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

Author(s)

Vigato, Aryane Alves ^[1] ; Querobino, Samyr Machado ^[1] ; de Faria, Naially Cardoso ^[1] ; Pinheiro de Freitas, Andrea Carolina ^[2] ; Leonardi, Gislaine Ricci ^[2] ; de Paula, Eneida ^[3] ; Saia Cereda, Cintia Maria ^[4] ; Tofoli, Giovana Radomille ^[4] ; de Araujo, Daniele Ribeiro ^[1]

Affiliation

^[1] Fed Univ ABC, Human & Nat Sci Ctr, Av Estados 5001, Bloco A, Torre 3, Lab 503-3, BR-09021058 Santo Andre, SP - Brazil

^[2] Univ Estadual Campinas, Fac Pharmaceut Sci, Campinas, SP - Brazil

^[3] Univ Estadual Campinas, Dept Biochem, Campinas, SP - Brazil

^[4] Sao Leopoldo Mandic Fac, Sao Leopoldo Mandic Res Unit, Campinas, SP - Brazil

• Document type: Journal article
• Source: European Journal of Pharmaceutical Sciences; v. 128, p. 270-278, FEB 1 2019.
• Web of Science Citations: 4

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. (AU)

• FAPESP's process: 18/02482-6 - Preparation and characterization of nanostructured lipid organogels as skin-drug delivery systems
• Grantee: Naially Cardoso de Faria
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• FAPESP's process: 14/14457-5 - Lipid-based nanocarriers (SLN/NLC and remote-loading liposomes) used to improve the upload and potency of local anesthetics
• Grantee: Eneida de Paula
• Support Opportunities: Research Projects - Thematic Grants
• FAPESP's process: 18/04036-3 - Organogels LECITIN-POLOXAMER-BASED for skin delivery: development, ex vivo permeation profile and stratum corneum structural evaluation
• Grantee: Aryane Alves Vigato
• Support Opportunities: Scholarships in Brazil - Master