Polyoxazolines based mixed micelles as PEG free formulations for an effective quercetin antioxidant topical delivery
[Display omitted] •Amphiphilic polyoxazolines have less impact on cell viability than its poly(ethylene glycol) equivalent.•First formulation for topical delivery with polyoxazolines as a non ionic surfactant.•Stable nanosized formulations successfully encapsulate quercetin antioxidant.•Loaded mixed...
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Veröffentlicht in: | International journal of pharmaceutics 2019-10, Vol.570, p.118516-118516, Article 118516 |
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container_title | International journal of pharmaceutics |
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creator | Simon, L. Vincent, M. Le Saux, S. Lapinte, V. Marcotte, N. Morille, M. Dorandeu, C. Devoisselle, J.M. Bégu, S. |
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•Amphiphilic polyoxazolines have less impact on cell viability than its poly(ethylene glycol) equivalent.•First formulation for topical delivery with polyoxazolines as a non ionic surfactant.•Stable nanosized formulations successfully encapsulate quercetin antioxidant.•Loaded mixed-micelles improved cell viability and antioxidant activity compared to crude quercetin.
This study aims to prove the value of the polyoxazolines polymer family as surfactant in formulations for topical application and as an alternative to PEG overuse. The amphiphilic polyoxazolines (POx) were demonstrated to have less impact on cell viability of mice fibroblasts (NIH3T3) than their PEG counterparts. Mixed micelles, made of POx and phosphatidylcholine, were manufactured using thin film and high pressure homogenizer process. The mixed micelles were optimized to produce nanosized vesicles of about 20 nm with a spherical shape and stable over 28 days. The natural lipophilic antioxidant, quercetin, was successfully encapsulated (encapsulation efficiency 94 ± 4% and drug loading 3.6 ± 0.2%) in the mixed micelles with no morphological variation. Once loaded in the formulation, the quercetin impact on cell viability of NIH3T3 was decreased while its antioxidant activity remained unchanged. This work highlights the capacity of amphiphilic POx to create, in association with phospholipids, stable nanoformulations which show promise for topical delivery of antioxidant and ensure skin protection against oxidative stress. |
doi_str_mv | 10.1016/j.ijpharm.2019.118516 |
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•Amphiphilic polyoxazolines have less impact on cell viability than its poly(ethylene glycol) equivalent.•First formulation for topical delivery with polyoxazolines as a non ionic surfactant.•Stable nanosized formulations successfully encapsulate quercetin antioxidant.•Loaded mixed-micelles improved cell viability and antioxidant activity compared to crude quercetin.
This study aims to prove the value of the polyoxazolines polymer family as surfactant in formulations for topical application and as an alternative to PEG overuse. The amphiphilic polyoxazolines (POx) were demonstrated to have less impact on cell viability of mice fibroblasts (NIH3T3) than their PEG counterparts. Mixed micelles, made of POx and phosphatidylcholine, were manufactured using thin film and high pressure homogenizer process. The mixed micelles were optimized to produce nanosized vesicles of about 20 nm with a spherical shape and stable over 28 days. The natural lipophilic antioxidant, quercetin, was successfully encapsulated (encapsulation efficiency 94 ± 4% and drug loading 3.6 ± 0.2%) in the mixed micelles with no morphological variation. Once loaded in the formulation, the quercetin impact on cell viability of NIH3T3 was decreased while its antioxidant activity remained unchanged. This work highlights the capacity of amphiphilic POx to create, in association with phospholipids, stable nanoformulations which show promise for topical delivery of antioxidant and ensure skin protection against oxidative stress.