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Published on: February 28, 2019
Lipidic spherulites: formulation optimisation by paired optical and cryoelectron microscopy
Sylvie Crauste-Manciet1, Eric Larquet, Karel Khawand
1Université Paris-Descartes - Paris Cité Sorbonne, Faculté des sciences pharmaceutiques et biologiques, Unité de Pharmacologie Chimique et Génétique et d'Imagerie, Paris, France.
Summary
This study optimized spherulite formation, finding that excipient resting and shearing stress are key. This novel process yields smaller spherulites with enhanced encapsulation of hydrophobic compounds like fisetin.
Area of Science:
- Materials Science
- Nanotechnology
- Biotechnology
Background:
- Spherulites are nanoscale structures with potential applications in drug delivery.
- Previous methods for spherulite obtention were not fully optimized.
- Understanding the formation process is crucial for controlling size and properties.
Purpose of the Study:
- To optimize the formulation, resting, and hydration steps for spherulite production.
- To compare green-based and organic-based processes for spherulite formation.
- To characterize the size of newly formed spherulites and their encapsulation efficiency.
Main Methods:
- Optical and cryoelectron microscopy were employed to assess spherulite formation.
- Excipient resting and hydration phases were systematically varied.
- Shearing stress was applied to hydrated excipients.
- Encapsulation of a hydrophobic compound (fisetin) was evaluated.
Main Results:
- Spherulite formation requires a prior resting phase for excipients and shearing stress on hydrated excipients.
- A new formulation produced spherulites in the 100-200 nm range, smaller than previously reported.
- The optimized process significantly increased the encapsulation of the hydrophobic compound fisetin compared to liposomal encapsulation.
Conclusions:
- The optimized laboratory-scale process enables efficient production of small spherulites.
- These spherulites offer superior encapsulation of hydrophobic compounds, showing promise for drug delivery applications.
- The findings pave the way for integrating these advanced spherulites into various prospective studies.
