PMID- 25891482 OWN - NLM STAT- MEDLINE DCOM- 20160125 LR - 20150504 IS - 1791-244X (Electronic) IS - 1107-3756 (Linking) VI - 35 IP - 6 DP - 2015 Jun TI - Influence of particle size on the in vitro and in vivo anti-inflammatory and anti-allergic activities of a curcumin lipid nanoemulsion. PG - 1720-8 LID - 10.3892/ijmm.2015.2186 [doi] AB - The polyphenolic compound, curcumin, is a natural yellow pigment component of turmeric. It exerts various biological effects, such as anti-inflammatory effects, and we have previously demonstrated that curcumin is a specific inhibitor of DNA polymerase lambda. Curcumin is characterized by poor bioavailability as it is water-insoluble, is poorly absorbed and is systemically eliminated. In order to increase the bioavailability of curcumin, in this study, we produced a curcumin-loaded lipid nanoemulsion of various particle sizes (50, 100 and 200 nm). The curcumin lipid nanoemulsion was prepared by a modified thin-film hydration method followed by sonication. To identify the optimal particle size which exhibits the strongest physiological activity, we investigated the inhibitory effects of the obtained nanoemulsions against inflammatory and allergic activities. In in vitro cell culture experiments, the 100-nm curcumin lipid nanoemulsion showed the most prominent inhibitory effect on the production of tumor necrosis factor-alpha (TNF-alpha) induced by lipopolysaccharide (LPS) in RAW264.7 murine macrophages, and on the release of beta-hexosaminidase induced by the calcium ionophore, A23187, in rat basophilic leukemia RBL-2H3 cells. In an in vivo experiment, in which mice were administered the curcumin-loaded lipid nanoemulsion of various particle sizes, the 100-nm curcumin lipid nanoemulsion showed the most prominent anti-inflammatory and anti-allergic effects, inhibiting 12-O-tetradecanoylphorbol-13-acetate-induced inflammatory ear edema and immunoglobulin E (IgE)-induced passive cutaneous anaphylactic (PCA) reaction. The effects of particle size on serum curcumin absorption were also assessed in mice, and the 100-nm lipid nanoemulsion showed the greatest absorption. The results from our study suggest that the physiological activities of curcumin lipid nanoemulsions differ depending on particle size. Our data indicate that the curcumin lipid nanoemulsion with a particle size of 100 nm has potential for use in enhancing the bioavailability and medical value of curcumin. FAU - Onodera, Takefumi AU - Onodera T AD - Laboratory of Food and Nutritional Sciences, Faculty of Nutrition, Kobe Gakuin University, Kobe, Hyogo 651-2180, Japan. FAU - Kuriyama, Isoko AU - Kuriyama I AD - Cooperative Research Center of Life Sciences, Kobe Gakuin University, Kobe, Hyogo 651-8586, Japan. FAU - Andoh, Tooru AU - Andoh T AD - Cooperative Research Center of Life Sciences, Kobe Gakuin University, Kobe, Hyogo 651-8586, Japan. FAU - Ichikawa, Hideki AU - Ichikawa H AD - Cooperative Research Center of Life Sciences, Kobe Gakuin University, Kobe, Hyogo 651-8586, Japan. FAU - Sakamoto, Yuka AU - Sakamoto Y AD - Laboratory of Food and Nutritional Sciences, Faculty of Nutrition, Kobe Gakuin University, Kobe, Hyogo 651-2180, Japan. FAU - Lee-Hiraiwa, Eibai AU - Lee-Hiraiwa E AD - Cooperative Research Center of Life Sciences, Kobe Gakuin University, Kobe, Hyogo 651-8586, Japan. FAU - Mizushina, Yoshiyuki AU - Mizushina Y AD - Cooperative Research Center of Life Sciences, Kobe Gakuin University, Kobe, Hyogo 651-8586, Japan. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20150416 PL - Greece TA - Int J Mol Med JT - International journal of molecular medicine JID - 9810955 RN - 0 (Anti-Inflammatory Agents) RN - 0 (Drug Carriers) RN - 0 (Emulsions) RN - 0 (Tumor Necrosis Factor-alpha) RN - IT942ZTH98 (Curcumin) RN - NI40JAQ945 (Tetradecanoylphorbol Acetate) SB - IM MH - Animals MH - *Anti-Inflammatory Agents/chemistry/pharmacology MH - Cell Line, Tumor MH - *Curcumin/chemistry/pharmacology MH - *Drug Carriers/chemistry/pharmacology MH - Edema/chemically induced/*drug therapy/metabolism/pathology MH - Emulsions MH - Macrophages/metabolism/pathology MH - Male MH - Mice MH - Mice, Inbred ICR MH - Nanoparticles/*chemistry MH - Particle Size MH - Rats MH - Tetradecanoylphorbol Acetate/toxicity MH - Tumor Necrosis Factor-alpha/metabolism EDAT- 2015/04/22 06:00 MHDA- 2016/01/26 06:00 CRDT- 2015/04/21 06:00 PHST- 2015/02/05 00:00 [received] PHST- 2015/04/09 00:00 [accepted] PHST- 2015/04/21 06:00 [entrez] PHST- 2015/04/22 06:00 [pubmed] PHST- 2016/01/26 06:00 [medline] AID - 10.3892/ijmm.2015.2186 [doi] PST - ppublish SO - Int J Mol Med. 2015 Jun;35(6):1720-8. doi: 10.3892/ijmm.2015.2186. Epub 2015 Apr 16.