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Formulation and evaluation of gemcitabine-loaded solid lipid nanoparticles.

P T Nandini1, R C Doijad, H N Shivakumar

  • 1KLEU College of Pharmacy , Belgaum, Karnataka , India and.

Drug Delivery
|November 29, 2013
PubMed
Summary

Gemcitabine-loaded solid lipid nanoparticles (SLNs) demonstrate effective liver and spleen targeting. These nanoparticles show good stability and controlled drug release, indicating potential for improved cancer therapy.

Keywords:
Entrapment efficiencygemcitabinein-vivo tissue distributionsolid lipid nanoparticlesstearic acid

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Area of Science:

  • Nanotechnology
  • Pharmaceutics
  • Drug Delivery

Background:

  • Solid lipid nanoparticles (SLNs) offer a promising platform for drug delivery.
  • Gemcitabine is a widely used chemotherapeutic agent with limitations in delivery and targeting.

Purpose of the Study:

  • To develop and characterize gemcitabine-loaded solid lipid nanoparticles (SLNs).
  • To evaluate the in vitro drug release, in vivo tissue distribution, and stability of the optimized SLN formulation.

Main Methods:

  • SLNs were prepared using a double emulsification technique with stearic acid, soy lecithin, and sodium taurocholate.
  • Characterization included particle size, surface morphology (SEM), particle yield, entrapment efficiency, and zeta potential.
  • In vitro release studies were conducted in PBS (pH 7.4), followed by in vivo tissue distribution and stability assessments.

Main Results:

  • The optimized formulation (F6) achieved an entrapment efficiency of 72.42% with satisfactory in vitro release.
  • In vivo studies revealed preferential drug targeting to the liver, followed by spleen, lungs, kidneys, and heart.
  • Stability studies indicated no significant change in particle size and a slight decrease in entrapment efficiency over three months at 25 ± 2 °C/60 ± 5% RH.

Conclusions:

  • Gemcitabine-loaded SLNs prepared via double emulsification are stable and exhibit favorable characteristics for drug delivery.
  • The developed SLNs demonstrate significant potential for targeted delivery of gemcitabine, particularly to the liver and spleen.
  • This formulation holds promise for enhancing the efficacy of gemcitabine-based cancer chemotherapy.