Aljuffali Ibrahim A, Pan Tai-Long, Sung Calvin T, Chang Shu-Hao, Fang Jia-You
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
School of Traditional Chinese Medicine, Chang Gung University, Kweishan, Taoyuan, Taiwan; Liver Research Center, Division of Hepatology, Department of Gastroenterology and Hepatology, Chang Gung Memorial Hospital, Kweishan, Taoyuan, Taiwan.
Nanomedicine. 2015 Aug;11(6):1321-30. doi: 10.1016/j.nano.2015.04.009. Epub 2015 Apr 29.
This study developed lipid nanocarriers, called squarticles, conjugated with anti-platelet-derived growth factor (PDGF)-receptor β antibody to determine whether targeted Minoxidil (MXD) delivery to the follicles and dermal papilla cells (DPCs) could be achieved. Squalene and hexadecyl palmitate (HP) were used as the matrix of the squarticles. The PDGF-squarticles showed a mean diameter and zeta potential of 195 nm and -46 mV, respectively. Nanoparticle encapsulation enhanced MXD porcine skin deposition from 0.11 to 0.23 μg/mg. The antibody-conjugated nanoparticles ameliorated follicular uptake of MXD by 3-fold compared to that of the control solution in the in vivo mouse model. Both vertical and horizontal skin sections exhibited a wide distribution of nanoparticles in the follicles, epidermis, and deeper skin strata. The encapsulated MXD moderately elicited proliferation of DPCs and vascular endothelial growth factor (VEGF) expression. The active targeting of PDGF-squarticles may be advantageous to improving the limited success of alopecia therapy.
Topical use of minoxidil is only one of the very few treatment options for alopecia. Nonetheless, the current delivery method is far from ideal. In this article, the authors developed lipid nanocarriers with anti-platelet-derived growth factor receptor ? antibody to target dermal papilla cells, and showed enhanced uptake of minoxidil.
本研究开发了一种名为“方形微粒”的脂质纳米载体,其与抗血小板衍生生长因子(PDGF)受体β抗体偶联,以确定是否能够实现将米诺地尔(MXD)靶向递送至毛囊和真皮乳头细胞(DPCs)。角鲨烯和十六烷基棕榈酸酯(HP)被用作方形微粒的基质。PDGF方形微粒的平均直径和zeta电位分别为195nm和-46mV。纳米颗粒包封使MXD在猪皮肤中的沉积量从0.11μg/mg提高到0.23μg/mg。在体内小鼠模型中,与对照溶液相比,抗体偶联的纳米颗粒使MXD的毛囊摄取量提高了3倍。垂直和水平皮肤切片均显示纳米颗粒在毛囊、表皮和更深层皮肤中广泛分布。包封的MXD适度地诱导了DPCs的增殖和血管内皮生长因子(VEGF)的表达。PDGF方形微粒的主动靶向可能有利于改善脱发治疗有限的成功率。
局部使用米诺地尔只是治疗脱发的极少数选择之一。尽管如此,目前的给药方法远非理想。在本文中,作者开发了带有抗血小板衍生生长因子受体?抗体的脂质纳米载体以靶向真皮乳头细胞,并显示米诺地尔的摄取增加。