Polyvinyl alcohol-based electrospun matrix as a delivery system for nanoemulsion containing chalcone against Leishmania (Leishmania) amazonensis
[Display omitted] •Nanotechnological strategies increase cytotoxic activity of chalcone in vitro.•Nanostructures system to improve leishmanicidal toxicity against L. amazonensis.•Two nanotechnology methods associated for treatment of cutaneous leishmaniasis.•PVA matrix associated with chalcone'...
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creator | Coelho, Daniela Veleirinho, Beatriz Mazzarino, Letícia Alberti, Thaís Buzanello, Elizandra Oliveira, Regina Eva Yunes, Rosendo Augusto Moraes, Milene Steindel, Mário Maraschin, Marcelo |
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•Nanotechnological strategies increase cytotoxic activity of chalcone in vitro.•Nanostructures system to improve leishmanicidal toxicity against L. amazonensis.•Two nanotechnology methods associated for treatment of cutaneous leishmaniasis.•PVA matrix associated with chalcone's nanoemulsion for leishmaniasis treatment.
Cutaneous leishmaniasis is a worldwide public health problem. Conventional therapies, in addition to the high cost, have many adverse effects and cases of parasite’s resistance. Chalcones are secondary metabolites precursors in the flavonoid pathway and can be obtained naturally, but with low yield from plant raw material. Thus, the use of synthetic chalcones has been a promising strategy for the development of molecules with leishmanicidal activity. Thus, this work aimed to develop a controlled release system of two synthetic chalcone (trans-chalcones and 3'-(trifluormethyl)-chalcone) using polyvinyl alcohol nanofibers (PVA) as scaffold. The association of chalcones to the nanofibers was made by nanoemulsions (NE) thereof, i.e., a colloidal system on a nanometric scale, which allows compounds with opposite polarities to remain miscible and stable throughout their manipulation. Chalcone nanoemulsions were developed using the spontaneous emulsification technique. The NE were characterized regarding their particle size, polydispersion index (PDI), and zeta potential. The results showed NE with spherical shape, absolute values of zeta potential were higher than 30 mV and homogeneous distribution pattern (PDI < 0.3). Dynamics light scattering (DLS) analysis showed similar hydrodynamic rays, i.e., 180 nm (trans-chalcone NE) and 178 nm (NE containing 3′-(trifluormethyl)-chalcone, in addition to presenting encapsulation efficiency values close to 100 %. Subsequently, the NE were added to a polymeric solution of polyvinyl alcohol (PVA) and processed via the electrospinning technique affording a PVA matrix (15 %, w/v) nanofiber containing the chalcones NE at 1 mg.mL−1. In a follow-up experiment, the skin permeation assay of the PVA matrix-chalcone NE was performed in vitro using Franz type diffusion cells and porcine ear as biological model of study. The results showed that the treatments with the nanofibers containing the chalcone NE were retained mainly in the stratum corneum, while the NE suspensions containing chalcone were retained in the epidermis and dermis. This result is thought to be relevant, since parasites are located m |
doi_str_mv | 10.1016/j.colsurfb.2020.111390 |
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•Nanotechnological strategies increase cytotoxic activity of chalcone in vitro.•Nanostructures system to improve leishmanicidal toxicity against L. amazonensis.•Two nanotechnology methods associated for treatment of cutaneous leishmaniasis.•PVA matrix associated with chalcone's nanoemulsion for leishmaniasis treatment.
