Details

Autor(en) / Beteiligte

• Vigato, Aryane Alves
• Querobino, Samyr Machado
• de Faria, Naially Cardoso
• de Freitas, Andréa Carolina Pinheiro
• Leonardi, Gislaine Ricci
• de Paula, Eneida
• Cereda, Cíntia Maria Saia
• Tófoli, Giovana Radomille
• de Araujo, Daniele Ribeiro

Titel

Synthesis and characterization of nanostructured lipid-poloxamer organogels for enhanced skin local anesthesia

Ist Teil von

• European journal of pharmaceutical sciences, 2019-02, Vol.128, p.270-278

Ort / Verlag

Netherlands: Elsevier B.V

Erscheinungsjahr

2019

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• The aim of this study was to synthesize a novel drug delivery system using organogels (ORGs) and characterize its physicochemical properties, in vitro and ex vivo permeation abilities, cytotoxicity and in vivo local anesthetic effects. The ORG formulations contained a mixture of oleic acid-lanolin (OA-LAN), poloxamer (PL407), and the commonly used local anesthetic lidocaine (LDC). The main focus was to evaluate the impact of LAN and PL407 concentrations on the ORG structural features and their biopharmaceutical performance. Results revealed that LDC, OA, and LAN incorporation separately shifted the systems transitions phase temperatures and modified the elastic/viscous moduli relationships (G′/G″ = ~15×). Additionally, the formulation with the highest concentrations of LAN and PL407 reduced the LDC flux from ~17 to 12 μg·cm−2·h−1 and the permeability coefficients from 1.2 to 0.62 cm·h−1 through ex vivo skin. In vivo pharmacological evaluation showed that the ORG-based drug delivery system presented low cytotoxicity, increased and prolonged the local anesthetic effects compared to commercial alternatives. The data from this study indicate that ORG represent a promising new approach to effectively enhance the topical administration of local anesthetics. [Display omitted]