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

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  • Theme: Lipid-Based Drug Delivery Strategies for Oral Drug Delivery
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Abstract

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 AUC0-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.

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Acknowledgements

The authors also thank the University Ethics Committee for the kind guidance in the animal experiments.

Funding

This work was supported by National Natural Science Foundation of China (81473172, 81503025, 81720108030 and 81773695), National “Twelfth Five-Year” Plan for Science & Technology Support (Grant 2013BAD16B07-1), Special Funds for 333 and 331 projects (BRA2013198), Industry-University-Research Institution Cooperation (JHB2012-37, GY2013055) in Jiangsu Province and Zhenjiang City, Program for Scientific Research Innovation Team in Colleges and Universities of Jiangsu Province (SJK-2015-4), and a project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions.

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Authors and Affiliations

  1. Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, No.301, Xuefu Road, Jingkou District, Zhenjiang City, 212013, Jiangsu Province, China

    Qiuyu Wei, Qiuxuan Yang, Qilong Wang, Congyong Sun, Yuan Zhu, Ya Niu, Jiangnan Yu & Ximing Xu

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  1. Qiuyu Wei
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  2. Qiuxuan Yang
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  3. Qilong Wang
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  4. Congyong Sun
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  7. Jiangnan Yu
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Correspondence to Jiangnan Yu or Ximing Xu.

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Healthy male Sprague-Dawley rats were obtained from Experimental Animal Center of Jiangsu University (Zhenjiang, China), and the in vivo experimental procedures all abided by the ethics and regulations of animal experiments approved by the Ethic Committee of Jiangsu University.

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The authors declare that they have no conflicts of interest.

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Guest Editor: Sanyog Jain

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Wei, Q., Yang, Q., Wang, Q. et al. Formulation, Characterization, and Pharmacokinetic Studies of 6-Gingerol-Loaded Nanostructured Lipid Carriers. AAPS PharmSciTech 19, 3661–3669 (2018). https://doi.org/10.1208/s12249-018-1165-2

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