Safety and Antioxidant Efficacy Profiles of Rutin-Loaded Ethosomes for Topical Application
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Topical application of dermocosmetics containing antioxidant and/or the intake of antioxidants through diet or supplementation are remarkable tools in an attempt to slow down some of the harmful effects of free radicals. Rutin is a strong antioxidant compound used in food and pharmaceutical industries. It was established that rutin presents a low skin permeation rate, a property that could be considered an inconvenience to the satisfactory action for a dermocosmetic formulation to perform its antioxidant activity onto the skin. Therefore, it is indispensable to improve its delivery, aiming at increasing its antioxidant capacity in deeper layers of the epidermis, being a possibility to associate the rutin to liposomal vesicles, such as ethosomes. Thus, in this work, the pre-clinical safety of rutin-loaded ethosomes was investigated employing an in vitro method, and the clinical safety and efficacy were also assessed. Rutin-loaded ethosomes were efficaciously obtained in a nanoscale dimension with a relevant bioactive compound loading (80.2%) and provided antioxidant in vitro activity in comparison with the blank sample. Pre-clinical and clinical safety assays assured the innocuous profile of the rutin-loaded ethosomes. The ethosomes containing the bioactive compound accomplished a more functional delivery system profile, since in the tape stripping assay, the deeper layers presented higher rutin amounts than the active delivered in its free state. However, the ex vivo antioxidant efficacy test detected no positive antioxidant activity from the rutin-loaded ethosomes, even though the in vitro assay demonstrated an affirmative antioxidant action.
KEY WORDSEthosomes Rutin Antioxidant activity Safety Tape stripping
The authors gratefully acknowledge the financial support of Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP; process number 2012/04435-9) and Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq).
- 8.Pietta PG. Flavonoids as antioxidants. J Nat Prod [Internet]. 2000 Jul [cited 2014 Mar 24];63(7):1035–42. Available from: http://www.ncbi.nlm.nih.gov/pubmed/10924197.
- 10.Oliveira CA, Peres DD, Rugno CM, Kojima M, Pinto CASDO, Consiglieri VO, et al. Functional photostability and cutaneous compatibility of bioactive UVA sun care products. J Photochem Photobiol B Biol [Internet]. 2015;148:154–9. Available from: http://linkinghub.elsevier.com/retrieve/pii/S101113441500130X.
- 11.Velasco MVR, Sarruf FD, Salgado-Santos IMN, Haroutiounian-Filho CA, Kaneko TM, Baby AR. Broad spectrum bioactive sunscreens. Int J Pharm [Internet]. 2008 Nov 3 [cited 2013 Feb 14];363(1–2):50–7. Available from: http://www.ncbi.nlm.nih.gov/pubmed/18662760.
- 12.Baby AR. Avaliação in vitro da permeabilidade cutânea da rutina em emulsões cosméticas.São Paulo. 2007. 144 f. Tese (Doutorado) – Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, São Paulo; 2007.Google Scholar
- 14.Dongare SU, Raut S, Bonde S, Tayshete S, Gurav K. Ethosomes as novel vesicular carriers for enhanced drug delivery. Citeseer. 2012;4(2):2100–18.Google Scholar
- 15.Park SN, Lee HJ, Gu HA. Enhanced skin delivery and characterization of rutin-loaded ethosomes. Korean J Chem Eng [Internet]. 2014 Jan 10 [cited 2014 Nov 26];31(3):485–9. Available from: http://link.springer.com/10.1007/s11814-013-0232-3.
- 22.Rakesh R, Anoop KR. Ethosomes for transdermal and topical drug delivery. Int J Pharm Pharm Sci. 2012;4(SUPPL.3):17–24.Google Scholar
- 24.De Oliveira CA, Peres DD, Graziola F, Chacra NAB, De Araújo GLB, Flórido AC, et al. Cutaneous biocompatible rutin-loaded gelatin-based nanoparticles increase the SPF of the association of UVA and UVB filters. Eur J Pharm Sci [Internet]. 2016;81:1–9. Available from: http://linkinghub.elsevier.com/retrieve/pii/S0928098715300245.
- 26.Wilson TD, Steck WF. Research Section. A modified HET ± CAM assay approach to the assessment of anti-irritant properties of plant extracts. 2000;38:867–872.Google Scholar
- 30.Filipe V, Hawe A, Jiskoot W. Critical evaluation of nanoparticle tracking analysis (NTA) by NanoSight for the measurement of nanoparticles and protein aggregates. Pharm Res [Internet]. 2010 May [cited 2014 Jul 14];27(5):796–810. Available from: http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=2852530&tool=pmcentrez&rendertype=abstract.
- 31.Bartenstein JE, Robertson J, Battaglia G, Briscoe WH. Stability of polymersomes prepared by size exclusion chromatography and extrusion. Colloids Surf A Physicochem Eng Asp [Internet]. 2016;506:739–46. Available from: https://doi.org/10.1016/j.colsurfa.2016.07.032.
- 36.Alonso C, Barba C, Rubio L, Scott S, Kilimnik A, Coderch L, et al. An ex vivo methodology to assess the lipid peroxidation in stratum corneum. J Photochem Photobiol B Biol [Internet]. 2009;97(2):71–6. Available from: https://doi.org/10.1016/j.jphotobiol.2009.08.003.
- 37.Lademann J, Jacobi U, Surber C, Weigmann H-J, Fluhr JW. The tape stripping procedure—evaluation of some critical parameters. Eur J Pharm Biopharm [Internet]. 2009 Jun [cited 2014 Oct 26];72(2):317–23. Available from: http://www.ncbi.nlm.nih.gov/pubmed/18775778.