smartPearls - Novel physically stable amorphous delivery system for poorly soluble dermal actives

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Dermal Drug Delivery

Background:

• Poorly soluble actives in cosmetics and pharmaceuticals exhibit limited skin penetration, especially when insoluble in both water and oil phases.
• Crystalline actives have lower saturation solubility, reducing the concentration gradient and diffusive flux into the skin.
• The amorphous state enhances solubility and penetration but is inherently unstable for marketable products.

Purpose of the Study:

• To evaluate smartPearls, a novel technology for stabilizing amorphous actives, for dermal delivery.
• To compare the skin penetration of actives loaded in smartPearls against established dermal delivery systems.
• To assess the technical, regulatory, and marketing feasibility of smartPearls technology.

Main Methods:

• Loading poorly soluble actives into mesoporous silica particles (smartPearls) to preserve their amorphous state.
• Comparing skin penetration of smartPearls-loaded actives with amorphous microparticles, amorphous nanoparticles, and nanocrystals.
• Investigating the physical stability of smartPearls in semi-solid vehicles using sedimentation analysis.

Main Results:

• smartPearls demonstrated skin penetration performance equal to or better than current gold standards.
• Enhanced active solubility was attributed to the amorphous state and nanostructure within the micro-sized smartPearls.
• Viscoelastic repulsion effectively stabilized dense smartPearls in semi-solid formulations, preventing sedimentation.

Conclusions:

• smartPearls technology offers efficient long-term stabilization of amorphous actives for improved dermal delivery.
• The technology provides a viable alternative to nanoparticles, offering comparable efficacy with potential advantages.
• smartPearls represent a promising dermal delivery system for poorly soluble actives with significant market potential.