Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

Linghui Dian,^1,2,* Zhiwen Yang,^3,* Feng Li,¹ Zhouhua Wang,¹ Xin Pan,¹ Xinsheng Peng,² Xintian Huang,¹ Zhefei Guo,¹ Guilan Quan,¹ Xuan Shi,¹ Bao Chen,¹ Ge Li,⁴ Chuanbin Wu<sup>1,4

1</sup>School of Pharmaceutical Sciences, Sun Yat-Sen University, University Town, Guangzhou, People’s Republic of China; ²School of Pharmaceutical Sciences, Guangdong Medical College, Dongguan, People’s Republic of China; ³Department of Gastroenterology, Songjiang Branch of the Affiliated First People’s Hospital of Shanghai Jiaotong University, Shanghai, People’s Republic of China; ⁴Guangdong Research Center for Drug Delivery Systems, Guangzhou, People’s Republic of China

*These authors contributed equally to this work

Abstract: In order to improve the oral bioavailability of ibuprofen, ibuprofen-loaded cubic nanoparticles were prepared as a delivery system for aqueous formulations. The cubic inner structure was verified by cryogenic transmission electron microscopy. With an encapsulation efficiency greater than 85%, the ibuprofen-loaded cubic nanoparticles had a narrow size distribution around a mean size of 238 nm. Differential scanning calorimetry and X-ray diffraction determined that ibuprofen was in an amorphous and molecular form within the lipid matrix. The in vitro release of ibuprofen from cubic nanoparticles was greater than 80% at 24 hours, showing sustained characteristics. The pharmacokinetic study in beagle dogs showed improved absorption of ibuprofen from cubic nanoparticles compared to that of pure ibuprofen, with evidence of a longer half-life and a relative oral bioavailability of 222% (P < 0.05). The ibuprofen-loaded cubic nanoparticles provide a promising carrier candidate with an efficient drug delivery for therapeutic treatment.

Keywords: ibuprofen, cubic nanoparticles, oral drug delivery, bioavailability