Cutaneous leishmaniasis is a worldwide public health problem. Conventional therapies, in addition to the high cost, have many adverse effects and cases of parasite’s resistance. Chalcones are secondary metabolites precursors in the flavonoid pathway and can be obtained naturally, but with low yield from plant raw material. Thus, the use of synthetic chalcones has been a promising strategy for the development of molecules with leishmanicidal activity. Thus, this work aimed to develop a controlled release system of two synthetic chalcone (trans-chalcones and 3'-(trifluormethyl)-chalcone) using polyvinyl alcohol nanofibers (PVA) as scaffold. The association of chalcones to the nanofibers was made by nanoemulsions (NE) thereof, i.e., a colloidal system on a nanometric scale, which allows compounds with opposite polarities to remain miscible and stable throughout their manipulation. Chalcone nanoemulsions were developed using the spontaneous emulsification technique. The NE were characterized regarding their particle size, polydispersion index (PDI), and zeta potential. The results showed NE with spherical shape, absolute values of zeta potential were higher than 30 mV and homogeneous distribution pattern (PDI < 0.3). Dynamics light scattering (DLS) analysis showed similar hydrodynamic rays, i.e., 180 nm (trans-chalcone NE) and 178 nm (NE containing 3′-(trifluormethyl)-chalcone, in addition to presenting encapsulation efficiency values close to 100 %. Subsequently, the NE were added to a polymeric solution of polyvinyl alcohol (PVA) and processed via the electrospinning technique affording a PVA matrix (15 %, w/v) nanofiber containing the chalcones NE at 1 mg.mL−1. In a follow-up experiment, the skin permeation assay of the PVA matrix-chalcone NE was performed in vitro using Franz type diffusion cells and porcine ear as biological model of study. The results showed that the treatments with the nanofibers containing the chalcone NE were retained mainly in the stratum corneum, while the NE suspensions containing chalcone were retained in the epidermis and dermis. This result is thought to be relevant, since parasites are located mainly in the dermis. Further, in vitro assay against the amastigote form of L. (L) amazonensis, showed IC50 values to trans-chalcone and 3'-(trifluormethyl)-chalcone of 24.42 ± 6.76 μg.mL−1 and 15.36 ± 4.61 μg.mL−1, respectively. In addition to improving the solubility of the compounds tested in culture medium without using organic solvents, chalcones in nano-emulsified form reduced the IC50 to 9.09 ± 1.24 μg.mL−1 (trans-chalcone) and 10.27 ± 2.27 μg.mL−1 (3'-(trifluormethyl)-chalcone) which confirmed the potential of the nanoemulsion containing chalcone for cutaneous leishmaniasis treatment.</description><identifier>ISSN: 0927-7765</identifier><identifier>EISSN: 1873-4367</identifier><identifier>DOI: 10.1016/j.colsurfb.2020.111390</identifier><identifier>PMID: 33208279</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Cutaneous leishmaniasis ; Nanoemulsions ; Polyvinyl alcohol electrospinning ; Trans-chalcone</subject><ispartof>Colloids and surfaces, B, Biointerfaces, 2021-02, Vol.198, p.111390-111390, Article 111390</ispartof><rights>2020</rights><rights>Copyright © 2020. Published by Elsevier B.V.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c368t-7f2a2d44328743f405fa62e0d910dfc502c100d88e0686d8fa1ee4f677fd4e583</citedby><cites>FETCH-LOGICAL-c368t-7f2a2d44328743f405fa62e0d910dfc502c100d88e0686d8fa1ee4f677fd4e583</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.colsurfb.2020.111390$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33208279$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Coelho, Daniela</creatorcontrib><creatorcontrib>Veleirinho, Beatriz</creatorcontrib><creatorcontrib>Mazzarino, Letícia</creatorcontrib><creatorcontrib>Alberti, Thaís</creatorcontrib><creatorcontrib>Buzanello, Elizandra</creatorcontrib><creatorcontrib>Oliveira, Regina Eva</creatorcontrib><creatorcontrib>Yunes, Rosendo Augusto</creatorcontrib><creatorcontrib>Moraes, Milene</creatorcontrib><creatorcontrib>Steindel, Mário</creatorcontrib><creatorcontrib>Maraschin, Marcelo</creatorcontrib><title>Polyvinyl alcohol-based electrospun matrix as a delivery system for nanoemulsion containing chalcone against Leishmania (Leishmania) amazonensis</title><title>Colloids and surfaces, B, Biointerfaces</title><addtitle>Colloids Surf B Biointerfaces</addtitle><description>[Display omitted]
•Nanotechnological strategies increase cytotoxic activity of chalcone in vitro.•Nanostructures system to improve leishmanicidal toxicity against L. amazonensis.•Two nanotechnology methods associated for treatment of cutaneous leishmaniasis.•PVA matrix associated with chalcone's nanoemulsion for leishmaniasis treatment.
