Physico-Chemical Characterization and Biopharmaceutical Evaluation of Lipid-Poloxamer-Based Organogels for Curcumin Skin Delivery

Author(s):Show less -

Vigato, Aryane Alves ^[1] ; Querobino, Samyr Machado ^[2] ; de Faria, Naially Cardoso ^[1] ; Bolela Bovo Candido, Ana Carolina ^[3] ; Magalhaes, Lizandra Guidi ^[3] ; Saia Cereda, Cintia Maria ^[4] ; Tofoli, Giovana Radomille ^[4] ; Ramos Campos, Estefania Vangelie ^{[1, 5]} ; Machado, Ian Pompermayer ^[6] ; Fraceto, Leonardo Fernandes ^[5] ; de Sairre, Mirela Ines ^[1] ; de Araujo, Daniele Ribeiro ^[1]

Affiliation

^[1] ABC Fed Univ, Human & Nat Sci Ctr, Santo Andre - Brazil

^[2] Univ Estado Minas Gerais, Dept Biomed Sci, Passos - Brazil

^[3] Univ Franca, Ctr Res Sci & Technol, Res Grp Nat Prod, Franca - Brazil

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

^[5] State Univ Julio de Mesquita Filho, Dept Environm Engn, Sorocaba - Brazil

^[6] Univ Sao Paulo, Dept Fundamental Chem, Inst Chem, Sao Paulo - Brazil

• Document type: Journal article
• Source: FRONTIERS IN PHARMACOLOGY; v. 10, SEP 12 2019.
• Web of Science Citations: 0

Abstract

Organogels (ORGs) are semi-solid materials, in which an organic phase is immobilized by a three-dimensional network composed of self-organized system, forming the aqueous phase. In this context, lipid-Pluronics (PLs) ORGs form a two-phase system which can be effectively used as skin delivery systems, favoring their permeation across the skin. In this study, we presented the development of ORG skin drug-delivery systems for curcumin (CUR), a liposoluble phenolic pigment extracted from the turmeric rhizome. In special, we designed the formulation compositions in order to carry high amounts of CUR soluble in oleic acid (OA), as organic phase, entrapped into an aqueous phase composed of micellar PL-based hydrogels by associating two polymers with different hydrophilic-lipophilic balances, Pluronic F-127 (PL F-127), and Pluronic L-81 (PL L-81), to enhance the permeation across the skin. Results revealed that the incorporation of PL L-81 favored the CUR incorporation into micelle-micelle interface. CUR insertion into OA-PL F-127/L-81 reduced both G'/G `' relationship (similar to 16 x) and viscosity values (eta{*} similar to 54 mPa.s, at 32.5 degrees C), disturbing the ORG network structural organization. In vitro permeation assays through Strat-M (R) skin-model membranes showed that higher CUR-permeated amounts were obtained for OA-PL F-127/L-81 (4.83 mu g.cm(-2)) compared to OA-PL F-127 (3.51 mu g.cm(-2)) and OA (2.25 mu g.cm(-2)) or hydrogels (similar to 1.2 mu g.cm(-2)), p < 0.001). Additionally, ORG formulations presented low cytotoxic effects and evoked pronounced antileishmanial activity (IC50 < 1.25 mu g.ml(-1)), suggesting their potential use as skin delivery systems against Leishmania amazonensis. Results from this study pointed out OA-PL-based ORGs as promising new formulations for possible CUR topical administration. (AU)

• 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
• FAPESP's process: 16/24456-1 - Monoketo enone curcuminoids the treatment of schistosomiasis: an pre-clinical evaluation of schistosomicidal activity
• Grantee: Lizandra Guidi Magalhães
• Support Opportunities: Regular Research Grants
• FAPESP's process: 16/18045-9 - Study of Hantzsch multicomponent reaction for the synthesis of new dipeptidyl peptidase 4 (DPP-4) inhibitors for treatment of type II Diabetes
• Grantee: Mirela Inês de Sairre
• Support Opportunities: Regular Research Grants
• 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