Title: Synthesis and characterization of nanostructured lipid-poloxamer organogels for enhanced skin local anesthesia
Author: 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
Is part of: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, v. 128, p. 270 - 278
Citation: 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; Synthesis and characterization of nanostructured lipid-poloxamer organogels for enhanced skin local anesthesia. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, v.128, p. 270-278, 2019
Abstract: 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 '' = similar to 15x). Additionally, the formulation with the highest concentrations of LAN and PL407 reduced the LDC flux from similar to 17 to 12 mu g.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.
Keywords: drug delivery; hydrogels; lidocaine;
Subjects: CIENCIAS_BIOLOGICAS; Farmacologia Bioquímica e Molecular;
Funding: This research work was supported by Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES), Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP 2014/14457-5, 2018/04036-3, 2018/02482-6), Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq 309207/2016-9, 402838/2016-5) and UFABC Multiuser Central Facilities (CEM-UFABC). We would also like to thank Dr. Viviane Aparecida Guilherme, Gustavo Henrique Rodrigues da Silva, Paulo Sergio Castilho Prete and Marcio Aparecido Paschoal for their kind assistance.