Enhanced bioavailability and efficiency of curcumin for the treatment of asthma by its formulation in solid lipid nanoparticles.
Enhanced bioavailability and efficiency of curcumin for the treatment of asthma by its formulation in solid lipid nanoparticles.
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通过将姜黄素制成固体脂质纳米颗粒，提高姜黄素治疗哮喘的生物利用度和效率
DOI：
10.2147/ijn.s30428
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发表时间：
2012
影响因子：
8
通讯作者：
Wang S
中科院分区：
文献类型：
--
作者：
Wang W;Zhu R;Xie Q;Li A;Xiao Y;Li K;Liu H;Cui D;Chen Y;Wang S
姜黄素已显示出相当大的药理活性，包括抗炎，但其生物利用度差和代谢快限制了其应用。本研究的目的是制备姜黄素固体脂质纳米颗粒（姜黄素slns），以提高其对卵清蛋白（OVA）诱导的过敏性哮喘大鼠模型的治疗效果。采用溶剂注射法制备姜黄素单核苷酸。研究了姜黄素sln的理化性质，并进行了体外释放实验。研究其在小鼠组织分布中的药代动力学，并在模型上评价其治疗效果。其平均粒径为190 nm， zeta电位值为- 20.7 mV，包封效率为75%。x射线衍射分析揭示了包膜姜黄素的无定形性质。姜黄素sln的释放表现为先爆发后缓释。血浆混悬液中姜黄素的浓度显著高于单独使用姜黄素的浓度。服用姜黄素sln后，所有组织中姜黄素浓度均升高，尤其是肺和肝。在哮喘动物模型中，与哮喘组和姜黄素治疗组相比，姜黄素- sln能有效抑制气道高反应性和炎症细胞浸润，并显著抑制支气管肺泡灌洗液中白细胞介素-4、白细胞介素-13等t -helper-2型细胞因子的表达。这些观察结果暗示姜黄素sln可能是哮喘治疗的有希望的候选者。
Curcumin has shown considerable pharmacological activity, including anti-inflammatory, but its poor bioavailability and rapid metabolization have limited its application. The purpose of the present study was to formulate curcumin-solid lipid nanoparticles (curcumin-SLNs) to improve its therapeutic efficacy in an ovalbumin (OVA)-induced allergic rat model of asthma. A solvent injection method was used to prepare the curcumin-SLNs. Physiochemical properties of curcumin-SLNs were characterized, and release experiments were performed in vitro. The pharmacokinetics in tissue distribution was studied in mice, and the therapeutic effect of the formulation was evaluated in the model. The prepared formulation showed an average size of 190 nm with a zeta potential value of −20.7 mV and 75% drug entrapment efficiency. X-ray diffraction analysis revealed the amorphous nature of the encapsulated curcumin. The release profile of curcumin-SLNs was an initial burst followed by sustained release. The curcumin concentrations in plasma suspension were significantly higher than those obtained with curcumin alone. Following administration of the curcumin-SLNs, all the tissue concentrations of curcumin increased, especially in lung and liver. In the animal model of asthma, curcumin-SLNs effectively suppressed airway hyperresponsiveness and inflammatory cell infiltration and also significantly inhibited the expression of T-helper-2-type cytokines, such as interleukin-4 and interleukin-13, in bronchoalveolar lavage fluid compared to the asthma group and curcumin-treated group. These observations implied that curcumin-SLNs could be a promising candidate for asthma therapy.