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2019.118516</identifier><identifier>PMID: 31319148</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Administration, Topical ; Animals ; Antioxidant ; Antioxidants - administration & dosage ; Antioxidants - chemistry ; Cell Line ; Cell Survival - drug effects ; Chemistry, Pharmaceutical - methods ; Drug Carriers - chemistry ; Drug Delivery Systems - methods ; Drug Liberation - drug effects ; Fibroblasts - drug effects ; Hybrid vesicle ; Life Sciences ; Mice ; Micelles ; NIH 3T3 Cells ; Oxazolone - analogs & derivatives ; Oxazolone - chemistry ; Oxidative Stress - drug effects ; Particle Size ; PEG free ; Pharmaceutical sciences ; Polyethylene Glycols - chemistry ; Polymers - chemistry ; Polyoxazolines ; Quercetin - administration & dosage ; Quercetin - chemistry ; Skin protection ; Topical delivery</subject><ispartof>International journal of pharmaceutics, 2019-10, Vol.570, p.118516-118516, Article 118516</ispartof><rights>2019</rights><rights>Copyright © 2019. Published by Elsevier B.V.</rights><rights>Attribution - NonCommercial</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c446t-e4e07ce8c9f1a449813b738c2012c9e08614b35e02fd6deb7bf2b6ead7e670673</citedby><cites>FETCH-LOGICAL-c446t-e4e07ce8c9f1a449813b738c2012c9e08614b35e02fd6deb7bf2b6ead7e670673</cites><orcidid>0000-0001-8224-7346</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0378517319305605$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,776,780,881,3537,27901,27902,65534</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/31319148$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://hal.science/hal-03212233$$DView record in HAL$$Hfree_for_read</backlink></links><search><creatorcontrib>Simon, L.</creatorcontrib><creatorcontrib>Vincent, M.</creatorcontrib><creatorcontrib>Le Saux, S.</creatorcontrib><creatorcontrib>Lapinte, V.</creatorcontrib><creatorcontrib>Marcotte, N.</creatorcontrib><creatorcontrib>Morille, M.</creatorcontrib><creatorcontrib>Dorandeu, C.</creatorcontrib><creatorcontrib>Devoisselle, J.M.</creatorcontrib><creatorcontrib>Bégu, S.</creatorcontrib><title>Polyoxazolines based mixed micelles as PEG free formulations for an effective quercetin antioxidant topical delivery</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>[Display omitted]
•Amphiphilic polyoxazolines have less impact on cell viability than its poly(ethylene glycol) equivalent.•First formulation for topical delivery with polyoxazolines as a non ionic surfactant.•Stable nanosized formulations successfully encapsulate quercetin antioxidant.•Loaded mixed-micelles improved cell viability and antioxidant activity compared to crude quercetin.
This study aims to prove the value of the polyoxazolines polymer family as surfactant in formulations for topical application and as an alternative to PEG overuse. The amphiphilic polyoxazolines (POx) were demonstrated to have less impact on cell viability of mice fibroblasts (NIH3T3) than their PEG counterparts. Mixed micelles, made of POx and phosphatidylcholine, were manufactured using thin film and high pressure homogenizer process. The mixed micelles were optimized to produce nanosized vesicles of about 20 nm with a spherical shape and stable over 28 days. The natural lipophilic antioxidant, quercetin, was successfully encapsulated (encapsulation efficiency 94 ± 4% and drug loading 3.6 ± 0.2%) in the mixed micelles with no morphological variation. Once loaded in the formulation, the quercetin impact on cell viability of NIH3T3 was decreased while its antioxidant activity remained unchanged. This work highlights the capacity of amphiphilic POx to create, in association with phospholipids, stable nanoformulations which show promise for topical delivery of antioxidant and ensure skin protection against oxidative stress.