Development of flurbiprofen-loaded nanoparticles with a narrow size distribution using sucrose

作者：Oh Dong Hoon; Yan Yi Dong; Kim Dong Wuk; Kim Jong Oh; Yong Chul Soon; Choi Han Gon^*

来源：Drug Development and Industrial Pharmacy, 2014, 40(2): 172-177.

DOI：10.3109/03639045.2012.752501

• Flurbiprofen
• membrane emulsification
• nanoparticle
• narrow size distribution
• spray drying
• sucrose

Objective: A novel flurbiprofen-loaded nanoemulsion which gave uniform emulsion droplets with a narrow size distribution was previously reported to be prepared using membrane emulsification method. The purpose of this study is to develop a novel flurbiprofen-loaded nanoparticle with a narrow size distribution and improved bioavailability. %26lt;br%26gt;Method: The nanoparticle was prepared by solidifying nanoemulsion using sucrose as a carrier via spray drying method. Its physicochemical properties were investigated using SEM, DSC and PXRD. Furthermore, dissolution and bioavailability in rats were evaluated compared to a flurbiprofen-loaded commercial product. Results: The flurbiprofen-loaded nanoparticles with flurbiprofen/sucrose/surfactant mixture (1/20/2, weight ratio) gave good solidification and no stickiness. They associated with about 70000-fold improved drug solubility and had a mean size of about 300 nm with a narrow size distribution. Flurbiprofen was present in a changed amorphous state in these nanoparticles. Moreover, the nanoparticles gave significantly shorter T-max, and higher AUC and C-max of the drug compared to the commercial product (p%26lt;0.05). In particular, they showed about ninefold higher AUC of the drug than did the commercial product %26lt;br%26gt;Conclusion: These flurbiprofen-loaded nanoparticles prepared with sucrose by the membrane emulsification and spray drying method would be a potential candidate for orally delivering poorly water-soluble flurbiprofen with enhanced bioavailability.

• 出版日期2014-2