Novel antipsoriatic fluidized spanlastic nanovesicles: In vitro physicochemical characterization, ex vivo cutaneous retention and exploratory clinical therapeutic efficacy
[Display omitted] Tazarotene (TAZ) is a topical synthetic retinoid used in psoriasis treatment, however, it is extremely lipophilic and exhibits skin irritation. Research is in a state of continuous advancement in the field of nanocarriers fabrication, and in this regard, we investigated the formula...
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Veröffentlicht in: | International journal of pharmaceutics 2019-09, Vol.568, p.118556-118556, Article 118556 |
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creator | Elmowafy, Enas El-Gogary, Riham I. Ragai, Maha H. Nasr, Maha |
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Tazarotene (TAZ) is a topical synthetic retinoid used in psoriasis treatment, however, it is extremely lipophilic and exhibits skin irritation. Research is in a state of continuous advancement in the field of nanocarriers fabrication, and in this regard, we investigated the formulation of novel topically oriented nanovesicles; representing a combination of spanlastics and penetration enhancer vesicles, to be termed (fluidized-SNs). TAZ-loaded fluidized SNs were physicochemically characterized, tested for ex vivo cutaneous retention, and the selected formulation was compared with the marketed product Acnitaz® regarding clinical antipsoriatic activity. The selected fluidized-SNs enriched with 1% cineole exhibited high entrapment for TAZ (76.19%), suitable size and zeta potential of 241.5 ± 5.68 nm and −36.10 ± 2.50 mV respectively, and retaining of stability after refrigeration storage for one month. As hypothesized, cineole enriched fluidized-SNs exhibited remarkable TAZ deposition amounting to a total of 81.51% in the different skin layers. Upon clinical assessment, the presented formulation displayed superior traits compared to the marketed product, in terms of dermoscopic imaging, morphometric analysis of psoriatic lesions, and statistical analysis of PASI scores. Results confirmed that the prepared novel fluidized spanlastics formulation holds great promise for the treatment of psoriasis, and its benefit should futuristically be investigated in other topical diseases. |
doi_str_mv | 10.1016/j.ijpharm.2019.118556 |
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Tazarotene (TAZ) is a topical synthetic retinoid used in psoriasis treatment, however, it is extremely lipophilic and exhibits skin irritation. Research is in a state of continuous advancement in the field of nanocarriers fabrication, and in this regard, we investigated the formulation of novel topically oriented nanovesicles; representing a combination of spanlastics and penetration enhancer vesicles, to be termed (fluidized-SNs). TAZ-loaded fluidized SNs were physicochemically characterized, tested for ex vivo cutaneous retention, and the selected formulation was compared with the marketed product Acnitaz® regarding clinical antipsoriatic activity. The selected fluidized-SNs enriched with 1% cineole exhibited high entrapment for TAZ (76.19%), suitable size and zeta potential of 241.5 ± 5.68 nm and −36.10 ± 2.50 mV respectively, and retaining of stability after refrigeration storage for one month. As hypothesized, cineole enriched fluidized-SNs exhibited remarkable TAZ deposition amounting to a total of 81.51% in the different skin layers. Upon clinical assessment, the presented formulation displayed superior traits compared to the marketed product, in terms of dermoscopic imaging, morphometric analysis of psoriatic lesions, and statistical analysis of PASI scores. Results confirmed that the prepared novel fluidized spanlastics formulation holds great promise for the treatment of psoriasis, and its benefit should futuristically be investigated in other topical diseases.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2019.118556</identifier><identifier>PMID: 31348982</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject><![CDATA[Administration, Cutaneous ; Adult ; Animals ; Clinical efficacy ; Cutaneous retention ; Dermatologic Agents - administration & dosage ; Eucalyptol - administration & dosage ; Female ; Hexoses - administration & dosage ; Humans ; Male ; Middle Aged ; Nanostructures - administration & dosage ; Nicotinic Acids - administration & dosage ; Polysorbates - administration & dosage ; Psoriasis ; Psoriasis - drug therapy ; Psoriasis - pathology ; Rats ; Skin - drug effects ; Skin - metabolism ; Skin - pathology ; Skin Absorption ; Spanlastic nanovesicles ; Tazarotene ; Treatment Outcome ; Young Adult]]></subject><ispartof>International journal of pharmaceutics, 2019-09, Vol.568, p.118556-118556, Article 118556</ispartof><rights>2019 Elsevier B.V.