Improved bioavailability and antiasthmatic efficacy of poorly soluble curcumin-solid dispersion granules obtained using fluid bed granulation

Issue title: Frontiers in Biomedical Engineering and Biotechnology – Proceedings of the 2nd International Conference on Biomedical Engineering and Biotechnology, 11–13 October 2013, Wuhan, China

Article type: Research Article

Authors: Jang, Dong-Jin | Kim, Sung Tae | Lee, Kooyeon^{; ;} | Oh, Euichaul^;

Affiliations: College of Pharmacy, The Catholic University of Korea, Bucheon, Gyeonggi 420-743, Republic of Korea | Department of Chemistry, University of Massachusetts-Amherst, 710 North Pleasant St., Amherst, Massachusetts 01003, United State | Department of Bio-Health Technology, Kangwon National University, Chuncheon 200-701, Kangwon, Republic of Korea | Institute of Bioscience and Biotechnology, Kangwon National University, Chuncheon 200-701, Republic of Korea

Note: [] Corresponding authors. E-mail: [email protected] (Kooyeon Lee) and [email protected] (Euichaul Oh)

Note: [] Corresponding authors. E-mail: [email protected] (Kooyeon Lee) and [email protected] (Euichaul Oh)

Abstract: The intestinal absorption and antiasthmatic efficacy of poorly water-soluble curcumin (CUR), which has low solubility and permeability, was increased by fabricating solid dispersion granules (SDGs). The SDG containing CUR (SDG-CUR) was prepared by dispersing CUR in excess Cremophor RH40 as a solubilizer and Ryoto sugar ester L-1695 as an absorption enhancer using fluid bed granulation. We evaluated the physicochemical properties such as crystallinity and dissolution, pharmacokinetics, and antiasthmatic efficacy of SDG-CUR. Our results showed that CUR was molecularly dispersed, and the dissolution of SDG-CUR was significantly higher than that of native CUR. In addition, the blood concentration of SDG-CUR in rats was much higher than that of native CUR. Compared to CUR, SDG-CUR showed a 9.1- and 13.1-fold increase in area under the plasma concentration-time curve (AUC) and maximum plasma concentration (Cmax), respectively. Further, SDG-CUR effectively alleviated airway hyperresponsiveness and levels of T-helper 2 cytokines (interleukin-4, interleukin-5, and interleukin-13) in a murine model of asthma. In conclusion, our results suggest that the SDGs could be considered as a potential oral formulation to enhance the absorption and efficacy of CUR.

Keywords: curcumin, absorption enhancer, fluid bed granulation, solid dispersion granule, antiasthmatic efficacy

DOI: 10.3233/BME-130826

Journal: Bio-Medical Materials and Engineering, vol. 24, no. 1, pp. 413-429, 2014