Chitosan mediated solid lipid nanoparticles for enhanced liver delivery of zedoary turmeric oil in vivo

Int J Biol Macromol. 2020 Apr 15;149:108-115. doi: 10.1016/j.ijbiomac.2020.01.222. Epub 2020 Jan 24.

Abstract

Zedoary turmeric oil (ZTO) has a strong antitumor activity. However, its volatility, insolubility, low bioavailability, and difficulty of medication owing to oily liquid limit its clinical applications. Solid lipid nanoparticles can provide hydrophobic environment to dissolve hydrophobic drug and solidify the oily active composition to decrease the volatility and facilitate the medication. Chitosan has been widely used in pharmaceutics in recent years and coating with chitosan further enhances the internalization of particles by cells due to charge attract. Here, Chitosan (CS)-coated solid lipid nanoparticles (SLN) loaded with ZTO was prepared and characterized using dynamic laser scanner (DLS) and transmission electron microscope (TEM). The uptake and distribution of drug were evaluated in vitro and in vivo. The average sizes of ZTO-SLN and CS-ZTO-SLN were 134.3 ± 3.42 nm and 210.7 ± 4.59 nm, respectively. CS coating inverted the surface charge of particles from -8.93 ± 1.92 mV to +9.12 ± 2.03 mV. The liver accumulation of CS-ZTO-SLN was higher than ZTO-SLN (chitosan-uncoated particles) by analysis of tissue homogenate using HPLC, and the bioavailability of ZTO was also obviously improved. The results suggested that SLN coated with CS improved the features of ZTO formulation and efficiently deliver drug to the liver.

Keywords: Chitosan; Lipid nanoparticle; Liver targeting accumulation; Zedoary turmeric oil.

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic* / chemistry
  • Antineoplastic Agents, Phytogenic* / pharmacokinetics
  • Antineoplastic Agents, Phytogenic* / pharmacology
  • Chitosan / chemistry
  • Chitosan / pharmacokinetics
  • Chitosan / pharmacology
  • Curcuma / chemistry*
  • Drug Carriers* / chemistry
  • Drug Carriers* / pharmacokinetics
  • Drug Carriers* / pharmacology
  • Hep G2 Cells
  • Humans
  • Lipids / chemistry
  • Lipids / pharmacokinetics
  • Lipids / pharmacology
  • Liver / metabolism*
  • Male
  • Mice
  • Nanoparticles* / chemistry
  • Nanoparticles* / therapeutic use
  • Plant Oils* / chemistry
  • Plant Oils* / pharmacokinetics
  • Plant Oils* / pharmacology
  • Rhizome / chemistry*

Substances

  • Antineoplastic Agents, Phytogenic
  • Drug Carriers
  • Lipids
  • Plant Oils
  • Chitosan