Department of Pharmaceutics, The University of Mississippi, University, Mississippi 38677, USA.
J Pharm Sci. 2010 Oct;99(10):4267-76. doi: 10.1002/jps.22150.
The present study aimed to develop bilayered nail lacquer of terbinafine hydrochloride (TH) for treatment of onychomycosis. The composite nail lacquer formed an underlying drug-loaded hydrophilic layer and overlying hydrophobic vinyl layer. The hydrophilic lacquer made of hydroxylpropyl methylcellulose E-15 contained polyethylene glycol 400 (PEG 400) as a drug permeation enhancer. The vinyl lacquer was composed of poly (4-vinyl phenol) as a water-resistant film former. In vitro permeation studies in Franz diffusion cells indicated that the amount of TH permeated across the human cadaver nail in 6 days was 0.32 +/- 0.14, 1.12 +/- 0.42, and 1.42 +/- 0.53 microg/cm(2) from control (hydrophilic lacquer devoid of PEG 400), monolayer (hydrophilic lacquer alone), and bilayered nail lacquers, respectively. A higher nail drug load was seen in vitro with the bilayered lacquer (0.59 +/- 0.13 microg/mg) as compared to monolayer (0.36 +/- 0.09 microg/mg) and control (0.28 +/- 0.07 microg/mg) lacquers. The drug loss despite multiple washing was significantly low (p < 0.001) for the bilayered lacquer owing to the protective vinyl coating. Clinical studies demonstrated the efficacy of bilayered lacquer to achieve better drug load in the nail plate (1.27 +/- 0.184 microg/mg) compared to monolayer (0.67 +/- 0.18 microg/mg) and control (0.21 +/- 0.04 microg/mg) lacquers.
本研究旨在开发盐酸特比萘芬(TH)双层指甲油,用于治疗甲真菌病。复合指甲油形成了一个底层载药亲水性层和上层疏水性乙烯基层。由羟丙基甲基纤维素 E-15 制成的亲水性指甲油含有聚乙二醇 400(PEG 400)作为药物渗透增强剂。乙烯基漆由聚(4-乙烯基苯酚)组成,作为耐水成膜剂。Franz 扩散池体外渗透研究表明,TH 透过人体尸体指甲的量在 6 天内分别为 0.32 +/- 0.14、1.12 +/- 0.42 和 1.42 +/- 0.53 microg/cm(2),来自对照(不含 PEG 400 的亲水性漆)、单层(亲水性漆单独)和双层指甲油。体外观察到双层漆的指甲药物载量更高(0.59 +/- 0.13 microg/mg),而单层漆(0.36 +/- 0.09 microg/mg)和对照漆(0.28 +/- 0.07 microg/mg)。尽管多次洗涤,但双层漆的药物损失明显较低(p < 0.001),这是由于其保护性乙烯基涂层。临床研究表明,双层漆能够更好地将药物载入指甲板,达到更好的疗效(1.27 +/- 0.184 microg/mg),而单层漆(0.67 +/- 0.18 microg/mg)和对照漆(0.21 +/- 0.04 microg/mg)。