Jianan Wang1, Lulu Wang2,3, Lan Zhang2, Dandan He2,3, Jianming Ju2,3, Weiguang Li4. 1. Department of Pharmacy, Jining Medical University, Shandong, China. 2. Hospital of Integrated Traditional Chinese and Western Medicine Affiliated to Nanjing University of Chinese Medicine, Nanjing, China. 3. Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, China. 4. Department of Marine Pharmacy, China Pharmaceutical University, Nanjing, China.
Abstract
OBJECTIVES: With the purpose of developing a curcumin phospholipid complex (CPC) formulation with high performance, the CPC was prepared and solidified with Soluplus® in this study. METHODS: Soluplus® was used as a carrier to solidify CPC. The structures of the CPC and curcumin phospholipid complex - Soluplus® solidified powder (CSP) - were also characterized by differential scanning electron microscope, differential scanning calorimetry, Fourier transform infrared spectroscopy and X-ray diffractometer, and flowability, in-vitro dissolution and oral bioavailability were also investigated. KEY FINDINGS: All analysis indicated that curcumin was completely converted from crystalline to amorphous state in solidified powder. The angle of repose calculated in flowability study indicated a marked improvement from 'cannot be measured' to '37°'. Meanwhile, the dissolution study showed that in phosphate buffer condition, the dissolution rate of CSP had released 76.34% in pH 6.8 and the 78.19% in pH 1.2. Furthermore, in pharmacokinetic study, significant (P < 0.01) improvement of AUC0-∞ value was observed between CPC and CSP groups, and the results showed that AUC0-∞ value was increased from 205.84 ± 50.46 μg h/ml to 330.47 μg h/ml. CONCLUSIONS: A simple and convenient solidifying process was used in this study, and the data suggested that this process not only could improve the flowability and dissolution of phospholipid complex, but also increased the oral bioavailability of curcumin.
OBJECTIVES: With the purpose of developing a curcumin phospholipid complex (CPC) formulation with high performance, the CPC was prepared and solidified with Soluplus® in this study. METHODS: Soluplus® was used as a carrier to solidify CPC. The structures of the CPC and curcumin phospholipid complex - Soluplus® solidified powder (CSP) - were also characterized by differential scanning electron microscope, differential scanning calorimetry, Fourier transform infrared spectroscopy and X-ray diffractometer, and flowability, in-vitro dissolution and oral bioavailability were also investigated. KEY FINDINGS: All analysis indicated that curcumin was completely converted from crystalline to amorphous state in solidified powder. The angle of repose calculated in flowability study indicated a marked improvement from 'cannot be measured' to '37°'. Meanwhile, the dissolution study showed that in phosphate buffer condition, the dissolution rate of CSP had released 76.34% in pH 6.8 and the 78.19% in pH 1.2. Furthermore, in pharmacokinetic study, significant (P < 0.01) improvement of AUC0-∞ value was observed between CPC and CSP groups, and the results showed that AUC0-∞ value was increased from 205.84 ± 50.46 μg h/ml to 330.47 μg h/ml. CONCLUSIONS: A simple and convenient solidifying process was used in this study, and the data suggested that this process not only could improve the flowability and dissolution of phospholipid complex, but also increased the oral bioavailability of curcumin.