Influence of particle size on the in vitro and in vivo anti-inflammatory and anti-allergic activities of a curcumin lipid nanoemulsion
Influence of particle size on the in vitro and in vivo anti-inflammatory and anti-allergic activities of a curcumin lipid nanoemulsion
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DOI：
10.3892/ijmm.2015.2186
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发表时间：
2015-06-01
影响因子：
5.4
通讯作者：
Mizushina, Yoshiyuki
中科院分区：
文献类型：
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作者：
Onodera, Takefumi;Kuriyama, Isoko;Mizushina, Yoshiyuki
多酚化合物姜黄素是姜黄的天然黄色色素成分。它发挥各种生物学作用，如抗炎作用，我们以前已经证明姜黄素是DNA聚合酶的特异性抑制剂。姜黄素的特点是生物利用度差，因为它是水不溶性的，吸收差，全身消除。为了提高姜黄素的生物利用度，在这项研究中，我们生产了不同粒径（50，100和200 nm）的姜黄素负载的脂质纳米乳剂。采用改进的薄膜水化-超声法制备姜黄素脂质纳米乳。为了确定表现出最强生理活性的最佳粒径，我们研究了所获得的纳米乳剂对炎症和过敏活性的抑制作用。在体外细胞培养实验中，100 nm姜黄素脂质纳米乳剂对RAW 264.7小鼠巨噬细胞中脂多糖（LPS）诱导的肿瘤坏死因子-α（TNF-α）的产生以及对大鼠嗜碱性白血病RBL-2 H3细胞中钙离子载体A23187诱导的β-氨基己糖苷酶的释放显示出最显著的抑制作用。在体内实验中，其中小鼠被给予各种粒度的姜黄素负载的脂质纳米乳剂，100-nm姜黄素脂质纳米乳剂显示出最突出的抗炎和抗过敏作用，抑制12-O-十四酰基佛波醇-13-乙酸酯诱导的炎性耳水肿和免疫球蛋白E（IgE）诱导的被动皮肤过敏（PCA）反应。还在小鼠中评估了粒径对血清姜黄素吸收的影响，并且100 nm脂质纳米乳剂显示出最大吸收。我们的研究结果表明，姜黄素脂质纳米乳剂的生理活性取决于粒径。我们的数据表明，粒径为100 nm的姜黄素脂质纳米乳具有提高姜黄素生物利用度和药用价值的潜力。
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.. 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.