Formulation, Characterization, and Pharmacokinetic Studies of 6-Gingerol-Loaded Nanostructured Lipid Carriers

• Published in: AAPS PharmSciTech Vol. 19; no. 8; pp. 3661 - 3669
• Main Authors: Wei, Qiuyu, Yang, Qiuxuan, Wang, Qilong, Sun, Congyong, Zhu, Yuan, Niu, Ya, Yu, Jiangnan, Xu, Ximing
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.11.2018
• Subjects: Animals; Biochemistry; Biological Availability; Biomedical and Life Sciences; Biomedicine; Biotechnology; Catechols - chemistry; Catechols - pharmacokinetics; Drug Carriers - chemistry; Fatty Alcohols - chemistry; Fatty Alcohols - pharmacokinetics; Glycerides; Lipids - chemistry; Male; Nanostructures - chemistry; Pharmacology/Toxicology; Pharmacy; Rats; Rats, Sprague-Dawley; Research Article; Solubility; Theme: Lipid-Based Drug Delivery Strategies for Oral Drug Delivery; 6-Gingerol; sustained release; bioavailability; nanostructured lipid carriers
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-018-1165-2

In this study, an optimized nanostructured lipid carriers (NLCs) were developed and investigated for improving the solubility and oral availability of 6-Gingerol (6G), an active and abundant component of ginger with limited applications due to its poor water solubility plus oral biological availability. The NLCs consisted of a solid lipid (glyceryl monostearate), another liquid lipid (decanoyl/octanoyl-glycerides) and mixed surfactants (Tween 80 and Poloxamer 188), and was prepared by high pressure homogenization method. The optimal 6G-NLC formulation was evaluated through physical properties such as appearance, mean particle size, zeta potential, encapsulation efficiency, and in vitro drug release, alongside techniques viz. , transmission electron microscopy (TEM), differential scanning calorimetry (DSC), as well as powder X-ray diffraction (XRD). Pharmacokinetics were also evaluated in rats. The 6G-NLCs prepared with optimal formulation exhibited a homogenous spherical shape with mean particle size and zeta potential of 63.59 ± 5.54 nm and − 12.18 ± 1.06 mV. Encapsulation efficiency and drug loading were 76.71 ± 1.11 and 1.17 ± 0.35%, respectively. In vitro release profile of 6G from NLCs was sustained and fitted with Weibull equation. After oral administration of the 6G-NLCs, drug concentrations in serum, MRT, and AUC 0-t were significantly higher as compared with the free 6G suspension. All these results indicated that the developed NLC formulation could be effective and promising drug carriers to improve the water solubility of 6G while sustaining the drug release as well as prolonging in vivo acting time of the drug coupled with oral bioavailability enhancement.