Optimized nonionic emulsifier for the efficient delivery of astaxanthin nanodispersions to retina: in vivo and ex vivo evaluations

Drug Deliv. 2019 Dec;26(1):1222-1234. doi: 10.1080/10717544.2019.1682718.


Astaxanthin (AST) is a naturally occurring carotenoid with potent anti-oxidative and anti-inflammatory potency against chronic diseases. In this study, we suspended AST in different nonionic emulsifiers to produce nanodispersions. The basic physicochemical properties of the produced AST nanodispersions were verified to select the optimized nonionic emulsifier. Among the tested emulsifiers, Polysorbate 20 produced the AST nanoemulsions with smaller particle diameters, narrower size distributions, and higher AST contents among these emulsifiers. The N-methyl-N-nitrosourea (MNU) administered mouse is a chemically induced retinal degeneration (RD) model with rapid progress rate. AST suspended in Polysorbate 20 was demonstrated to ameliorate the dramatic consequences of MNU on retina architectures and function in several different tests encompassing from electrophysiology to histology and molecular tests. Furthermore, the multi-electrodes array (MEA) was used to detect the firing activities of retinal ganglion cells within the inner retinal circuits. We found that AST nanodispersions could restrain the spontaneous firing response, enhance the light induced firing response, and preserve the basic configurations of visual signal pathway in degenerative retinas. The MEA assay provided an appropriate example to evaluate the potency of pharmacological compounds on retinal plasticity. In summary, emulsifier type affects the basic physicochemical characteristic of AST nanodispersions. Polysorbate 20 acts as an optimized nonionic emulsifier for the efficient delivery of AST nanodispersions to retina. AST nanodispersions can alleviate the photoreceptor loss and rectify the abnormities in visual signal transmission.

Keywords: Medicine delivery; nano-astaxanthin; neurodegenration; therapeutics.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / administration & dosage*
  • Anti-Inflammatory Agents / therapeutic use
  • Disease Models, Animal
  • Drug Carriers / chemistry*
  • Emulsifying Agents / chemistry*
  • Female
  • Male
  • Methylnitrosourea / pharmacology
  • Mice, Inbred C57BL
  • Nanoparticles / chemistry*
  • Photoreceptor Cells, Vertebrate / metabolism
  • Retina / drug effects*
  • Retina / metabolism
  • Retinal Degeneration / chemically induced
  • Retinal Degeneration / prevention & control
  • Xanthophylls / administration & dosage
  • Xanthophylls / therapeutic use


  • Anti-Inflammatory Agents
  • Drug Carriers
  • Emulsifying Agents
  • Xanthophylls
  • Methylnitrosourea
  • astaxanthine

Grant support

This study is supported in part by the National Natural Science Foundation of China [Grant No. 81600767]; Open foundation of National Key Laboratory for renal disease in Chinese PLA general hospital [Grant No. KF-01-114]