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dc.contributor.author
Caimi, Ayelen Tatiana
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dc.contributor.author
Ramirez, Cecilia
dc.contributor.author
Perez, Ana Paula
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dc.contributor.author
Romero, Eder Lilia
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dc.contributor.author
Morilla, María José
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dc.date.available
2023-07-31T13:24:51Z
dc.date.issued
2022-11
dc.identifier.citation
Caimi, Ayelen Tatiana; Ramirez, Cecilia; Perez, Ana Paula; Romero, Eder Lilia; Morilla, María José; In vitro anti-melanoma activity of imiquimod in ultradeformable nanovesicles; Taylor & Francis; Drug Development and Industrial Pharmacy; 48; 11; 11-2022; 657-666
dc.identifier.issn
0363-9045
dc.identifier.uri
http://hdl.handle.net/11336/206121
dc.description.abstract
Background: The wide spectrum of antitumoral mechanisms of imiquimod (IMQ), made it a good candidate for topical therapy of melanoma. However, physicochemical properties make IMQ formulation a difficult task. Solubility and skin penetration of IMQ are increased when loaded into ultradeformable nanovesicles. Objective: Survey the in vitro anti-melanoma activity of IMQ loaded into two types of ultradeformable nanovesicles: archaeosomes (UDA-IMQ) (containing sn-2,3 ether-linked phytanyl saturated archaeolipids extracted from Halorubrum tebenquichense) and liposomes lacking archaeolipids (UDL-IMQ). Methods: We prepared and structurally characterized UDA-IMQ and UDL-IMQ. Cytotoxicity was determined on human melanoma cells (SK-Mel-28) and keratinocytes (HaCaT cells) by MTT assay and LDH release. The cellular uptake was determined by flow cytometry. Apoptosis/necrosis induction was determined by fluorescence microscopy after double staining with YO-PRO-1® and propidium iodide. Results: Neither IMQ nor IMQ-nanovesicles reduced the viability of HaCaT cells; but UDL-IMQ (371 nm, −24 mV ζ potential, 31 µg IMQ/mg lipids) and UDA-IMQ (216 nm, −32 mV ζ potential, 61 µg IMQ/mg lipids) showed time and concentration-dependent cytotoxicity on SK-Mel-28 that resulted between 4 and 33 folds higher than free IMQ, respectively. While both UDA-IMQ and UDL-IMQ retained 60% of IMQ against dilution, UDA-IMQ uptaken by SK-Mel-28 cells was nine-fold higher than UDL-IMQ. UDL-IMQ induced early apoptosis, but UDA-IMQ induced both apoptosis and necrosis on SK-Mel-28 cells. Conclusions: UDA-IMQ was innocuous to keratinocytes but was highly uptaken and induced apoptosis and necrosis on melanoma cells, being a candidate for future investigations as adjuvant topical anti-melanoma therapy.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Taylor & Francis
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dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
APOPTOSIS
dc.subject
ARCHAEOLIPIDS
dc.subject
INTRACELLULAR DELIVERY
dc.subject
SK-MEL-28 CELLS
dc.subject
TOPICAL
dc.subject.classification
Otras Nanotecnología
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dc.subject.classification
Nanotecnología
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dc.subject.classification
INGENIERÍAS Y TECNOLOGÍAS
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dc.title
In vitro anti-melanoma activity of imiquimod in ultradeformable nanovesicles
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2023-07-28T17:33:46Z
dc.journal.volume
48
dc.journal.number
11
dc.journal.pagination
657-666
dc.journal.pais
Estados Unidos
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dc.description.fil
Fil: Caimi, Ayelen Tatiana. Universidad Nacional de Quilmes; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Ramirez, Cecilia. Universidad Nacional de Quilmes; Argentina
dc.description.fil
Fil: Perez, Ana Paula. Universidad Nacional de Quilmes; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Romero, Eder Lilia. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes; Argentina
dc.description.fil
Fil: Morilla, María José. Universidad Nacional de Quilmes; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.journal.title
Drug Development and Industrial Pharmacy
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1080/03639045.2022.2153861
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