</description><subject>Administration, Topical</subject><subject>Animals</subject><subject>Antioxidant</subject><subject>Antioxidants - administration & dosage</subject><subject>Antioxidants - chemistry</subject><subject>Cell Line</subject><subject>Cell Survival - drug effects</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Delivery Systems - methods</subject><subject>Drug Liberation - drug effects</subject><subject>Fibroblasts - drug effects</subject><subject>Hybrid vesicle</subject><subject>Life Sciences</subject><subject>Mice</subject><subject>Micelles</subject><subject>NIH 3T3 Cells</subject><subject>Oxazolone - analogs & derivatives</subject><subject>Oxazolone - chemistry</subject><subject>Oxidative Stress - drug effects</subject><subject>Particle Size</subject><subject>PEG free</subject><subject>Pharmaceutical sciences</subject><subject>Polyethylene Glycols - chemistry</subject><subject>Polymers - chemistry</subject><subject>Polyoxazolines</subject><subject>Quercetin - administration & dosage</subject><subject>Quercetin - chemistry</subject><subject>Skin protection</subject><subject>Topical delivery</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU9v1DAQxS1ERZfCRwD5SA_ZeuzETk6oqvoHaSV6gLPl2BPVqyRe7Oxql0-PQ5ZeuXjkp9_M6M0j5BOwNTCQN9u13-5eTBzWnEGzBqgrkG_ICmolClEq-ZasmFB1UYESl-R9SlvGmOQg3pFLAQIaKOsVmZ5DfwpH8zv0fsREW5PQ0cEf_74W-z6LJtHn-0faRUTahTjsezP5MKb5Q81IsevQTv6A9Nceo8XJj1nOyNG7XOkUdt6anjrsMxRPH8hFZ_qEH8_1ivx8uP9x91Rsvj9-u7vdFLYs5VRgiUxZrG3TgSnLpgbRKlHbbJjbBlktoWxFhYx3TjpsVdvxVqJxCqViUokrcr3MfTG93kU_mHjSwXj9dLvRs8YEB86FOEBmvyzsLobsIk168Gn2b0YM-6Q5l8Blo6p5bLWgNoaUInavs4HpORy91edw9ByOXsLJfZ_PK_btgO61618aGfi6AJiPcvAYdbIeR4vOx3xg7YL_z4o_jvCkSg</recordid><startdate>20191030</startdate><enddate>20191030</enddate><creator>Simon, L.</creator><creator>Vincent, M.</creator><creator>Le Saux, S.</creator><creator>Lapinte, V.</creator><creator>Marcotte, N.</creator><creator>Morille, M.</creator><creator>Dorandeu, C.</creator><creator>Devoisselle, J.M.</creator><creator>Bégu, S.</creator><general>Elsevier B.V</general><general>Elsevier</general><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><scope>1XC</scope><scope>VOOES</scope><orcidid>https://orcid.org/0000-0001-8224-7346</orcidid></search><sort><creationdate>20191030</creationdate><title>Polyoxazolines based mixed micelles as PEG free formulations for an effective quercetin antioxidant topical delivery</title><author>Simon, L. ; Vincent, M. ; Le Saux, S. ; Lapinte, V. ; Marcotte, N. ; Morille, M. ; Dorandeu, C. ; Devoisselle, J.M. ; Bégu, S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c446t-e4e07ce8c9f1a449813b738c2012c9e08614b35e02fd6deb7bf2b6ead7e670673</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>Administration, Topical</topic><topic>Animals</topic><topic>Antioxidant</topic><topic>Antioxidants - administration & dosage</topic><topic>Antioxidants - chemistry</topic><topic>Cell Line</topic><topic>Cell Survival - drug effects</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Delivery Systems - methods</topic><topic>Drug Liberation - drug effects</topic><topic>Fibroblasts - drug effects</topic><topic>Hybrid vesicle</topic><topic>Life Sciences</topic><topic>Mice</topic><topic>Micelles</topic><topic>NIH 3T3 Cells</topic><topic>Oxazolone - analogs & derivatives</topic><topic>Oxazolone - chemistry</topic><topic>Oxidative Stress - drug effects</topic><topic>Particle Size</topic><topic>PEG free</topic><topic>Pharmaceutical sciences</topic><topic>Polyethylene Glycols - chemistry</topic><topic>Polymers - chemistry</topic><topic>Polyoxazolines</topic><topic>Quercetin - administration & dosage</topic><topic>Quercetin - chemistry</topic><topic>Skin protection</topic><topic>Topical delivery</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Simon, L.