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辅酶 Q10 纳米结构脂质载体的研制、表征、分子对接及透皮递送研究——以三硬脂精和硬脂醇为载体

Development, characterization, molecular docking, and skin penetration of coenzyme Q10 nanostructured lipid carriers using tristearin and stearyl alcohol for dermal delivery.

机构信息

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Airlangga University, Surabaya, Indonesia.

Department of Pharmaceutics, Faculty of Pharmacy, University of Surabaya, Surabaya, Indonesia.

出版信息

J Basic Clin Physiol Pharmacol. 2021 Jun 25;32(4):517-525. doi: 10.1515/jbcpp-2020-0512.

Abstract

OBJECTIVES

This study aims to develop coenzyme Q10 nanostructured lipid carriers (NLCs) using tristearin and stearyl alcohol as well as isopropyl palmitate (IPP) as solid and liquid lipid respectively for the dermal delivery system.

METHODS

The coenzyme Q10 NLCs were optimized using tristearin, and stearyl alcohol in different concentrations and further characterized by dynamic light scattering (DLS) for particle size, polydispersity index (PDI), zeta potential, differential scanning calorimetry (DSC) and X-ray diffractometry for crystallinity behavior, Fourier transform infrared spectroscopy (FT-IR) for drug-lipid interaction, scanning electron microscopy (SEM) for particle shape, viscometer for viscosity, and pH meter for pH value. Furthermore, entrapment efficiency (EE), drug loading (DL), and skin penetration were also evaluated while molecular docking was conducted to examine the interaction between coenzyme Q10 and the lipids.

RESULTS

The coenzyme Q10 NLCs with tristearin-IPP and stearyl alcohol-IPP as lipid matrix had <1,000 nm particle size, <0.3 PDI, less negative than -30 mV zeta potential, about 41% crystallinity index, and about six as the pH value. Moreover, the EE, DL, viscosity, and skin penetration of the NLCs using tristearin were higher compared to stearyl alcohol, however, the skin penetration depths for both NLCs were not significantly different. Furthermore, the binding energy of coenzyme Q10-tristearin was lower compared to coenzyme Q10-stearyl alcohol. Both of them showed hydrophobic and van der Waals interaction.

CONCLUSIONS

The NLCs of coenzyme Q10 were formulated successfully using tristearin-IPP and stearyl alcohol-IPP for dermal delivery.

摘要

目的

本研究旨在开发使用三硬脂精和硬脂醇以及异十六烷作为固体和液体脂质的辅酶 Q10 纳米结构化脂质载体(NLCs),用于皮肤传递系统。

方法

使用三硬脂精和不同浓度的硬脂醇优化辅酶 Q10 NLCs,并通过动态光散射(DLS)测量粒径、多分散指数(PDI)、Zeta 电位、差示扫描量热法(DSC)和 X 射线衍射法(XRD)测量结晶行为、傅里叶变换红外光谱(FT-IR)测量药物-脂质相互作用、扫描电子显微镜(SEM)测量颗粒形状、粘度计测量粘度以及 pH 计测量 pH 值对其进行进一步表征。此外,还评估了包封效率(EE)、载药量(DL)和皮肤渗透,同时进行分子对接以检查辅酶 Q10 与脂质之间的相互作用。

结果

以三硬脂精-IPP 和硬脂醇-IPP 为脂质基质的辅酶 Q10 NLCs 的粒径<1000nm、PDI<0.3、Zeta 电位小于-30mV、结晶度指数约为 41%、pH 值约为 6。此外,与硬脂醇相比,使用三硬脂精的 NLCs 的 EE、DL、粘度和皮肤渗透较高,但两种 NLCs 的皮肤渗透深度没有显著差异。此外,辅酶 Q10-三硬脂精的结合能低于辅酶 Q10-硬脂醇。两者均显示出疏水和范德华相互作用。

结论

使用三硬脂精-IPP 和硬脂醇-IPP 成功制备了用于皮肤传递的辅酶 Q10 NLCs。

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