Główka Eliza, Wosicka-Frąckowiak Hanna, Hyla Kinga, Stefanowska Justyna, Jastrzębska Katarzyna, Klapiszewski Łukasz, Jesionowski Teofil, Cal Krzysztof
Department of Pharmaceutical Technology, Poznan University of Medical Sciences, Poznań, Poland.
Department of Pharmaceutical Technology, Poznan University of Medical Sciences, Poznań, Poland.
Eur J Pharm Biopharm. 2014 Sep;88(1):75-84. doi: 10.1016/j.ejpb.2014.06.019. Epub 2014 Jul 9.
Drug delivery into hair follicles with the use of nanoparticles (NPs) is gaining more importance as drug-loaded NPs may accumulate in hair follicle openings. The aim was to develop and evaluate a pluronic lecithin organogel (PLO) with roxithromycin (ROX)-loaded NPs for follicular targeting. Polymeric NPs were evaluated in terms of particle shape, size, zeta potential, suspension stability, encapsulation efficiency and in vitro drug release. Lyophilized NPs were incorporated into the PLO and rheological measurements of the nanoparticles-embedded organogels were done. The fate of the NPs in the skin was traced by incorporation of a fluorescent dye into the NPs. As a result, ROX was efficiently incorporated into polymeric NPs characterized by the appropriate size (approximately 300 nm) allowing drug delivery to hair follicles. In ex vivo human skin penetration studies, horizontal skin sections revealed fluorescence deep in the hair follicles. Although the organogel has higher affinity to the lipidic follicular area than an aqueous suspension of NPs, it did not seem to improve penetration of the NPs along the hair shaft. The results proved that it was possible to achieve preferential targeting to the pilosebaceous unit using polymeric NPs formulated either into the aqueous suspension or semisolid topical formulation.
随着载药纳米颗粒(NPs)可能在毛囊开口处蓄积,利用纳米颗粒向毛囊递送药物正变得越来越重要。本研究旨在开发并评估一种含有载罗红霉素(ROX)纳米颗粒的泊洛沙姆卵磷脂有机凝胶(PLO)用于毛囊靶向。对聚合物纳米颗粒的颗粒形状、大小、zeta电位、混悬稳定性、包封率及体外药物释放进行了评估。将冻干的纳米颗粒加入到PLO中,并对包埋纳米颗粒的有机凝胶进行流变学测量。通过在纳米颗粒中掺入荧光染料来追踪纳米颗粒在皮肤中的去向。结果显示,ROX被有效地包入聚合物纳米颗粒中,其大小合适(约300nm),有利于向毛囊递送药物。在离体人皮肤渗透研究中,水平皮肤切片显示毛囊深部有荧光。尽管有机凝胶对毛囊脂质区域的亲和力高于纳米颗粒的水混悬液,但它似乎并未改善纳米颗粒沿毛干的渗透。结果证明,将聚合物纳米颗粒制成水混悬液或半固体局部制剂能够实现对皮脂腺单位的优先靶向。