Laboratory of Food, Drug, and Cosmetics (LTMAC), School of Health Sciences, University of Brasília, 70910-900 Brasília, DF, Brazil.
Laboratory of Food, Drug, and Cosmetics (LTMAC), School of Health Sciences, University of Brasília, 70910-900 Brasília, DF, Brazil.
Int J Biol Macromol. 2020 May 15;151:56-61. doi: 10.1016/j.ijbiomac.2020.02.143. Epub 2020 Feb 14.
In general, nanometer-sized drug delivery systems have a natural tendency for accommodation in the follicular cavities, which makes them advantageous in the treatment of conditions affecting these structures. Still, follicular targeting enhancement can improve therapy outcomes. Here, we compare two strategies to further promote dutasteride follicular-targeted delivery: the chemical modulation of nanosystem surface properties by coating with the natural polymer chitosan, and the application of a massage. For this, poly-(ɛ-caprolactone)-lipid-core nanocapsules (NC) containing dutasteride were developed and had their permeation profile compared to chitosan-coated nanocapsules (NC-CS). Nanocapsules showed high drug encapsulation efficiency (>94%), and stability for up to 90 days of storage. As expected, chitosan coating increased the size and zeta potential, from 199.0 ± 0.5 nm (PdI of 0.12) and - 13.6 ± 0.6 mV to 224.9 ± 3.4 nm (PdI 0.23) and + 40.2 ± 0.8 mV, respectively. Both coated and non-coated nanoparticles targeted the hair follicles compared to a drug solution. Enhanced hair follicles targeting was observed after the massage procedure, with 5 and 2-fold increases relative to NC and NC-CS, respectively. In conclusion, this work demonstrates dutasteride nanocapsules can target the follicular casts, and a simple physical stimulation can enhance 5-times the drug amount accumulated.
一般来说,纳米级药物递送系统具有自然倾向于容纳在滤泡腔中,这使得它们在治疗影响这些结构的疾病方面具有优势。然而,滤泡靶向增强可以改善治疗效果。在这里,我们比较了两种进一步促进度他雄胺滤泡靶向递送的策略:通过用天然聚合物壳聚糖涂覆来化学调节纳米系统表面性质,以及应用按摩。为此,开发了含有度他雄胺的聚(ε-己内酯)-脂质核纳米胶囊(NC),并将其渗透特性与壳聚糖涂层纳米胶囊(NC-CS)进行了比较。纳米胶囊显示出高药物包封效率(>94%),并在储存长达 90 天的时间内保持稳定。正如预期的那样,壳聚糖涂层增加了尺寸和 Zeta 电位,从 199.0 ± 0.5nm(PdI 为 0.12)和-13.6 ± 0.6mV 分别增加到 224.9 ± 3.4nm(PdI 0.23)和+40.2 ± 0.8mV。与药物溶液相比,两种涂层和未涂层的纳米粒子都靶向毛囊。按摩后观察到毛囊靶向增强,与 NC 和 NC-CS 相比,分别增加了 5 倍和 2 倍。总之,这项工作表明度他雄胺纳米胶囊可以靶向毛囊管,并且简单的物理刺激可以使累积的药物量增加 5 倍。