</rights><rights>Copyright © 2019 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c365t-6a6433b287db2b0ceb3c66980ba50474f39bc8535cf50cb525feea3d440e8fc53</citedby><cites>FETCH-LOGICAL-c365t-6a6433b287db2b0ceb3c66980ba50474f39bc8535cf50cb525feea3d440e8fc53</cites><orcidid>0000-0003-3534-8800</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ijpharm.2019.118556$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/31348982$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Elmowafy, Enas</creatorcontrib><creatorcontrib>El-Gogary, Riham I.</creatorcontrib><creatorcontrib>Ragai, Maha H.</creatorcontrib><creatorcontrib>Nasr, Maha</creatorcontrib><title>Novel antipsoriatic fluidized spanlastic nanovesicles: In vitro physicochemical characterization, ex vivo cutaneous retention and exploratory clinical therapeutic efficacy</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>[Display omitted]
Tazarotene (TAZ) is a topical synthetic retinoid used in psoriasis treatment, however, it is extremely lipophilic and exhibits skin irritation. Research is in a state of continuous advancement in the field of nanocarriers fabrication, and in this regard, we investigated the formulation of novel topically oriented nanovesicles; representing a combination of spanlastics and penetration enhancer vesicles, to be termed (fluidized-SNs). TAZ-loaded fluidized SNs were physicochemically characterized, tested for ex vivo cutaneous retention, and the selected formulation was compared with the marketed product Acnitaz® regarding clinical antipsoriatic activity. The selected fluidized-SNs enriched with 1% cineole exhibited high entrapment for TAZ (76.19%), suitable size and zeta potential of 241.5 ± 5.68 nm and −36.10 ± 2.50 mV respectively, and retaining of stability after refrigeration storage for one month. As hypothesized, cineole enriched fluidized-SNs exhibited remarkable TAZ deposition amounting to a total of 81.51% in the different skin layers. Upon clinical assessment, the presented formulation displayed superior traits compared to the marketed product, in terms of dermoscopic imaging, morphometric analysis of psoriatic lesions, and statistical analysis of PASI scores. Results confirmed that the prepared novel fluidized spanlastics formulation holds great promise for the treatment of psoriasis, and its benefit should futuristically be investigated in other topical diseases.</description><subject>Administration, Cutaneous</subject><subject>Adult</subject><subject>Animals</subject><subject>Clinical efficacy</subject><subject>Cutaneous retention</subject><subject>Dermatologic Agents - administration & dosage</subject><subject>Eucalyptol - administration & dosage</subject><subject>Female</subject><subject>Hexoses - administration & dosage</subject><subject>Humans</subject><subject>Male</subject><subject>Middle Aged</subject><subject>Nanostructures - administration & dosage</subject><subject>Nicotinic Acids - administration & dosage</subject><subject>Polysorbates - administration & dosage</subject><subject>Psoriasis</subject><subject>Psoriasis - drug therapy</subject><subject>Psoriasis - pathology</subject><subject>Rats</subject><subject>Skin - drug effects</subject><subject>Skin - metabolism</subject><subject>Skin - pathology</subject><subject>Skin Absorption</subject><subject>Spanlastic nanovesicles</subject><subject>Tazarotene</subject><subject>Treatment Outcome</subject><subject>Young Adult</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>eNqFkc2O1DAQhCMEYoeFRwD5yIEMdhw7CRe0WvGz0goucLacTkfjkWMH2xkx-0q8JA4ZuHKyVP11VVtVFC8Z3TPK5Nvj3hzngw7TvqKs2zPWCiEfFTvWNrzkdSMfFzvKm7YUrOFXxbMYj5RSWTH-tLjijNdt11a74tcXf0JLtEtmjj4YnQyQ0S5mMA84kDhrZ3VcRaddRqMBi_EduXPkZFLwZD6cs-bhgJMBbQnkmzQkDOYhe3n3huDPjJ48gSVph36JJGBCtw5z7pDns_VBJx_OBKxxf2zSAYOecVmTcRyzBufnxZNR24gvLu918f3jh2-3n8v7r5_ubm_uS-BSpFJqWXPeV20z9FVPAXsOUnYt7bWgdVOPvOuhFVzAKCj0ohIjouZDXVNsRxD8uni9-c7B_1gwJjWZCGjtdr6qKika2QneZlRsKAQfY8BRzcFMOpwVo2rtSR3VpSe19qS2nvLeq0vE0k84_Nv6W0wG3m8A5o-eDAYVwaADHExASGrw5j8RvwEjR61V</recordid><startdate>20190910</startdate><enddate>20190910</enddate><creator>Elmowafy, Enas</creator><creator>El-Gogary, Riham I.</creator><creator>Ragai, Maha H.