Development and evaluation of nanoemulsion and microsuspension formulations of curcuminoids for lung delivery with a novel approach to understanding the aerosol performance of nanoparticles
Development and evaluation of nanoemulsion and microsuspension formulations of curcuminoids for lung delivery with a novel approach to understanding the aerosol performance of nanoparticles
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DOI：
10.1016/j.ijpharm.2018.12.042
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发表时间：
2019-02-25
影响因子：
5.8
通讯作者：
Assi, K. H.
中科院分区：
文献类型：
--
作者：
Al Ayoub, Yuosef;Gopalan, R. C.;Assi, K. H.
广泛的研究已经证明了姜黄素对各种疾病的潜在有效性，包括哮喘和癌症。然而，很少有研究在姜黄素制剂的制备中使用基于液体的载体。因此，目前的研究提出了使用纳米乳液和微悬浮液制剂来制备用于肺部递送的雾化姜黄素。此外，这项工作表达了一种新的方法来理解纳米颗粒的气溶胶性能相比，微悬浮制剂。还评估了制剂的遗传毒性。使用柠檬烯和油酸作为油相制备三种浓度（100、250和500 μ g/ml）的类姜黄素纳米乳液制剂，同时通过将类姜黄素颗粒悬浮在0.02%Tween 80的等渗溶液（盐水溶液）中制备微悬浮液溶液。对于1000 μ g/ml和100 μ g/ml，雾化微悬浮液制剂的平均细颗粒分数（FPF）和质量中值空气动力学直径（MMAD）分别为26%和7.1 μ m至40%和5.7 μ m。在雾化纳米乳剂的低和高药物浓度的比较中，用柠檬烯油制备的雾化纳米乳剂制剂的平均FPF和MMAD分别为50%和4.6 μ m至45%和5.6 μ m;而用油酸油制备的雾化纳米乳剂的FPF和MMAD分别为46%和4.9 μ m至44%和5.6 μ m。微悬浮液制剂的气雾剂性能是浓度依赖性的，而纳米乳液制剂似乎不依赖于姜黄素浓度。制剂的性能和遗传毒性结果表明，这些制剂适用于进一步的动物吸入研究。
Extensive research has demonstrated the potential effectiveness of curcumin against various diseases, including asthma and cancers. However, few studies have used liquid-based vehicles in the preparation of curcumin formulations. Therefore, the current study proposed the use of nanoemulsion and microsuspension formulations to prepare nebulised curcuminoid for lung delivery. Furthermore, this work expressed a new approach to understanding the aerosol performance of nanoparticles compared to microsuspension formulations. The genotoxicity of the formulations was also assessed. Curcuminoid nanoemulsion formulations were prepared in three concentrations (100, 250 and 500 mu g/ml) using limonene and oleic acid as oil phases, while microsuspension solutions were prepared by suspending curcuminoid particles in isotonic solution (saline solution) of 0.02% Tween 80. The average fine particle fraction (FPF) and mass median aerodynamic diameter (MMAD) of the nebulised microsuspension formulations ranged from 26% and 7.1 mu m to 40% and 5.7 mu m for 1000 mu g/ml and 100 mu g/ml respectively. In a comparison of the low and high drug concentrations of the nebulised nanoemulsion, the average FPF and MMAD of the nebulised nanoemulsion formulations prepared with limonene oil ranged from 50% and 4.6 mu m to 45% and 5.6 mu m respectively; whereas the FPF and MMAD of the nebulised nanoemulsion prepared with oleic acid oil ranged from 46% and 4.9 mu m to 44% and 5.6 mu m respectively. The aerosol performance of the microsuspension formulations were concentration dependent, while the nanoemulsion formulations did not appear to be dependent on the curcuminoids concentration. The performance and genotoxicity results of the formulations suggest the suitability of these preparations for further inhalation studies in animals.