Skin penetration and dermal tolerability of acrylic nanocapsules: Influence of the surface charge and a chitosan gel used as vehicle
[Display omitted] For an improved understanding of the relevant particle features for cutaneous use, we studied the effect of the surface charge of acrylic nanocapsules (around 150nm) and the effect of a chitosan gel vehicle on the particle penetration into normal and stripped human skin ex vivo as...
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| Veröffentlicht in: | International journal of pharmaceutics 2016-06, Vol.507 (1-2), p.12-20 |
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| container_title | International journal of pharmaceutics |
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| creator | Contri, R.V. Fiel, L.A. Alnasif, N. Pohlmann, A.R. Guterres, S.S. Schäfer-Korting, M. |
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For an improved understanding of the relevant particle features for cutaneous use, we studied the effect of the surface charge of acrylic nanocapsules (around 150nm) and the effect of a chitosan gel vehicle on the particle penetration into normal and stripped human skin ex vivo as well as local tolerability (cytotoxicity and irritancy). Rhodamin-tagged nanocapsules penetrated and remained in the stratum corneum. Penetration of cationic nanocapsules exceeded the penetration of anionic nanocapsules. When applied on stripped skin, however, the fluorescence was also recorded in the viable epidermis and dermis. Cationic surface charge and embedding the particles into chitosan gel favored access to deeper skin. Keratinocytes took up the nanocapsules rapidly. Cytotoxicity (viability |
| doi_str_mv | 10.1016/j.ijpharm.2016.03.046 |
| format | Article |
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For an improved understanding of the relevant particle features for cutaneous use, we studied the effect of the surface charge of acrylic nanocapsules (around 150nm) and the effect of a chitosan gel vehicle on the particle penetration into normal and stripped human skin ex vivo as well as local tolerability (cytotoxicity and irritancy). Rhodamin-tagged nanocapsules penetrated and remained in the stratum corneum. Penetration of cationic nanocapsules exceeded the penetration of anionic nanocapsules. When applied on stripped skin, however, the fluorescence was also recorded in the viable epidermis and dermis. Cationic surface charge and embedding the particles into chitosan gel favored access to deeper skin. Keratinocytes took up the nanocapsules rapidly. Cytotoxicity (viability<80%), following exposure for ≥24h, appears to be due to the surfactant polysorbate 80, used for nanocapsuleś stabilization. Uptake by fibroblasts was low and no cytotoxicity was observed. No irritant reactions were detected in the HET-CAM test. In conclusion, the surface charge and chitosan vehicle, as well as the skin barrier integrity, influence the skin penetration of acrylic nanocapsules. Particle localization in the intact stratum corneum of normal skin and good tolerability make the nanocapsules candidates for topical use on the skin, provided that the polymer wall allows the release of the active encapsulated substance.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2016.03.046</identifier><identifier>PMID: 27130364</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Cell Survival - drug effects ; Cells, Cultured ; Chitosan ; Chitosan - administration & dosage ; Chitosan - adverse effects ; Chitosan - chemistry ; Chitosan - pharmacokinetics ; Cytotoxicity ; Dermis - metabolism ; Epidermis - metabolism ; Fibroblasts - drug effects ; Fibroblasts - metabolism ; Gels - administration & dosage ; Gels - adverse effects ; Gels - chemistry ; Humans ; Irritancy ; Keratinocytes - drug effects ; Keratinocytes - metabolism ; Nanocapsules ; Nanocapsules - administration & dosage ; Nanocapsules - adverse effects ; Nanocapsules - chemistry ; Particle Size ; Polymer ; Polymethacrylic Acids - administration & dosage ; Polymethacrylic Acids - adverse effects ; Polymethacrylic Acids - chemistry ; Polysorbates - administration & dosage ; Polysorbates - adverse effects ; Polysorbates - chemistry ; Skin Absorption - drug effects ; Skin penetration ; Surface Properties</subject><ispartof>International journal of pharmaceutics, 2016-06, Vol.507 (1-2), p.12-20</ispartof><rights>2016 Elsevier B.V.</rights><rights>Copyright © 2016 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c478t-9176b79b31a0fc316e8c37d88c38de98fef31cfbc2548a5fba96cf8d56d93a973</citedby><cites>FETCH-LOGICAL-c478t-9176b79b31a0fc316e8c37d88c38de98fef31cfbc2548a5fba96cf8d56d93a973</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ijpharm.2016.03.046$$EHTML$$P50$$Gelsevier$$Hfree_for_read</linktohtml><link.rule.ids>315,781,785,3551,27929,27930,46000</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27130364$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Contri, R.V.</creatorcontrib><creatorcontrib>Fiel, L.A.</creatorcontrib><creatorcontrib>Alnasif, N.</creatorcontrib><creatorcontrib>Pohlmann, A.R.</creatorcontrib><creatorcontrib>Guterres, S.S.</creatorcontrib><creatorcontrib>Schäfer-Korting, M.</creatorcontrib><title>Skin penetration and dermal tolerability of acrylic nanocapsules: Influence of the surface charge and a chitosan gel used as vehicle</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>[Display omitted]
