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A Quality by Design Approach for Developing SNEDDS Loaded with Vemurafenib for Enhanced Oral Bioavailability
Vemurafenib (VMF) is a practically insoluble (
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Published in: | AAPS PharmSciTech 2024-01, Vol.25 (1), p.14-14, Article 14 |
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creator | JVUS, Chakradhar Kothuri, Naresh Singh, Sanjay Verma, Sonia Shafi, Hasham Reddy, D. V. Siva Kedar, Ashwini Rana, Rafquat Mishra, Keerti Sharma, Deepak Chourasia, Manish K. |
description | Vemurafenib (VMF) is a practically insoluble ( |
doi_str_mv | 10.1208/s12249-023-02725-2 |
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in vitro
release profile of the drug loaded in SNEDDS was compared to the free drug in two media, pH 6.8 and 1.2, and the data obtained were analyzed with different mathematical models. A reverse-phase ultra-pressure liquid chromatography (UPLC) technique with high sensitivity and selectivity was developed and validated for the quantification of VMF in analytical and bioanalytical samples. Dissolution efficiency for SNEDDS was estimated using different models, which proved that the developed novel SNEDDS formulation had a better
in vitro
dissolution profile than the free drug. A 2.13-fold enhanced oral bioavailability of VMF-loaded SNEDDS compared to the free drug demonstrates the superiority of the developed formulation. This work thus presents an overview of VMF-loaded SNEDDS as a promising alternative to improve the oral bioavailability of the drug.
Graphical Abstract</description><identifier>ISSN: 1530-9932</identifier><identifier>EISSN: 1530-9932</identifier><identifier>DOI: 10.1208/s12249-023-02725-2</identifier><identifier>PMID: 38191830</identifier><language>eng</language><publisher>Cham: Springer International Publishing</publisher><subject>Biochemistry ; Biological Availability ; Biomedical and Life Sciences ; Biomedicine ; Biotechnology ; Chromatography, Reverse-Phase ; Pharmacology/Toxicology ; Pharmacy ; Polysorbates ; Research Article ; Solubility ; Vemurafenib</subject><ispartof>AAPS PharmSciTech, 2024-01, Vol.25 (1), p.14-14, Article 14</ispartof><rights>The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists 2024. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.</rights><rights>2024. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c347t-260e8138036c993b7614023a43530b283cc937173f040b3bbc1a2ece94b52ba43</citedby><cites>FETCH-LOGICAL-c347t-260e8138036c993b7614023a43530b283cc937173f040b3bbc1a2ece94b52ba43</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/38191830$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>JVUS, Chakradhar</creatorcontrib><creatorcontrib>Kothuri, Naresh</creatorcontrib><creatorcontrib>Singh, Sanjay</creatorcontrib><creatorcontrib>Verma, Sonia</creatorcontrib><creatorcontrib>Shafi, Hasham</creatorcontrib><creatorcontrib>Reddy, D. V. Siva</creatorcontrib><creatorcontrib>Kedar, Ashwini</creatorcontrib><creatorcontrib>Rana, Rafquat</creatorcontrib><creatorcontrib>Mishra, Keerti</creatorcontrib><creatorcontrib>Sharma, Deepak</creatorcontrib><creatorcontrib>Chourasia, Manish K.</creatorcontrib><title>A Quality by Design Approach for Developing SNEDDS Loaded with Vemurafenib for Enhanced Oral Bioavailability</title><title>AAPS PharmSciTech</title><addtitle>AAPS PharmSciTech</addtitle><addtitle>AAPS PharmSciTech</addtitle><description>Vemurafenib (VMF) is a practically insoluble (< 0.1 μg/mL) and least bioavailable (1%) drug. To enhance its oral bioavailability and solubility, we formulated a reliable self-nano emulsifying drug delivery system (SNEDDS). A Quality by Design (QbD) approach was used to optimize the ratio of Capryol 90, Tween 80, and Transcutol HP. VMF-loaded SNEDDS was characterized for its size, polydispersity index (PDI), zeta potential, drug content, and transmittance. The
in vitro
release profile of the drug loaded in SNEDDS was compared to the free drug in two media, pH 6.8 and 1.2, and the data obtained were analyzed with different mathematical models. A reverse-phase ultra-pressure liquid chromatography (UPLC) technique with high sensitivity and selectivity was developed and validated for the quantification of VMF in analytical and bioanalytical samples. Dissolution efficiency for SNEDDS was estimated using different models, which proved that the developed novel SNEDDS formulation had a better
in vitro
dissolution profile than the free drug. A 2.13-fold enhanced oral bioavailability of VMF-loaded SNEDDS compared to the free drug demonstrates the superiority of the developed formulation. This work thus presents an overview of VMF-loaded SNEDDS as a promising alternative to improve the oral bioavailability of the drug.
