Inoue Yutaka, Hibino Mitsue, Murata Isamu, Kanamoto Ikuo
Laboratory of Drug Safety Management, Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado-shi, Saitama, 3500295, Japan.
Pharm Res. 2017 Dec 28;35(1):1. doi: 10.1007/s11095-017-2311-3.
As trisodium L-ascorbyl 2-phosphate 6-palmitate (APPS), an ascorbic acid derivative, is an amphiphilic substance, it forms micelles in aqueous solutions. Micelles are used as drug carriers and can emulsify drugs that are poorly soluble in water, such as nadifloxacin (NDFX). The purpose of this study was to prepare nanocarriers using APPS to carry NDFX into Yucatan micropig skin.
After synthesis of the NDFX nanoparticles by using the hydration method, physical evaluations were carried out that included assessments of particle size and zeta potential, encapsulation efficiency, particle structure by transmission electron microscopy, P-NMR spectra, and particle stability. Functional evaluations of the nanoparticles included 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assays, skin penetration tests, and fluorescence microscopy observations.
The encapsulation efficiency of NDFX in the nanoparticles was approximately 75%. With added magnesium chloride, the nanoparticles remained stably dispersed in aqueous solution for at least 14 days at 25°C under protection from light. In addition, the nanoparticle formulation improved the skin permeability of NDFX.
APPS-derived nanoparticles were shown to be useful as skin-targeting nanocarriers.
L-抗坏血酸2-磷酸6-棕榈酸三钠（APPS）作为一种抗坏血酸衍生物，是一种两亲性物质，在水溶液中形成胶束。胶束用作药物载体，可乳化难溶于水的药物，如那氟沙星（NDFX）。本研究的目的是制备以APPS为载体将NDFX导入尤卡坦小型猪皮肤的纳米载体。
采用水化法合成NDFX纳米颗粒后，进行了包括粒径和zeta电位评估、包封率、透射电子显微镜观察颗粒结构、P-NMR光谱以及颗粒稳定性等物理评价。纳米颗粒的功能评价包括2,2-二苯基-1-苦基肼（DPPH）自由基清除试验、皮肤渗透试验和荧光显微镜观察。
NDFX在纳米颗粒中的包封率约为75%。添加氯化镁后，纳米颗粒在25°C避光条件下在水溶液中至少稳定分散14天。此外，纳米颗粒制剂提高了NDFX的皮肤渗透性。
APPS衍生的纳米颗粒被证明可作为皮肤靶向纳米载体。
