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用于肺部给药的载槲皮素棕榈油酯基纳米乳剂配方的优化

Optimization of Quercetin loaded Palm Oil Ester Based Nanoemulsion Formulation for Pulmonary Delivery.

作者信息

Arbain Noor Hafizah, Salim Norazlinaliza, Wui Wong Tin, Basri Mahiran, Rahman Mohd Basyaruddin Abdul

机构信息

Integrated Chemical Biophysics Research, Faculty of Science, Universiti Putra Malaysia.

Department of Chemistry, Faculty of Science, Universiti Putra Malaysia.

出版信息

J Oleo Sci. 2018 Aug 1;67(8):933-940. doi: 10.5650/jos.ess17253. Epub 2018 Jul 17.

Abstract

In this research, the palm oil ester (POE)- based nanoemulsion formulation containing quercetin for pulmonary delivery was developed. The nanoemulsion formulation was prepared by high energy emulsification method and then further optimized using D-optimal mixture design. The concentration effects of the mixture of POE:ricinoleic acid (RC), ratio 1:1 (1.50-4.50 wt.%), lecithin (1.50-2.50 wt.%), Tween 80 (0.50-1.00 wt.%), glycerol (1.50-3.00 wt.%), and water (88.0-94.9 wt.%) towards the droplet size were investigated. The results showed that the optimum formulation with 1.50 wt.% POE:RC, 1.50 wt.% lecithin, 1.50 wt.% Tween 80, 1.50 wt.% glycerol and 93.90 % water was obtained. The droplet size, polydispersity index (PDI) and zeta potential of the optimized formulation were 110.3 nm, 0.290 and -37.7 mV, respectively. The formulation also exhibited good stability against storage at 4℃ for 90 days. In vitro aerosols delivery evaluation showed that the aerosols output, aerosols rate and median mass aerodynamic diameter of the optimized nanoemulsion were 99.31%, 0.19 g/min and 4.25 µm, respectively. The characterization of physical properties and efficiency for aerosols delivery results suggest that POE- based nanoemulsion containing quercetin has the potential to be used for pulmonary delivery specifically for lung cancer treatment.

摘要

在本研究中,开发了一种用于肺部给药的含槲皮素的棕榈油酯(POE)基纳米乳剂配方。该纳米乳剂配方采用高能乳化法制备,然后使用D-最优混合设计进一步优化。研究了POE:蓖麻油酸(RC)混合物(比例1:1,1.50 - 4.50 wt.%)、卵磷脂(1.50 - 2.50 wt.%)、吐温80(0.50 - 1.00 wt.%)、甘油(1.50 - 3.00 wt.%)和水(88.0 - 94.9 wt.%)的浓度对液滴尺寸的影响。结果表明,获得了最佳配方,其中POE:RC为1.50 wt.%、卵磷脂为1.50 wt.%、吐温80为1.50 wt.%、甘油为1.50 wt.%,水为93.90%。优化配方的液滴尺寸、多分散指数(PDI)和zeta电位分别为110.3 nm、0.290和-37.7 mV。该配方在4℃储存90天也表现出良好的稳定性。体外气雾剂递送评估表明,优化后的纳米乳剂的气雾剂输出量、气雾剂速率和质量中值空气动力学直径分别为99.31%、0.19 g/min和4.25 µm。物理性质表征和气雾剂递送效率结果表明,含槲皮素的POE基纳米乳剂有潜力用于肺部给药,特别是用于肺癌治疗。

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