Abstract
Hypericin (Hy) is a potent lipid-soluble photosensitizerhaving broad pharmacological spectrum. Nevertheless, its poor water solubilityleads to its aggregation in the biological systems that consequently diminishesits photodynamic activity (PDA) and its therapeutic applications. Therefore,this study presents novel hydro-solving bilayer microneedle (MN) arraysincorporating Hy-loaded lipid nanocapsules (LNC) to prevent drug aggregation,enhance its delivery and local PDA. The Hy-LNC were prepared by phase inversiontechnique and showed homogenous particle size distribution and highencapsulation efficiency (88.42 ± 0.11%). The bilayer MNs consist of a hydrogelcross-linked, drug-free base plate and a Hy-loaded MN for a one-stepapplication. The dissolving MNs were fabricated from aqueous blends of 10% w/wpolyvinyl alcohol and 30% w/w polyvinyl pyrrolidone by casting and pressure.The MN arrays were characterized for mechanical strength and insertion depth.The bilayer arrays showed good mechanical strength under a compression force of32 N, with a height reduction of 10.14 ± 0.55% and sufficient insertion depthin both Parafilm M® and the excised porcine skin. After 2h of application toexcised pig skin, the MNs were completely dissolved ensuring the delivery ofits payload and the base plate was removed intact free from MN residuals. Inconclusion, the incorporation of Hy-LNC into this novel bilayer MNs overcomeits aggregation and ensured the complete insertion of the drug-loaded MNs. ThisLNC-MN system is promising for improving Hy local availability and thusenhancing its photodynamic application.
Highlights
A phenanthroperylenequinone derivative, is a naturally-occurring photosensitizer extracted from Hypericum perforatum
The present study aims at overcoming the aforementioned limitations by encapsulating the Hy inside lipid nanocapsules (LNC), further incorporation into bilayer dissolving MNs
Blank and Hy-loaded LNCs with LabrafacTM oily core and surfactant shell of Solutol HS 15 and Lipoid S 100 were prepared by the phase inversion method and
Summary
Hypericin (Hy) is a potent lipid soluble photosensitizer having broad pharmacological spectrum. Its poor water solubility leads to its aggregation in biological systems that diminishes its photodynamic activity (PDA) and its therapeutic applications. This study presents novel hydro-solving bilayer microneedle (MN) arrays incorporating Hy-loaded lipid nanocapsules (LNC) to prevent drug aggregation, enhance its delivery and local PDA. The bilayer MNs consist of a hydrogel cross-linked, drug free base plate and a Hy-loaded MN for onestep application. The bilayer arrays showed good mechanical strength under a compression force of 32 N, with a height reduction of 10.14 ± 0.55% and sufficient insertion depth in both Parafilm M® and excised porcine skin. After 2h of application to excised pig skin, the MNs were completely dissolved ensuring the delivery of their payload and the base plate was removed intact, free from MN residuals
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