BBD-Based Development of Itraconazole Loaded Nanostructured Lipid Carrier for Topical Delivery: In Vitro Evaluation and Antimicrobial Assessment

Objectives The present study was aimed to develop itraconazole (ITZL)-loaded NLC for the treatment of fungal infection. Methods The formulation was prepared and optimized by the hot homogenization method and Box-Behnken statistical design. The total lipid ratio (A), surfactant (B), and homogenizatio...

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Veröffentlicht in:Journal of pharmaceutical innovation 2021-03, Vol.16 (1), p.85-98
Hauptverfasser: Ameeduzzafar, Qumber, Mohd, Alruwaili, Nabil K, Bukhari, Syed Nasir Abbas, Alharbi, Khalid Saad, Imam, Syed Sarim, Afzal, Muhammad, Alsuwayt, Bader, Mujtaba, Ali, Ali, Asgar
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container_end_page 98
container_issue 1
container_start_page 85
container_title Journal of pharmaceutical innovation
container_volume 16
creator Ameeduzzafar
Qumber, Mohd
Alruwaili, Nabil K
Bukhari, Syed Nasir Abbas
Alharbi, Khalid Saad
Imam, Syed Sarim
Afzal, Muhammad
Alsuwayt, Bader
Mujtaba, Ali
Ali, Asgar
description Objectives The present study was aimed to develop itraconazole (ITZL)-loaded NLC for the treatment of fungal infection. Methods The formulation was prepared and optimized by the hot homogenization method and Box-Behnken statistical design. The total lipid ratio (A), surfactant (B), and homogenization cycle (C) were selected as independent variables, and the effects of variables were evaluated on particle size (R 1 ), entrapment efficiency (R 2 ), and drug release in 12 h (R 3 ). Results The optimized formulation ITZLNLCopt showed particle size (147.31 ± 1.43 nm) high entrapment efficiency (86.36 ± 0.83%) and drug release (77.23 ± 3.33 %). The formulation ITZLNLCopt converted to carbopol (1% w/v) based gel (ITZLNLCopt gel) and showed good consistency and spreadability. The formulation ITZLNLCopt gel showed higher drug release (88.43 ± 2.54 % up to 24 h) and flux (2.46 fold) than control gel. The zone of inhibition results showed 2.6 and 2.36 fold higher inhibition ( P < 0.05) than control gel (ITZL gel) against Candida albicans and Aspergillus fumigatus . Conclusions It could be concluded that ITZLNLC gel as a potential alternative for the treatment of topical fungal infection after clinical study in the future.
doi_str_mv 10.1007/s12247-019-09420-5
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Methods The formulation was prepared and optimized by the hot homogenization method and Box-Behnken statistical design. The total lipid ratio (A), surfactant (B), and homogenization cycle (C) were selected as independent variables, and the effects of variables were evaluated on particle size (R 1 ), entrapment efficiency (R 2 ), and drug release in 12 h (R 3 ). Results The optimized formulation ITZLNLCopt showed particle size (147.31 ± 1.43 nm) high entrapment efficiency (86.36 ± 0.83%) and drug release (77.23 ± 3.33 %). The formulation ITZLNLCopt converted to carbopol (1% w/v) based gel (ITZLNLCopt gel) and showed good consistency and spreadability. The formulation ITZLNLCopt gel showed higher drug release (88.43 ± 2.54 % up to 24 h) and flux (2.46 fold) than control gel. The zone of inhibition results showed 2.6 and 2.36 fold higher inhibition ( P &lt; 0.05) than control gel (ITZL gel) against Candida albicans and Aspergillus fumigatus . Conclusions It could be concluded that ITZLNLC gel as a potential alternative for the treatment of topical fungal infection after clinical study in the future.</description><identifier>ISSN: 1872-5120</identifier><identifier>EISSN: 1939-8042</identifier><identifier>DOI: 10.1007/s12247-019-09420-5</identifier><language>eng</language><publisher>New York: Springer US</publisher><subject>Biochemical Engineering ; Biomedical and Life Sciences ; Biomedicine ; Biotechnology ; Industrial and Production Engineering ; Life Sciences &amp; Biomedicine ; Original Article ; Pharmacology &amp; Pharmacy ; Pharmacology/Toxicology ; Science &amp; Technology</subject><ispartof>Journal of pharmaceutical innovation, 2021-03, Vol.16 (1), p.85-98</ispartof><rights>Springer Science+Business Media, LLC, part of Springer Nature 2020</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>true</woscitedreferencessubscribed><woscitedreferencescount>47</woscitedreferencescount><woscitedreferencesoriginalsourcerecordid>wos000574068800002</woscitedreferencesoriginalsourcerecordid><citedby>FETCH-LOGICAL-c357t-44724986ee073638d7e1d1292be4c409a35cfd15b89fd62931c90120c830160b3</citedby><cites>FETCH-LOGICAL-c357t-44724986ee073638d7e1d1292be4c409a35cfd15b89fd62931c90120c830160b3</cites><orcidid>0000-0003-0181-0278 ; 0000-0003-0393-1890 ; 0000-0003-2358-4259 ; 0000-0003-2570-3223 ; 0000-0001-8125-7972</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s12247-019-09420-5$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s12247-019-09420-5$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>315,781,785,27929,27930,39263,41493,42562,51324</link.rule.ids></links><search><creatorcontrib>Ameeduzzafar</creatorcontrib><creatorcontrib>Qumber, Mohd</creatorcontrib><creatorcontrib>Alruwaili, Nabil K</creatorcontrib><creatorcontrib>Bukhari, Syed Nasir Abbas</creatorcontrib><creatorcontrib>Alharbi, Khalid Saad</creatorcontrib><creatorcontrib>Imam, Syed Sarim</creatorcontrib><creatorcontrib>Afzal, Muhammad</creatorcontrib><creatorcontrib>Alsuwayt, Bader</creatorcontrib><creatorcontrib>Mujtaba, Ali</creatorcontrib><creatorcontrib>Ali, Asgar</creatorcontrib><title>BBD-Based Development of Itraconazole Loaded Nanostructured Lipid Carrier for Topical Delivery: In Vitro Evaluation and Antimicrobial Assessment</title><title>Journal of pharmaceutical innovation</title><addtitle>J Pharm Innov</addtitle><addtitle>J PHARM INNOV</addtitle><description>Objectives The present study was aimed to develop itraconazole (ITZL)-loaded NLC for the treatment of fungal infection. Methods The formulation was prepared and optimized by the hot homogenization method and Box-Behnken statistical design. The total lipid ratio (A), surfactant (B), and homogenization cycle (C) were selected as independent variables, and the effects of variables were evaluated on particle size (R 1 ), entrapment efficiency (R 2 ), and drug release in 12 h (R 3 ). Results The optimized formulation ITZLNLCopt showed particle size (147.31 ± 1.43 nm) high entrapment efficiency (86.36 ± 0.83%) and drug release (77.23 ± 3.33 %). The formulation ITZLNLCopt converted to carbopol (1% w/v) based gel (ITZLNLCopt gel) and showed good consistency and spreadability. The formulation ITZLNLCopt gel showed higher drug release (88.43 ± 2.54 % up to 24 h) and flux (2.46 fold) than control gel. The zone of inhibition results showed 2.6 and 2.36 fold higher inhibition ( P &lt; 0.05) than control gel (ITZL gel) against Candida albicans and Aspergillus fumigatus . Conclusions It could be concluded that ITZLNLC gel as a potential alternative for the treatment of topical fungal infection after clinical study in the future.</description><subject>Biochemical Engineering</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotechnology</subject><subject>Industrial and Production Engineering</subject><subject>Life Sciences &amp; Biomedicine</subject><subject>Original Article</subject><subject>Pharmacology &amp; Pharmacy</subject><subject>Pharmacology/Toxicology</subject><subject>Science &amp; Technology</subject><issn>1872-5120</issn><issn>1939-8042</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><sourceid>HGBXW</sourceid><recordid>eNqNkMtO3DAUhqOqSKXQF-jK-8rl-JLE7m4mUBhpRDe028hxTiqjjD2ynanoU_DINUzFErHysfR_5_JV1WcGXxlAe5EY57KlwDQFLTnQ-l11yrTQVIHk70utWk5rxuFD9TGle4BaNwCn1eN6fUnXJuFILvGAc9jv0GcSJrLJ0djgzd8wI9kGM5bIrfEh5bjYvMTy3bq9G0lnYnQYyRQiuQt7Z81ces3ugPHhG9l48svlGMjVwcyLyS54YvxIVj67nbMxDK7kVylhSk-jz6uTycwJP_1_z6qf36_uuhu6_XG96VZbakXdZiply6VWDSK0ohFqbJGNjGs-oLQStBG1nUZWD0pPY8O1YFZDOd8qAayBQZxV_Ni3rJBSxKnfR7cz8aFn0D857Y9O--K0f3ba1wVSR-gPDmFK1qG3-AJCsdpKaJQqFfDO5edzu7D4XNAvb0dLWhzTqST8b4z9fViiL0JeW-8fnyCcBg</recordid><startdate>20210301</startdate><enddate>20210301</enddate><creator>Ameeduzzafar</creator><creator>Qumber, Mohd</creator><creator>Alruwaili, Nabil K</creator><creator>Bukhari, Syed Nasir Abbas</creator><creator>Alharbi, Khalid Saad</creator><creator>Imam, Syed Sarim</creator><creator>Afzal, Muhammad</creator><creator>Alsuwayt, Bader</creator><creator>Mujtaba, Ali</creator><creator>Ali, Asgar</creator><general>Springer US</general><general>Springer Nature</general><scope>BLEPL</scope><scope>DTL</scope><scope>HGBXW</scope><scope>AAYXX</scope><scope>CITATION</scope><orcidid>https://orcid.org/0000-0003-0181-0278</orcidid><orcidid>https://orcid.org/0000-0003-0393-1890</orcidid><orcidid>https://orcid.org/0000-0003-2358-4259</orcidid><orcidid>https://orcid.org/0000-0003-2570-3223</orcidid><orcidid>https://orcid.org/0000-0001-8125-7972</orcidid></search><sort><creationdate>20210301</creationdate><title>BBD-Based Development of Itraconazole Loaded