title: Improved bioavailability and antiasthmatic efficacy of poorly soluble curcumin-solid dispersion granules obtained using fluid bed granulation.
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.
authors.affiliation: College of Pharmacy, The Catholic University of Korea, Bucheon, Gyeonggi 420-743, Republic of Korea.
authors.forename: Dong-Jin
authors.initials: DJ
authors.lastname: Jang
authors.forename: Sung Tae
authors.initials: ST
authors.lastname: Kim
authors.forename: Kooyeon
authors.initials: K
authors.lastname: Lee
authors.forename: Euichaul
authors.initials: E
authors.lastname: Oh
mesh_terms: D000818:Animals; D001249:Asthma / Q000188:drug therapy* / Q000473:pathology; D001682:Biological Availability; D018938:Caco-2 Cells; D002627:Chemistry, Physical; D003474:Curcumin / Q000493:pharmacokinetics*; D004195:Disease Models, Animal; D005260:Female; D006801:Humans; D007073:Immunoglobulin E / Q000097:blood; D018793:Interleukin-13 / Q000378:metabolism; D015847:Interleukin-4 / Q000378:metabolism; D015848:Interleukin-5 / Q000378:metabolism; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009821:Oils / Q000737:chemistry; D010539:Permeability; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D013997:Time Factors; D014961:X-Ray Diffraction
chemical_list: D018793:Interleukin-13; D015848:Interleukin-5; D009821:Oils; D013501:Surface-Active Agents; D015847:Interleukin-4; D007073:Immunoglobulin E; D003474:Curcumin
keywords: absorption enhancer; antiasthmatic efficacy; curcumin; fluid bed granulation; solid dispersion granule