For an improved understanding of the relevant particle features for cutaneous use, we studied the effect of the surface charge of acrylic nanocapsules (around 150nm) and the effect of a chitosan gel vehicle on the particle penetration into normal and stripped human skin ex vivo as well as local tolerability (cytotoxicity and irritancy). Rhodamin-tagged nanocapsules penetrated and remained in the stratum corneum. Penetration of cationic nanocapsules exceeded the penetration of anionic nanocapsules. When applied on stripped skin, however, the fluorescence was also recorded in the viable epidermis and dermis. Cationic surface charge and embedding the particles into chitosan gel favored access to deeper skin. Keratinocytes took up the nanocapsules rapidly. Cytotoxicity (viability<80%), following exposure for ≥24h, appears to be due to the surfactant polysorbate 80, used for nanocapsuleś stabilization. Uptake by fibroblasts was low and no cytotoxicity was observed. No irritant reactions were detected in the HET-CAM test. In conclusion, the surface charge and chitosan vehicle, as well as the skin barrier integrity, influence the skin penetration of acrylic nanocapsules. Particle localization in the intact stratum corneum of normal skin and good tolerability make the nanocapsules candidates for topical use on the skin, provided that the polymer wall allows the release of the active encapsulated substance.</description><subject>Cell Survival - drug effects</subject><subject>Cells, Cultured</subject><subject>Chitosan</subject><subject>Chitosan - administration & dosage</subject><subject>Chitosan - adverse effects</subject><subject>Chitosan - chemistry</subject><subject>Chitosan - pharmacokinetics</subject><subject>Cytotoxicity</subject><subject>Dermis - metabolism</subject><subject>Epidermis - metabolism</subject><subject>Fibroblasts - drug effects</subject><subject>Fibroblasts - metabolism</subject><subject>Gels - administration & dosage</subject><subject>Gels - adverse effects</subject><subject>Gels - chemistry</subject><subject>Humans</subject><subject>Irritancy</subject><subject>Keratinocytes - drug effects</subject><subject>Keratinocytes - metabolism</subject><subject>Nanocapsules</subject><subject>Nanocapsules - administration & dosage</subject><subject>Nanocapsules - adverse effects</subject><subject>Nanocapsules - chemistry</subject><subject>Particle Size</subject><subject>Polymer</subject><subject>Polymethacrylic Acids - administration & dosage</subject><subject>Polymethacrylic Acids - adverse effects</subject><subject>Polymethacrylic Acids - chemistry</subject><subject>Polysorbates - administration & dosage</subject><subject>Polysorbates - adverse effects</subject><subject>Polysorbates - chemistry</subject><subject>Skin Absorption - drug effects</subject><subject>Skin penetration</subject><subject>Surface Properties</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU1v1DAQhi1ERZfCTwD5yCXBjhM74YJQxUelSj3Qni3HGXe9OHawnUp754fjsAtXLjN6rWc-PC9CbyipKaH8_aG2h2Wv4lw3RdaE1aTlz9CO9oJVrBX8OdoRJvqqo4JdopcpHQghvKHsBbpsBGWE8XaHfn3_YT1ewEOOKtvgsfITniDOyuEcHEQ1WmfzEQeDlY5HZzX2ygetlrQ6SB_wjTduBa9hQ_IecFqjUUXqst4j_GmoirA5JOXxIzi8JihvCT_B3moHr9CFUS7B63O-Qg9fPt9ff6tu777eXH-6rXQr-lwNVPBRDCOjihjNKIdeMzH1JfYTDL0Bw6g2o266tledGdXAtemnjk8DU4NgV-jdqe8Sw88VUpazTRqcUx7CmiQVA2toM7AN7U6ojiGlCEYu0c4qHiUlcjNAHuTZALkZIAmTxYBS9_Y8Yh1nmP5V_b14AT6eACgffbIQZdJ2u95kI-gsp2D_M-I3yLGcWA</recordid><startdate>20160630</startdate><enddate>20160630</enddate><creator>Contri, R.V.</creator><creator>Fiel, L.A.</creator><creator>Alnasif, N.</creator><creator>Pohlmann, A.R.</creator><creator>Guterres, S.S.</creator><creator>Schäfer-Korting, M.</creator><general>Elsevier B.V</general><scope>6I.