Preparation and evaluation of stealth Tashinone IIA-loaded solid lipid nanoparticles: Influence of Poloxamer 188 coating on phagocytic uptake

J Microencapsul. 2008 May;25(3):203-9. doi: 10.1080/02652040701852181.

Abstract

Stealth Tashinone IIA-loaded solid lipid nanoparticles (TA-SSLN) have been prepared by a nanoprecipitation/solvent diffusion method. Poloxamer 188 was used as a stealth agent. Nanoparticles were characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The profile of Tashinone IIA release from TA-SSLN was studied. Phagocytosis was evaluated by incubating TA-SSLN and non-stealth Tashinone IIA-loaded solid lipid nanoparticles (TA-NSLN) with murine macrophages. Human serum was added to evaluate opsonization of serum proteins. Rhodamine B was incorporated into nanoparticles as a fluorescent marker to observe and compare the phagocytic uptake of two kinds of nanopreticles. The results showed that TA-SSLN had an average diameter of (92.4 +/- 5.2) nm, zeta potential of (-20.4 +/- 1.3) mV, drug loading of (4.6 +/- 0.2)% and entrapment efficiency of (93.3 +/- 2.1)%. In vitro release experiment confirmed a sustained release of TA-SSLN and showed that the release of Tashinone IIA from TA-SSLN was in accordance with the Weibull equation. Phagocytosis studies showed significant differences between TA-SSLN and TA-NSLN and demonstrated that the Poloxamer 188 coating could decrease the macrophages uptake.

MeSH terms

  • Animals
  • Benzofurans / administration & dosage*
  • Benzofurans / chemistry
  • Drug Delivery Systems*
  • Drug Design
  • Humans
  • Lipids / chemistry*
  • Macrophages / metabolism
  • Mice
  • Nanoparticles / chemistry*
  • Particle Size
  • Phagocytosis
  • Plant Extracts / administration & dosage
  • Poloxamer / administration & dosage
  • Poloxamer / chemistry*
  • Polyethylene Glycols / chemistry
  • Rhodamines / chemistry
  • Rhodamines / metabolism
  • Scattering, Radiation

Substances

  • Benzofurans
  • Lipids
  • Plant Extracts
  • Rhodamines
  • tashinone IIA
  • Poloxamer
  • Polyethylene Glycols
  • rhodamine B