</creator><creator>Nasr, Maha</creator><general>Elsevier B.V</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><orcidid>https://orcid.org/0000-0003-3534-8800</orcidid></search><sort><creationdate>20190910</creationdate><title>Novel antipsoriatic fluidized spanlastic nanovesicles: In vitro physicochemical characterization, ex vivo cutaneous retention and exploratory clinical therapeutic efficacy</title><author>Elmowafy, Enas ; El-Gogary, Riham I. ; Ragai, Maha H. ; Nasr, Maha</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c365t-6a6433b287db2b0ceb3c66980ba50474f39bc8535cf50cb525feea3d440e8fc53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>Administration, Cutaneous</topic><topic>Adult</topic><topic>Animals</topic><topic>Clinical efficacy</topic><topic>Cutaneous retention</topic><topic>Dermatologic Agents - administration & dosage</topic><topic>Eucalyptol - administration & dosage</topic><topic>Female</topic><topic>Hexoses - administration & dosage</topic><topic>Humans</topic><topic>Male</topic><topic>Middle Aged</topic><topic>Nanostructures - administration & dosage</topic><topic>Nicotinic Acids - administration & dosage</topic><topic>Polysorbates - administration & dosage</topic><topic>Psoriasis</topic><topic>Psoriasis - drug therapy</topic><topic>Psoriasis - pathology</topic><topic>Rats</topic><topic>Skin - drug effects</topic><topic>Skin - metabolism</topic><topic>Skin - pathology</topic><topic>Skin Absorption</topic><topic>Spanlastic nanovesicles</topic><topic>Tazarotene</topic><topic>Treatment Outcome</topic><topic>Young Adult</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Elmowafy, Enas</creatorcontrib><creatorcontrib>El-Gogary, Riham I.</creatorcontrib><creatorcontrib>Ragai, Maha H.</creatorcontrib><creatorcontrib>Nasr, Maha</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><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Elmowafy, Enas</au><au>El-Gogary, Riham I.</au><au>Ragai, Maha H.</au><au>Nasr, Maha</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel antipsoriatic fluidized spanlastic nanovesicles: In vitro physicochemical characterization, ex vivo cutaneous retention and exploratory clinical therapeutic efficacy</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2019-09-10</date><risdate>2019</risdate><volume>568</volume><spage>118556</spage><epage>118556</epage><pages>118556-118556</pages><artnum>118556</artnum><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>[Display omitted]
Tazarotene (TAZ) is a topical synthetic retinoid used in psoriasis treatment, however, it is extremely lipophilic and exhibits skin irritation. Research is in a state of continuous advancement in the field of nanocarriers fabrication, and in this regard, we investigated the formulation of novel topically oriented nanovesicles; representing a combination of spanlastics and penetration enhancer vesicles, to be termed (fluidized-SNs). TAZ-loaded fluidized SNs were physicochemically characterized, tested for ex vivo cutaneous retention, and the selected formulation was compared with the marketed product Acnitaz® regarding clinical antipsoriatic activity. The selected fluidized-SNs enriched with 1% cineole exhibited high entrapment for TAZ (76.19%), suitable size and zeta potential of 241.5 ± 5.68 nm and −36.10 ± 2.50 mV respectively, and retaining of stability after refrigeration storage for one month. As hypothesized, cineole enriched fluidized-SNs exhibited remarkable TAZ deposition amounting to a total of 81.51% in the different skin layers. Upon clinical assessment, the presented formulation displayed superior traits compared to the marketed product, in terms of dermoscopic imaging, morphometric analysis of psoriatic lesions, and statistical analysis of PASI scores. Results confirmed that the prepared novel fluidized spanlastics formulation holds great promise for the treatment of psoriasis, and its benefit should futuristically be investigated in other topical diseases.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>31348982</pmid><doi>10.1016/j.ijpharm.2019.118556</doi><tpages>1</tpages><orcidid>https://orcid.org/0000-0003-3534-8800</orcidid></addata></record> |
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subjects | Administration, Cutaneous Adult Animals Clinical efficacy Cutaneous retention Dermatologic Agents - administration & dosage Eucalyptol - administration & dosage Female Hexoses - administration & dosage Humans Male Middle Aged Nanostructures - administration & dosage Nicotinic Acids - administration & dosage Polysorbates - administration & dosage Psoriasis Psoriasis - drug therapy Psoriasis - pathology Rats Skin - drug effects Skin - metabolism Skin - pathology Skin Absorption Spanlastic nanovesicles Tazarotene Treatment Outcome Young Adult |
title | Novel antipsoriatic fluidized spanlastic nanovesicles: In vitro physicochemical characterization, ex vivo cutaneous retention and exploratory clinical therapeutic efficacy |
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