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EXPLOITING THE VERSATILITY OF CHOLESTEROL IN NANOPARTICLES FORMULATION.

D Belletti1, A M Grabrucker2, F Pederzoli1

  • 1Department of Life Sciences, University of Modena and Reggio Emilia, Modena, Italy.

International Journal of Pharmaceutics
|July 16, 2016
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Summary

Cholesterol nanoparticles stabilized by Pluronic-F68 show improved stability and neuronal cell affinity at 45°C. These findings suggest potential applications for neurodegenerative diseases like Huntington's disease.

Keywords:
CholesterolPluronic-F68formulation conditionsnanoparticlesneuronal cells

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Area of Science:

  • Materials Science
  • Nanotechnology
  • Biocompatibility

Background:

  • Biocompatibility of nanocarrier formulation components is critical for safe development.
  • Cholesterol (Chol) is a common biocompatible component in liposomal systems.
  • Solid nanoparticles (NPs) offer alternative nanocarrier structures.

Purpose of the Study:

  • To formulate and optimize Cholesterol-based solid nanoparticles (NPs) using only surfactants.
  • To investigate the influence of surfactant type, concentration, and temperature on NP characteristics.
  • To evaluate the biocompatibility and neuronal cell affinity of the optimized NPs.

Main Methods:

  • Formulation of Chol-based NPs using various surfactants (Solutol HS 15, cholic acid sodium salt, poly vinyl alcohol, Pluronic-F68) at different concentrations (0.2%, 0.5%, 1% w/v).
  • Optimization of working temperature (room temperature and 45°C).
  • Characterization of NPs for size, zeta potential, composition, thermal behavior, and structure.

Main Results:

  • Pluronic-F68 at 0.5% w/v yielded structured NPs with a mean diameter < 400nm.
  • Working temperature significantly impacted surfactant aggregation and NP stability.
  • NPs formulated at 45°C (NP-Chol/0.5-45) exhibited a compact, stable matricial structure compared to room temperature formulations.
  • NP-Chol/0.5-45 showed low toxicity and affinity for neuronal cells.

Conclusions:

  • Pluronic-F68 (0.5% w/v) and a working temperature of 45°C are optimal for creating stable Cholesterol nanoparticles.
  • Temperature plays a crucial role in the architecture and stability of surfactant-stabilized Cholesterol NPs.
  • The developed NP-Chol/0.5-45 formulation demonstrates potential for treating diseases affecting neuronal plasticity and synaptic communication, such as Huntington's disease.