Department of Pharmaceutical Sciences , University of Milan , via Giuseppe Colombo, 71 , 20133 Milan , Italy.
Department of Drug Chemistry and Technologies , "Sapienza" University of Rome , Piazzale Aldo Moro 5 , 00185 , Rome , Italy.
Mol Pharm. 2018 Mar 5;15(3):1028-1036. doi: 10.1021/acs.molpharmaceut.7b00926. Epub 2018 Feb 2.
The feasibility to use gellan nanohydrogels (Ge-NHs) as delivery system for the cutaneous administration of piroxicam (PRX) was investigated using gellan conjugated with cholesterol or riboflavin. The in vitro skin penetration studies through human epidermis were performed using a saturated aqueous drug solution, a 50% w/v Transcutol aqueous solution, and a commercially available PRX plaster as controls. Confocal microscopy, ATR-FTIR spectroscopy, circular dichroism, and a dynamometer assisted extrusion assay were performed to clarify the permeation mechanism of Ge-NHs. The skin permeation studies evidenced that Ge-NHs enhance the PRX retention in the epidermis and, at the same time, slow down the permeation process with respect to the controls. NHs can penetrate the stratum corneum, and then gradually disassemble thus diffusing in the viable epidermis reaching the spinosum layer. In conclusion, NHs represent a novel strategy to target poorly permeable compounds in the epidermis, thus improving the management of cutaneous pathologies.
研究了用接枝有胆固醇或核黄素的胶凝纳米水凝胶（Ge-NHs）作为吡罗昔康（PRX）经皮给药的递送系统的可行性。使用饱和水溶液、50% w/v Transcutol 水溶液和市售的 PRX 贴剂作为对照，通过人表皮进行体外皮肤渗透研究。共聚焦显微镜、ATR-FTIR 光谱、圆二色性和测力计辅助挤出测定用于阐明 Ge-NHs 的渗透机制。皮肤渗透研究表明，Ge-NHs 增强了 PRX 在表皮中的保留，同时相对于对照减慢了渗透过程。NHs 可以穿透角质层，然后逐渐分解，从而在有活力的表皮中扩散，到达棘状层。总之，NHs 代表了一种将表皮中渗透性差的化合物靶向的新策略，从而改善了皮肤病理的治疗效果。
