Effect of nanoemulsion modification with chitosan and sodium alginate on the topical delivery and efficacy of the cytotoxic agent piplartine in 2D and 3D skin cancer models
Autor: | Daniela V. Giacone, Luciana B. Lopes, Julia Sapienza Passos, Daniel A.G. Miranda, Erica Aparecida de Oliveira, Vanessa Franco Carvalho Dartora, Letícia V. Costa-Lotufo, Jenyffer Kelly Rocha De Matos, Silvya Stuchi Maria-Engler, Edilberto R. Silveira |
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Rok vydání: | 2020 |
Předmět: |
Drug
Skin Neoplasms Alginates media_common.quotation_subject 02 engineering and technology Pharmacology FARMACOLOGIA Biochemistry Chitosan 03 medical and health sciences chemistry.chemical_compound Structural Biology medicine Humans Cytotoxicity Melanoma Molecular Biology Piperidones Piperlongumine Cell Proliferation 030304 developmental biology media_common 0303 health sciences Cytotoxins General Medicine 021001 nanoscience & nanotechnology medicine.disease Oleic acid chemistry Melanocytes Nanoparticles Emulsions Nanocarriers Skin cancer 0210 nano-technology |
Zdroj: | Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual) Universidade de São Paulo (USP) instacron:USP |
ISSN: | 0141-8130 |
Popis: | Due to the limited options for topical management of skin cancer, this study aimed at developing and evaluating nanoemulsions (NE) for topical delivery of the cytotoxic agent piplartine (piperlongumine). NEs were modified with chitosan or sodium alginate, and the effects on the physicochemical properties, piplartine delivery and formulation efficacy were evaluated. The nanoemulsion droplets displayed similar size (96–112 nm), but opposite charge; the polysaccharides improved piplartine penetration into and across the skin (1.3–1.9-fold) in a similar manner, increasing the ratio “drug in the skin/receptor phase” by 1.4–1.5-fold compared to the plain NE and highlighting their relevance for cutaneous localization. Oleic acid addition to the chitosan-containing NE further increased drug penetration (~1.9–2.0-fold), as did increases in drug content from 0.5 to 1%. The cytotoxicity of piplartine was ~2.8-fold higher when the drug was incorporated in the chitosan-containing NE compared to its solution (IC50 = 14.6 μM) against melanoma cells. The effects of this nanocarrier on 3D melanoma tissues were concentration-related; at 1%, piplartine elicited marked epidermis destruction. These results support the potential applicability of the chitosan-modified nanoemulsion containing piplartine as a new strategy for local management of skin cancer. |
Databáze: | OpenAIRE |
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