Ganoderma lucidum-derived polysaccharide enhances coix oil-based microemulsion on stability and lung cancer-targeted therapy

Drug Deliv. 2018 Nov;25(1):1802-1810. doi: 10.1080/10717544.2018.1516006.

Abstract

The aim of this study is to explore the influence of Ganoderma lucidum-derived polysaccharides (GLP) to coix oil-based microemulsion on pharmaceutical performance and anti-lung cancer treatment. GLP-integrated coix oil-based microemulsion (MEs(PS-GLP)) exhibited a clear spherical shape, small particle size, and good hydrodynamics similar to the coix oil-based microemulsion, but showed a lower zeta potential and a better stability. Fluorescence resonance energy transfer analysis presented that GLP was integrated with microemulsion as a single system. Notably, the average molecular distance between polysaccharide and microemulsion was approximately 1.7 nm. The half-maximal inhibitory concentration of MEs(PS-GLP) against A549 cells was about 119 μg/mL. In vivo imaging studies showed that introduction of GLP promoted the tumor-specific accumulation of microemulsion in comparison with controls. In vivo, antitumor results showed that MEs(PS-GLP) markedly inhibited the tumor growth of A549-bearing xenograft nude mice and obviously improve the serum immune index. Collectively, this study demonstrates the potential mechanism of spatial relation between polysaccharides and microemulsion and validates the significances of GLP on tumoral accumulation and antitumor efficacy.

Keywords: Ganoderma lucidum polysaccharides; anti-lung cancer therapy; fluorescence resonance energy transfer; multicomponent microemulsion; spatial structure characterization.

MeSH terms

  • A549 Cells
  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / therapeutic use*
  • Antineoplastic Agents, Phytogenic / administration & dosage*
  • Antineoplastic Agents, Phytogenic / chemistry*
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Coix / chemistry*
  • Drug Compounding
  • Drug Stability
  • Emulsions
  • Humans
  • Lung Neoplasms / drug therapy*
  • Mice
  • Mice, Inbred BALB C
  • Particle Size
  • Plant Oils / administration & dosage*
  • Plant Oils / chemistry*
  • Plant Oils / pharmacology
  • Polysaccharides / chemistry
  • Polysaccharides / pharmacology*
  • Reishi / chemistry*
  • Tissue Distribution
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Antineoplastic Agents, Phytogenic
  • Emulsions
  • Plant Oils
  • Polysaccharides

Grant support

This work was supported by the National Natural Science Foundation of China (81673606); the Key Medical Talent Project of Jiangsu Province (ZDRCA2016036); and the Key Projects of Jiangsu Provincial Administration of Traditional Chinese Medicine (ZD201509).