Cutaneous leishmaniasis is a worldwide public health problem. Conventional therapies, in addition to the high cost, have many adverse effects and cases of parasite’s resistance. Chalcones are secondary metabolites precursors in the flavonoid pathway and can be obtained naturally, but with low yield from plant raw material. Thus, the use of synthetic chalcones has been a promising strategy for the development of molecules with leishmanicidal activity. Thus, this work aimed to develop a controlled release system of two synthetic chalcone (trans-chalcones and 3'-(trifluormethyl)-chalcone) using polyvinyl alcohol nanofibers (PVA) as scaffold. The association of chalcones to the nanofibers was made by nanoemulsions (NE) thereof, i.e., a colloidal system on a nanometric scale, which allows compounds with opposite polarities to remain miscible and stable throughout their manipulation. Chalcone nanoemulsions were developed using the spontaneous emulsification technique. The NE were characterized regarding their particle size, polydispersion index (PDI), and zeta potential. The results showed NE with spherical shape, absolute values of zeta potential were higher than 30 mV and homogeneous distribution pattern (PDI < 0.3). Dynamics light scattering (DLS) analysis showed similar hydrodynamic rays, i.e., 180 nm (trans-chalcone NE) and 178 nm (NE containing 3′-(trifluormethyl)-chalcone, in addition to presenting encapsulation efficiency values close to 100 %. Subsequently, the NE were added to a polymeric solution of polyvinyl alcohol (PVA) and processed via the electrospinning technique affording a PVA matrix (15 %, w/v) nanofiber containing the chalcones NE at 1 mg.mL−1. In a follow-up experiment, the skin permeation assay of the PVA matrix-chalcone NE was performed in vitro using Franz type diffusion cells and porcine ear as biological model of study. The results showed that the treatments with the nanofibers containing the chalcone NE were retained mainly in the stratum corneum, while the NE suspensions containing chalcone were retained in the epidermis and dermis. This result is thought to be relevant, since parasites are located mainly in the dermis. Further, in vitro assay against the amastigote form of L. (L) amazonensis, showed IC50 values to trans-chalcone and 3'-(trifluormethyl)-chalcone of 24.42 ± 6.76 μg.mL−1 and 15.36 ± 4.61 μg.mL−1, respectively. In addition to improving the solubility of the compounds tested in culture medium without using organic solvents, chalcones in nano-emulsified form reduced the IC50 to 9.09 ± 1.24 μg.mL−1 (trans-chalcone) and 10.27 ± 2.27 μg.mL−1 (3'-(trifluormethyl)-chalcone) which confirmed the potential of the nanoemulsion containing chalcone for cutaneous leishmaniasis treatment.</description><subject>Cutaneous leishmaniasis</subject><subject>Nanoemulsions</subject><subject>Polyvinyl alcohol electrospinning</subject><subject>Trans-chalcone</subject><issn>0927-7765</issn><issn>1873-4367</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><recordid>eNqFkcuOEzEQRS0EYsLAL4y8HBYd_Irt3oFGvKRIsIC15djliSO3HezuiOYr-GQ6ygwsWVWpdG6V6l6EbihZU0Llm8PaldSmGnZrRtgypJT35AlaUa14J7hUT9GK9Ex1SsnNFXrR2oEQwgRVz9EV54xopvoV-v21pPkU85ywTa7sS-p2toHHkMCNtbTjlPFgxxp_YtuwxR5SPEGdcZvbCAMOpeJsc4FhSi2WjF3Jo4055nvs9uedGbC9XyZtxFuIbT_YHC2-_de_xnawvxYut9heomfBpgavHuo1-v7h_be7T932y8fPd--2neNSj50KzDIvBGdaCR4E2QQrGRDfU-KD2xDmKCFeayBSS6-DpQAiSKWCF7DR_BrdXvYea_kxQRvNEJuDlGyGMjXDhGSC9FSfUXlB3eJHqxDMscbB1tlQYs5pmIN5TMOc0zCXNBbhzcONaTeA_yt7tH8B3l4AWD49RaimuQjZgY91sd_4Ev934w_9NaKW</recordid><startdate>202102</startdate><enddate>202102</enddate><creator>Coelho, Daniela</creator><creator>Veleirinho, Beatriz</creator><creator>Mazzarino, Letícia</creator><creator>Alberti, Thaís</creator><creator>Buzanello, Elizandra</creator><creator>Oliveira, Regina Eva</creator><creator>Yunes, Rosendo Augusto</creator><creator>Moraes, Milene</creator><creator>Steindel, Mário</creator><creator>Maraschin, Marcelo</creator><general>Elsevier B.V</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>202102</creationdate><title>Polyvinyl alcohol-based electrospun matrix as a delivery system for nanoemulsion containing chalcone against Leishmania (Leishmania) amazonensis</title><author>Coelho, Daniela ; Veleirinho, Beatriz ; Mazzarino, Letícia ; Alberti, Thaís ; Buzanello, Elizandra ; Oliveira, Regina Eva ; Yunes, Rosendo Augusto ; Moraes, Milene ; Steindel, Mário ; Maraschin, Marcelo</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c368t-7f2a2d44328743f405fa62e0d910dfc502c100d88e0686d8fa1ee4f677fd4e583</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>Cutaneous leishmaniasis</topic><topic>Nanoemulsions</topic><topic>Polyvinyl alcohol