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Exploring the co-loading of lidocaine chemical forms in surfactant/phospholipid vesicles for improved skin delivery
Carla Caddeo1, Donatella Valenti1, Amparo Nácher2,3
1Department Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Cagliari, Italy.
Objectives:
The present study was aimed at targeting the skin to deliver lidocaine loaded in surfactant/phospholipid vesicles tailored for improved local delivery. The influence of different formulation parameters was explored to maximise drug efficacy.
Methods:
The vesicles were prepared using a mixture of soy lipids (Phospholipon 50) and a surfactant with penetration-enhancing properties (Oramix CG110, Labrasol, Labrafac PG or Labrafac CC), and loaded with lidocaine. The formulations were analysed in detail by cryo-TEM, SAXS, Turbiscan Lab, and tested in permeation experiments through new born pig skin, as a function of the chemical form and concentration of lidocaine (i.e. free base or salt, 12.5 or 25 mg/ml).
Key Findings:
Small, spherical vesicles with good entrapment efficiency and exceptional long-term stability were produced. The lamellar organisation was affected by either the surfactant or the lidocaine form used. Permeation studies highlighted that the co-incorporation of lidocaine base + hydrochloride allowed the achievement of a superior deposition in the skin layers, especially when surfactant vesicles were used, as their content was presumably saturated with the maximum amount of loadable anaesthetic.
Conclusions:
The proposed systems based on surfactant/phospholipid vesicles co-loaded with both lidocaine forms are an effective approach for improving its local delivery.
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