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Thermoresponsive Hydrogel Containing Extract for Topic and Transdermal Use: Development, Stability and Cytotoxicity Activity.

Authors:
João V D C Batista Ana Paula S Matos Adriana P Oliveria Eduardo Ricci Júnior Zaida M Freitas Catarina A Oliveira Helena K Toma Marcia A M Capella Leandro M Rocha Ulrike Weissenstein Stephan Baumgartner Carla Holandino

Pharmaceutics 2021 Dec 24;14(1). Epub 2021 Dec 24.

Laboratório Multidisciplinar em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro 21941-902, RJ, Brazil.

L. (), also known as European mistletoe, is a semi-parasitic plant that grows on different host trees. Our group recently demonstrated the antitumoral activity of ethanolic extracts in vitro, depending on the dose and the host tree, ssp from being the most active extract. The goal of this work focused on the development of a new topical formulation containing extracts, evaluation of in vitro toxicity and ex vivo skin permeation assays. The Poloxamer 407 hydrogel containing 5% of dry (VA_DEH) or aqueous (VA_AEH) extract presented dermal compatible pH and microbiological stability for 180 days. The hydrogels flow curve presented a non-linear relation, characteristic of non-Newtonian fluids, and the mean viscosity for the VA_DEH and VA_AEH was 372.5 ± 7.78 and 331.0 ± 2.83 Pa.s, respectively, being statistically different (Welch's test; < 0.01). Additionally, WST-1 in vitro assays revealed a dose-dependent toxicity for both formulations and VA_DEH presented a higher activity than the VA_AEH. The promising cytotoxic potential of VA_DEH lead to the ex vivo skin permeation assay with 2.73 ± 0.19 µg/cm of chlorogenic acid, which permeated at 8 h, showing a transdermal potential. These in vitro results support the idea that VA_DEH is a novel promising candidate for mistletoe therapy. Therefore, further in vivo and pre-clinical experiments should be performed to evaluate the safety and efficacy of this new dermic delivery system.

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http://dx.doi.org/10.3390/pharmaceutics14010037DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8780802PMC
December 2021

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