electrospinning</topic><topic>Trans-chalcone</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Coelho, Daniela</creatorcontrib><creatorcontrib>Veleirinho, Beatriz</creatorcontrib><creatorcontrib>Mazzarino, Letícia</creatorcontrib><creatorcontrib>Alberti, Thaís</creatorcontrib><creatorcontrib>Buzanello, Elizandra</creatorcontrib><creatorcontrib>Oliveira, Regina Eva</creatorcontrib><creatorcontrib>Yunes, Rosendo Augusto</creatorcontrib><creatorcontrib>Moraes, Milene</creatorcontrib><creatorcontrib>Steindel, Mário</creatorcontrib><creatorcontrib>Maraschin, Marcelo</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Coelho, Daniela</au><au>Veleirinho, Beatriz</au><au>Mazzarino, Letícia</au><au>Alberti, Thaís</au><au>Buzanello, Elizandra</au><au>Oliveira, Regina Eva</au><au>Yunes, Rosendo Augusto</au><au>Moraes, Milene</au><au>Steindel, Mário</au><au>Maraschin, Marcelo</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Polyvinyl alcohol-based electrospun matrix as a delivery system for nanoemulsion containing chalcone against Leishmania (Leishmania) amazonensis</atitle><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle><addtitle>Colloids Surf B Biointerfaces</addtitle><date>2021-02</date><risdate>2021</risdate><volume>198</volume><spage>111390</spage><epage>111390</epage><pages>111390-111390</pages><artnum>111390</artnum><issn>0927-7765</issn><eissn>1873-4367</eissn><abstract>[Display omitted]
•Nanotechnological strategies increase cytotoxic activity of chalcone in vitro.•Nanostructures system to improve leishmanicidal toxicity against L. amazonensis.•Two nanotechnology methods associated for treatment of cutaneous leishmaniasis.•PVA matrix associated with chalcone's nanoemulsion for leishmaniasis treatment.
Cutaneous leishmaniasis is a worldwide public health problem. Conventional therapies, in addition to the high cost, have many adverse effects and cases of parasite’s resistance. Chalcones are secondary metabolites precursors in the flavonoid pathway and can be obtained naturally, but with low yield from plant raw material. Thus, the use of synthetic chalcones has been a promising strategy for the development of molecules with leishmanicidal activity. Thus, this work aimed to develop a controlled release system of two synthetic chalcone (trans-chalcones and 3'-(trifluormethyl)-chalcone) using polyvinyl alcohol nanofibers (PVA) as scaffold. The association of chalcones to the nanofibers was made by nanoemulsions (NE) thereof, i.e., a colloidal system on a nanometric scale, which allows compounds with opposite polarities to remain miscible and stable throughout their manipulation. Chalcone nanoemulsions were developed using the spontaneous emulsification technique. The NE were characterized regarding their particle size, polydispersion index (PDI), and zeta potential. The results showed NE with spherical shape, absolute values of zeta potential were higher than 30 mV and homogeneous distribution pattern (PDI < 0.3). Dynamics light scattering (DLS) analysis showed similar hydrodynamic rays, i.e., 180 nm (trans-chalcone NE) and 178 nm (NE containing 3′-(trifluormethyl)-chalcone, in addition to presenting encapsulation efficiency values close to 100 %. Subsequently, the NE were added to a polymeric solution of polyvinyl alcohol (PVA) and processed via the electrospinning technique affording a PVA matrix (15 %, w/v) nanofiber containing the chalcones NE at 1 mg.mL−1. In a follow-up experiment, the skin permeation assay of the PVA matrix-chalcone NE was performed in vitro using Franz type diffusion cells and porcine ear as biological model of study. The results showed that the treatments with the nanofibers containing the chalcone NE were retained mainly in the stratum corneum, while the NE suspensions containing chalcone were retained in the epidermis and dermis. This result is thought to be relevant, since parasites are located mainly in the dermis. Further, in vitro assay against the amastigote form of L. (L) amazonensis, showed IC50 values to trans-chalcone and 3'-(trifluormethyl)-chalcone of 24.42 ± 6.76 μg.mL−1 and 15.36 ± 4.61 μg.mL−1, respectively. In addition to improving the solubility of the compounds tested in culture medium without using organic solvents, chalcones in nano-emulsified form reduced the IC50 to 9.09 ± 1.24 μg.mL−1 (trans-chalcone) and 10.27 ± 2.27 μg.mL−1 (3'-(trifluormethyl)-chalcone) which confirmed the potential of the nanoemulsion containing chalcone for cutaneous leishmaniasis treatment.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>33208279</pmid><doi>10.1016/j.colsurfb.2020.111390</doi><tpages>1</tpages></addata></record> |
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subjects | Cutaneous leishmaniasis Nanoemulsions Polyvinyl alcohol electrospinning Trans-chalcone |
title | Polyvinyl alcohol-based electrospun matrix as a delivery system for nanoemulsion containing chalcone against Leishmania (Leishmania) amazonensis |
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