Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

Wei Huang,Zhigao Sun,Hua Wang,Houjiu Wu,Linhua Huang,Huating Dou

doi:10.1155/2017/2898342

Abstract

The objective of this manuscript was to investigate and optimise the potential of nanostructured lipid carriers (NLCs) as a carrier system for nobiletin (NOB), which was prepared by high-pressure homogenisation method. Additionally, this study was focused on the application of NOB-loaded NLC (NOB-NLC) in functional food. Response surface method with a three-level Box–Behnken design was validated through analysis of variance, and the robustness of the design was confirmed through the correspondence between the values measured in the experiments and the predicted ones. Properties of the prepared NOB-NLC, such as Z-average, polydispersity, entrapment efficiency, zeta potential, morphology, and crystallinity, were investigated. NOB-NLC exhibited a spherical shape with a diameter of 112.27 ± 5.33 nm, zeta potential of −35.1 ± 2.94 mV, a polydispersity index of 0.251 ± 0.058, and an EE of 81.06% ± 6.02%. Results from X-ray diffraction and differential scanning calorimetry of NOB-NLC reviewed that the NOB crystal might be converted to an amorphous state. Fourier transform infrared spectroscopic analysis demonstrated that chemical interaction was absent between the compound and lipid mixture in NOB-NLC.

Highlights

Nobiletin (5,6,7,8,3󸀠,4󸀠-hexametoxyflavone, NOB) is a citrus polymethoxylated flavone that possesses an extensive range of health benefits among others, including antioxidant activity, glucose regulation, and fat metabolism [1]
NOB-loaded nanostructured lipid carriers (NLCs) were successfully developed through a high-pressure homogenisation technique and optimised by seventeen-run, three-factor, three-level BBD
The optimised NOB-loaded NLC (NOB-NLC) manifested a size of 112.27 ± 5.33 nm with a polydispersity of 0.251 ± 0.058, an EE of 81.06 ± 6.02%, and zeta potential of −35.1 ± 2.94 mV

Summary

Introduction

Nobiletin (5,6,7,8,3󸀠,4󸀠-hexametoxyflavone, NOB) is a citrus polymethoxylated flavone that possesses an extensive range of health benefits among others, including antioxidant activity, glucose regulation, and fat metabolism [1]. It was previously reported that nobiletin could inhibit tumor angiogenesis by regulating Src, FAK, and STAT3 signalling through PXN in ER+ breast cancer cells [2] and showed its ameliorative effects toward ischemia–reperfusion injury by suppressing the function of Kupffer cells after liver transplantation in rats [3]. Nobiletin has been found to have positive effects of nobiletin on propofol-mediated antiinflammatory as well as having neuroprotective effect [4]. It may represent beneficial drug candidates for the treatment and prevention of Alzheimer’s and Parkinson’s disease because of its naturally occurring phytochemicals [5]. NOB exhibits poor water solubility because all hydroxyl groups in the structure are methoxylated, leading to low oral bioavailability, limiting the practical uses of NOB [6]

Objectives

Methods

Results

Conclusion