Nanostructured Lipid Carrier for Topical Delivery: In Vitro Evaluation and Antimicrobial Assessment</title><author>Ameeduzzafar ; Qumber, Mohd ; Alruwaili, Nabil K ; Bukhari, Syed Nasir Abbas ; Alharbi, Khalid Saad ; Imam, Syed Sarim ; Afzal, Muhammad ; Alsuwayt, Bader ; Mujtaba, Ali ; Ali, Asgar</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c357t-44724986ee073638d7e1d1292be4c409a35cfd15b89fd62931c90120c830160b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>Biochemical Engineering</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Biotechnology</topic><topic>Industrial and Production Engineering</topic><topic>Life Sciences &amp; Biomedicine</topic><topic>Original Article</topic><topic>Pharmacology &amp; Pharmacy</topic><topic>Pharmacology/Toxicology</topic><topic>Science &amp; Technology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ameeduzzafar</creatorcontrib><creatorcontrib>Qumber, Mohd</creatorcontrib><creatorcontrib>Alruwaili, Nabil K</creatorcontrib><creatorcontrib>Bukhari, Syed Nasir Abbas</creatorcontrib><creatorcontrib>Alharbi, Khalid Saad</creatorcontrib><creatorcontrib>Imam, Syed Sarim</creatorcontrib><creatorcontrib>Afzal, Muhammad</creatorcontrib><creatorcontrib>Alsuwayt, Bader</creatorcontrib><creatorcontrib>Mujtaba, Ali</creatorcontrib><creatorcontrib>Ali, Asgar</creatorcontrib><collection>Web of Science Core Collection</collection><collection>Science Citation Index Expanded</collection><collection>Web of Science - Science Citation Index Expanded - 2021</collection><collection>CrossRef</collection><jtitle>Journal of pharmaceutical innovation</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ameeduzzafar</au><au>Qumber, Mohd</au><au>Alruwaili, Nabil K</au><au>Bukhari, Syed Nasir Abbas</au><au>Alharbi, Khalid Saad</au><au>Imam, Syed Sarim</au><au>Afzal, Muhammad</au><au>Alsuwayt, Bader</au><au>Mujtaba, Ali</au><au>Ali, Asgar</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>BBD-Based Development of Itraconazole Loaded Nanostructured Lipid Carrier for Topical Delivery: In Vitro Evaluation and Antimicrobial Assessment</atitle><jtitle>Journal of pharmaceutical innovation</jtitle><stitle>J Pharm Innov</stitle><stitle>J PHARM INNOV</stitle><date>2021-03-01</date><risdate>2021</risdate><volume>16</volume><issue>1</issue><spage>85</spage><epage>98</epage><pages>85-98</pages><issn>1872-5120</issn><eissn>1939-8042</eissn><abstract>Objectives The present study was aimed to develop itraconazole (ITZL)-loaded NLC for the treatment of fungal infection. Methods The formulation was prepared and optimized by the hot homogenization method and Box-Behnken statistical design. The total lipid ratio (A), surfactant (B), and homogenization cycle (C) were selected as independent variables, and the effects of variables were evaluated on particle size (R 1 ), entrapment efficiency (R 2 ), and drug release in 12 h (R 3 ). Results The optimized formulation ITZLNLCopt showed particle size (147.31 ± 1.43 nm) high entrapment efficiency (86.36 ± 0.83%) and drug release (77.23 ± 3.33 %). The formulation ITZLNLCopt converted to carbopol (1% w/v) based gel (ITZLNLCopt gel) and showed good consistency and spreadability. The formulation ITZLNLCopt gel showed higher drug release (88.43 ± 2.54 % up to 24 h) and flux (2.46 fold) than control gel. The zone of inhibition results showed 2.6 and 2.36 fold higher inhibition ( P &lt; 0.05) than control gel (ITZL gel) against Candida albicans and Aspergillus fumigatus . Conclusions It could be concluded that ITZLNLC gel as a potential alternative for the treatment of topical fungal infection after clinical study in the future.</abstract><cop>New York</cop><pub>Springer US</pub><doi>10.1007/s12247-019-09420-5</doi><tpages>14</tpages><orcidid>https://orcid.org/0000-0003-0181-0278</orcidid><orcidid>https://orcid.org/0000-0003-0393-1890</orcidid><orcidid>https://orcid.org/0000-0003-2358-4259</orcidid><orcidid>https://orcid.org/0000-0003-2570-3223</orcidid><orcidid>https://orcid.org/0000-0001-8125-7972</orcidid></addata></record>
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subjects Biochemical Engineering
Biomedical and Life Sciences
Biomedicine
Biotechnology
Industrial and Production Engineering
Life Sciences & Biomedicine
Original Article
Pharmacology & Pharmacy
Pharmacology/Toxicology
Science & Technology
title BBD-Based Development of Itraconazole Loaded Nanostructured Lipid Carrier for Topical Delivery: In Vitro Evaluation and Antimicrobial Assessment
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