</scope><scope>AAFTH</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20160630</creationdate><title>Skin penetration and dermal tolerability of acrylic nanocapsules: Influence of the surface charge and a chitosan gel used as vehicle</title><author>Contri, R.V. ; Fiel, L.A. ; Alnasif, N. ; Pohlmann, A.R. ; Guterres, S.S. ; Schäfer-Korting, M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c478t-9176b79b31a0fc316e8c37d88c38de98fef31cfbc2548a5fba96cf8d56d93a973</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Cell Survival - drug effects</topic><topic>Cells, Cultured</topic><topic>Chitosan</topic><topic>Chitosan - administration & dosage</topic><topic>Chitosan - adverse effects</topic><topic>Chitosan - chemistry</topic><topic>Chitosan - pharmacokinetics</topic><topic>Cytotoxicity</topic><topic>Dermis - metabolism</topic><topic>Epidermis - metabolism</topic><topic>Fibroblasts - drug effects</topic><topic>Fibroblasts - metabolism</topic><topic>Gels - administration & dosage</topic><topic>Gels - adverse effects</topic><topic>Gels - chemistry</topic><topic>Humans</topic><topic>Irritancy</topic><topic>Keratinocytes - drug effects</topic><topic>Keratinocytes - metabolism</topic><topic>Nanocapsules</topic><topic>Nanocapsules - administration & dosage</topic><topic>Nanocapsules - adverse effects</topic><topic>Nanocapsules - chemistry</topic><topic>Particle Size</topic><topic>Polymer</topic><topic>Polymethacrylic Acids - administration & dosage</topic><topic>Polymethacrylic Acids - adverse effects</topic><topic>Polymethacrylic Acids - chemistry</topic><topic>Polysorbates - administration & dosage</topic><topic>Polysorbates - adverse effects</topic><topic>Polysorbates - chemistry</topic><topic>Skin Absorption - drug effects</topic><topic>Skin penetration</topic><topic>Surface Properties</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Contri, R.V.</creatorcontrib><creatorcontrib>Fiel, L.A.</creatorcontrib><creatorcontrib>Alnasif, N.</creatorcontrib><creatorcontrib>Pohlmann, A.R.</creatorcontrib><creatorcontrib>Guterres, S.S.</creatorcontrib><creatorcontrib>Schäfer-Korting, M.</creatorcontrib><collection>ScienceDirect Open Access Titles</collection><collection>Elsevier:ScienceDirect:Open Access</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Contri, R.V.</au><au>Fiel, L.A.</au><au>Alnasif, N.</au><au>Pohlmann, A.R.</au><au>Guterres, S.S.</au><au>Schäfer-Korting, M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Skin penetration and dermal tolerability of acrylic nanocapsules: Influence of the surface charge and a chitosan gel used as vehicle</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2016-06-30</date><risdate>2016</risdate><volume>507</volume><issue>1-2</issue><spage>12</spage><epage>20</epage><pages>12-20</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>[Display omitted]
For an improved understanding of the relevant particle features for cutaneous use, we studied the effect of the surface charge of acrylic nanocapsules (around 150nm) and the effect of a chitosan gel vehicle on the particle penetration into normal and stripped human skin ex vivo as well as local tolerability (cytotoxicity and irritancy). Rhodamin-tagged nanocapsules penetrated and remained in the stratum corneum. Penetration of cationic nanocapsules exceeded the penetration of anionic nanocapsules. When applied on stripped skin, however, the fluorescence was also recorded in the viable epidermis and dermis. Cationic surface charge and embedding the particles into chitosan gel favored access to deeper skin. Keratinocytes took up the nanocapsules rapidly. Cytotoxicity (viability<80%), following exposure for ≥24h, appears to be due to the surfactant polysorbate 80, used for nanocapsuleś stabilization. Uptake by fibroblasts was low and no cytotoxicity was observed. No irritant reactions were detected in the HET-CAM test. In conclusion, the surface charge and chitosan vehicle, as well as the skin barrier integrity, influence the skin penetration of acrylic nanocapsules. Particle localization in the intact stratum corneum of normal skin and good tolerability make the nanocapsules candidates for topical use on the skin, provided that the polymer wall allows the release of the active encapsulated substance.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>27130364</pmid><doi>10.1016/j.ijpharm.2016.03.046</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Cell Survival - drug effects Cells, Cultured Chitosan Chitosan - administration & dosage Chitosan - adverse effects Chitosan - chemistry Chitosan - pharmacokinetics Cytotoxicity Dermis - metabolism Epidermis - metabolism Fibroblasts - drug effects Fibroblasts - metabolism Gels - administration & dosage Gels - adverse effects Gels - chemistry Humans Irritancy Keratinocytes - drug effects Keratinocytes - metabolism Nanocapsules Nanocapsules - administration & dosage Nanocapsules - adverse effects Nanocapsules - chemistry Particle Size Polymer Polymethacrylic Acids - administration & dosage Polymethacrylic Acids - adverse effects Polymethacrylic Acids - chemistry Polysorbates - administration & dosage Polysorbates - adverse effects Polysorbates - chemistry Skin Absorption - drug effects Skin penetration Surface Properties |
| title | Skin penetration and dermal tolerability of acrylic nanocapsules: Influence of the surface charge and a chitosan gel used as vehicle |
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