Improved skin delivery of voriconazole with a nanostructured lipid carrier-based hydrogel formulation.
Improved skin delivery of voriconazole with a nanostructured lipid carrier-based hydrogel formulation.
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DOI：
10.1248/cpb.c14-00202
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发表时间：
2014-08
影响因子：
1.7
通讯作者：
S. Song;Kyung Min Lee;Jong Boo Kang;Sang Gon Lee;M. Kang;Y. Choi
中科院分区：
文献类型：
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作者：
S. Song;Kyung Min Lee;Jong Boo Kang;Sang Gon Lee;M. Kang;Y. Choi
为了开发伏立康唑（VRC）用于治疗皮肤真菌感染的局部制剂，开发了基于纳米结构脂质载体的水凝胶（NLC-凝胶）制剂，并检查了其物理特性、体外皮肤渗透性和保留曲线。通过高压均质化制备由Precirol ATO 5、Labrafil 1944 CS和Tween 80组成的负载VRC的NLC分散体，并将其包埋到Carbopol 940水凝胶中。水凝胶中的脂质纳米颗粒的尺寸约为210 nm，具有球形形状和-30 mV的ζ电位。在使用装有脱毛小鼠皮肤的Franz扩散池进行的皮肤渗透研究中，NLC-凝胶上级于常规乳膏和微乳液基凝胶制剂，分别显示出2.8倍和1.7倍的通量值。此外，与参比制剂相比，NLC-凝胶导致VRC在更深的皮肤层中显著更大的积累。总之，本文报告的新型局部制剂代表了皮肤感染（如念珠菌病）的替代治疗，与口服治疗相比，全身不良反应的可能性较小。
In order to develop topical preparations of voriconazole (VRC) for the treatment of mycotic infections of the skin, a nanostructured lipid carrier-based hydrogel (NLC-gel) formulation was developed and its physical characteristics, in vitro skin permeation, and retention profiles were examined. A VRC-loaded NLC dispersion, consisting of Precirol ATO 5, Labrafil 1944 CS, and Tween 80, was prepared by high-pressure homogenization and embedded into Carbopol 940 hydrogel. The lipid nanoparticles in the hydrogel were approximately 210 nm in size, with a spherical shape and zeta potential of -30 mV. In a skin permeation study using a Franz diffusion cell mounted with depilated mouse skin, the NLC-gel was superior to conventional cream and microemulsion-based gel formulations, showing 2.8- and 1.7-fold greater flux values, respectively. In addition, the NLC-gel led to markedly greater accumulation of VRC in deeper skin layers as compared with the reference formulations. In conclusion, the novel topical formulation reported here represents an alternative treatment for skin infections such as candidiasis, with less potential for systemic adverse effects than oral therapy.