Sütő Blanka, Berkó Szilvia, Kozma Gábor, Kukovecz Ákos, Budai-Szűcs Mária, Erős Gábor, Kemény Lajos, Sztojkov-Ivanov Anita, Gáspár Róbert, Csányi Erzsébet
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Szeged, Hungary.
Department of Applied and Environmental Chemistry, University of Szeged, Szeged, Hungary.
Int J Nanomedicine. 2016 Mar 30;11:1201-12. doi: 10.2147/IJN.S99198. eCollection 2016.
An ibuprofen-loaded nanostructured lipid carrier (IBU-NLC) was developed for enhanced skin penetration to improve the treatment of osteoarthritis and other musculoskeletal diseases. The mean particle size was 106 nm, with a spherical morphology, a smooth surface, and a zeta potential of -18.4 mV. X-ray diffraction studies revealed the amorphous state of the lipid matrix. Both Raman spectroscopy and Fourier transformation infrared analysis indicated no major shifts in the spectra of the formulations, which suggest rapid drug dissolution from the nanoparticles. The drug loading was 9.85%, and the entrapment efficiency was 98.51%. In vitro release of the NLC dispersion, in vitro permeation, and in vivo animal studies of IBU-NLC gel all confirmed that the permeation of IBU was significantly better than that of a reference after 6 hours. In conclusion, IBU-NLC gel is of great potential to enhance drug permeation through the skin and hence the efficacy of the treatment of chronic joint inflammation.
开发了一种负载布洛芬的纳米结构脂质载体(IBU-NLC),以增强皮肤渗透,改善骨关节炎和其他肌肉骨骼疾病的治疗。平均粒径为106nm,呈球形形态,表面光滑,zeta电位为-18.4mV。X射线衍射研究揭示了脂质基质的无定形状态。拉曼光谱和傅里叶变换红外分析均表明制剂光谱无重大位移,这表明药物从纳米颗粒中快速溶解。载药量为9.85%,包封率为98.51%。IBU-NLC凝胶的NLC分散体的体外释放、体外渗透和体内动物研究均证实,6小时后IBU的渗透明显优于参比制剂。总之,IBU-NLC凝胶在增强药物经皮渗透以及慢性关节炎症治疗效果方面具有巨大潜力。