Graphical Abstract</description><subject>Biochemistry</subject><subject>Biological Availability</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotechnology</subject><subject>Chromatography, Reverse-Phase</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Polysorbates</subject><subject>Research Article</subject><subject>Solubility</subject><subject>Vemurafenib</subject><issn>1530-9932</issn><issn>1530-9932</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><recordid>eNp9kEtPAjEUhRujEUX_gAvTpZvRPubVJQI-EiIxqNumLR0omelgO4Ph31sYNK5cNG16v3vuPQeAK4xuMUH5nceExCxChIaTkSQiR-AMJxRFjFFy_OfdA-fer1AgMaOnoEdzzHBO0RkoB_C1FaVptlBu4Uh7s7BwsF67WqglLGoX_ja6rNfGLuDsZTwazeCkFnM9h1-mWcIPXbVOFNoauafHdimsCtWpEyW8N7XYCFMKaXYjLsBJIUqvLw93H7w_jN-GT9Fk-vg8HEwiReOsiUiKdI5pjmiqwvYyS3EcVhcxDX4kyalSjGY4owWKkaRSKiyIVprFMiEyYH1w0-kGG5-t9g2vjFe6LIXVdes5YZgkJE3iPKCkQ5WrvXe64GtnKuG2HCO-S5l3KfOwAN-nzElouj7ot7LS89-Wn1gDQDvAh5JdaMdXdets8Pyf7DcJC4Zh</recordid><startdate>20240108</startdate><enddate>20240108</enddate><creator>JVUS, Chakradhar</creator><creator>Kothuri, Naresh</creator><creator>Singh, Sanjay</creator><creator>Verma, Sonia</creator><creator>Shafi, Hasham</creator><creator>Reddy, D. 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VMF-loaded SNEDDS was characterized for its size, polydispersity index (PDI), zeta potential, drug content, and transmittance. The
in vitro
release profile of the drug loaded in SNEDDS was compared to the free drug in two media, pH 6.8 and 1.2, and the data obtained were analyzed with different mathematical models. A reverse-phase ultra-pressure liquid chromatography (UPLC) technique with high sensitivity and selectivity was developed and validated for the quantification of VMF in analytical and bioanalytical samples. Dissolution efficiency for SNEDDS was estimated using different models, which proved that the developed novel SNEDDS formulation had a better
in vitro
dissolution profile than the free drug. A 2.13-fold enhanced oral bioavailability of VMF-loaded SNEDDS compared to the free drug demonstrates the superiority of the developed formulation. This work thus presents an overview of VMF-loaded SNEDDS as a promising alternative to improve the oral bioavailability of the drug.
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subjects | Biochemistry Biological Availability Biomedical and Life Sciences Biomedicine Biotechnology Chromatography, Reverse-Phase Pharmacology/Toxicology Pharmacy Polysorbates Research Article Solubility Vemurafenib |
title | A Quality by Design Approach for Developing SNEDDS Loaded with Vemurafenib for Enhanced Oral Bioavailability |
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