Synthesis, characterization, release kinetics and toxicity profile of drug-loaded starch nanoparticles

Int J Biol Macromol. 2015 Nov:81:718-29. doi: 10.1016/j.ijbiomac.2015.09.005. Epub 2015 Sep 7.

Abstract

The current research work focuses on the medical application of the cost-effective cross-linked starch nanoparticles, for the transdermal delivery using Diclofenac sodium (DS) as a model drug. The prepared DS-cross-linked starch nanoparticles were synthesized using nanoprecipitation technique at different concentrations of sodium tripolyphosphate (STPP) in the presence of Tween 80 as a surfactant. The resultant cross-linked starch nanoparticles loaded with DS were characterized using world-class facilities such as TEM, DLS, FT-IR, XRD, and DSc. The efficiency of DS loading was also evaluated via entrapment efficiency as well as in vitro release and histopathological study on rat skin. The optimum nanoparticles formulation selected by the JMP(®) software was the formula that composed of 5% maize starch, 57.7mg DS and 0.5% STPP and 0.4% Tween 80, with particle diameter of about 21.04nm, polydispersity index of 0.2 and zeta potential of -35.3mV. It is also worth noting that this selected formula shows an average entrapment efficiency of 95.01 and sustained DS release up to 6h. The histophathological studies using the best formula on rat skin advocate the use of designed transdermal DS loaded cross-linked starch nanoparticles as it is safe and non-irritant to rat skin. The overall results indicate that, the starch nanoparticles could be considered as a good carrier for DS drug regarding the enhancement in its controlled release and successful permeation, thus, offering a promising nanoparticulate system for the transdermal delivery non-steroidal anti-inflammatory drug (NSAID).

Keywords: Cross-linked starch nanoparticles; Drug Delivery; Histopathological study; In vitro release; Nanoprecipitation.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Calorimetry, Differential Scanning
  • Drug Carriers / chemistry*
  • Drug Compounding
  • Drug Delivery Systems
  • Drug Liberation
  • Kinetics
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Particle Size
  • Pharmaceutical Preparations / administration & dosage*
  • Rats
  • Skin / cytology
  • Skin / drug effects
  • Spectroscopy, Fourier Transform Infrared
  • Starch / chemistry*
  • X-Ray Diffraction

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Pharmaceutical Preparations
  • Starch