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

Abstract

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.

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 70 000-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 < 0.05). In particular, they showed about nine-fold higher AUC of the drug than did the commercial product

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.

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

Notes

Chul Soon Yong, College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712 749, South Korea. E-mail: [email protected]