</creatorcontrib><creatorcontrib>Vincent, M.</creatorcontrib><creatorcontrib>Le Saux, S.</creatorcontrib><creatorcontrib>Lapinte, V.</creatorcontrib><creatorcontrib>Marcotte, N.</creatorcontrib><creatorcontrib>Morille, M.</creatorcontrib><creatorcontrib>Dorandeu, C.</creatorcontrib><creatorcontrib>Devoisselle, J.M.</creatorcontrib><creatorcontrib>Bégu, S.</creatorcontrib><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><collection>Hyper Article en Ligne (HAL)</collection><collection>Hyper Article en Ligne (HAL) (Open Access)</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Simon, L.</au><au>Vincent, M.</au><au>Le Saux, S.</au><au>Lapinte, V.</au><au>Marcotte, N.</au><au>Morille, M.</au><au>Dorandeu, C.</au><au>Devoisselle, J.M.</au><au>Bégu, S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Polyoxazolines based mixed micelles as PEG free formulations for an effective quercetin antioxidant topical delivery</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2019-10-30</date><risdate>2019</risdate><volume>570</volume><spage>118516</spage><epage>118516</epage><pages>118516-118516</pages><artnum>118516</artnum><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>[Display omitted]
•Amphiphilic polyoxazolines have less impact on cell viability than its poly(ethylene glycol) equivalent.•First formulation for topical delivery with polyoxazolines as a non ionic surfactant.•Stable nanosized formulations successfully encapsulate quercetin antioxidant.•Loaded mixed-micelles improved cell viability and antioxidant activity compared to crude quercetin.
This study aims to prove the value of the polyoxazolines polymer family as surfactant in formulations for topical application and as an alternative to PEG overuse. The amphiphilic polyoxazolines (POx) were demonstrated to have less impact on cell viability of mice fibroblasts (NIH3T3) than their PEG counterparts. Mixed micelles, made of POx and phosphatidylcholine, were manufactured using thin film and high pressure homogenizer process. The mixed micelles were optimized to produce nanosized vesicles of about 20 nm with a spherical shape and stable over 28 days. The natural lipophilic antioxidant, quercetin, was successfully encapsulated (encapsulation efficiency 94 ± 4% and drug loading 3.6 ± 0.2%) in the mixed micelles with no morphological variation. Once loaded in the formulation, the quercetin impact on cell viability of NIH3T3 was decreased while its antioxidant activity remained unchanged. This work highlights the capacity of amphiphilic POx to create, in association with phospholipids, stable nanoformulations which show promise for topical delivery of antioxidant and ensure skin protection against oxidative stress.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>31319148</pmid><doi>10.1016/j.ijpharm.2019.118516</doi><tpages>1</tpages><orcidid>https://orcid.org/0000-0001-8224-7346</orcidid><oa>free_for_read</oa></addata></record> |
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subjects | Administration, Topical Animals Antioxidant Antioxidants - administration & dosage Antioxidants - chemistry Cell Line Cell Survival - drug effects Chemistry, Pharmaceutical - methods Drug Carriers - chemistry Drug Delivery Systems - methods Drug Liberation - drug effects Fibroblasts - drug effects Hybrid vesicle Life Sciences Mice Micelles NIH 3T3 Cells Oxazolone - analogs & derivatives Oxazolone - chemistry Oxidative Stress - drug effects Particle Size PEG free Pharmaceutical sciences Polyethylene Glycols - chemistry Polymers - chemistry Polyoxazolines Quercetin - administration & dosage Quercetin - chemistry Skin protection Topical delivery |
title | Polyoxazolines based mixed micelles as PEG free formulations for an effective quercetin antioxidant topical delivery |
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