胶囊。这两种纳米胶囊的粒径均接近 50nm，且粒径分布单一，多分散指数（PI）均小于 0.2，zeta 电位分别为-20±2 和+18±1。曲安奈德的包封效率在 68%至 80%之间。它们在 4°C 下储存至少 6 个月以及在生理温度下、使用不同的介质在 48 小时内均稳定。此外，在使用的浓度下，它们不会影响细胞活力。对于离体经皮实验，使用了新生猪皮。就曲安奈德经皮渗透而言，证明纳米胶囊具有促进吸收的作用，当药物纳米胶囊处于溶液中或负载到水凝胶中时，吸收的药物比对照品多 2 到 15 倍。此外，关于保留在皮肤中的曲安奈德，观察到当纳米系统处于溶液中或包含在水凝胶中时，脂质纳米胶囊作为曲安奈德促进剂发挥作用。与纳米胶囊相比，该载体表现出更大的曲安奈德储库效应，证明是一种很好的经皮传递曲安奈德的制剂载体。
