Burn injuries, trauma, and surgical procedures result in complex skin wounds that can lead to inflammation, infection, and scarring. Management of complex wounds remains a critical challenge for the medical community due to the lack of localized treatments that provide sustained drug release. Solid lipid nanoparticles (SLNs) are a promising platform for delivering lipophilic compounds topically to skin. Made entirely from ingredients generally regarded as safe (GRAS), the SLNs are biocompatible, stable, accept a wide range of therapeutics, and penetrate the epidermis. In this study, we synthesized sub-10 nm SLNs using the Phase Inversion Temperature (PIT) method. The SLNs are designed to melt at skin temperature (32�C) and thus release their payload in response to skin contact. A systematic Design of Experiments (DOE) approach investigated the role of synthesis parameters on SLN form and function. Particle size and polydispersity were measured as a function of dye solubility, phase inversion temperature, melting point, and latent heat of melting. The particle size distribution was largely invariant to these processing parameters, suggesting that SLNs may serve as a universal carrier for lipophilic therapeutic compounds. Inspection of ex vivo porcine skin samples further demonstrated the penetration of dyes across the entire viable epidermis. Also demonstrated was the delivery of an immunosuppressant drug, rapamycin, through approximately two-thirds of the porcine epidermis. For comparison, the control samples exhibited no penetration due to their spare solubility in water.Figure 1.  Schematic of solid lipid nanoparticle depicting the outer surfactant layer, inner lipid core, and entrained lipophilic compounds.

Sub-10 nm solid lipid nanoparticles for the topical delivery and thermally activated release of therapeutics

247th National Meeting (2014)

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