Formulation and characterization of voriconazole nanospray dried powders
Purpose: Voriconazole nanoparticles (API-NPs) were prepared by nanospray drying to improve the solubility of voriconazole and reduce its interindividual variability. Methods: The preparation procedure was optimized by central composite design-response surface methodology. The properties of the nanop...
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| Veröffentlicht in: | Pharmaceutical development and technology 2020-08, Vol.25 (7), p.815-822 |
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| creator | Chen, Rui Zhang, Tinghua Bao, Sha Liu, Yinkun Xu, Xiaohong |
| description | Purpose: Voriconazole nanoparticles (API-NPs) were prepared by nanospray drying to improve the solubility of voriconazole and reduce its interindividual variability.
Methods: The preparation procedure was optimized by central composite design-response surface methodology. The properties of the nanoparticles were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analyses. The solubility, dissolution, and stability of the API-NPs were determined experimentally. The pharmacokinetics were assessed based on rat plasma levels of voriconazole. An acute oral toxicity test of the API-NPs was performed in mice.
Results: The powers were formulated using cetyltrimethylammonium chloride (CTAC) as the carrier material. SEM and particle size results showed that the API-NPs had a narrow particle size distribution. The XRD, DSC, and FTIR analyses show a decrease in crystallinity and a polymorphic transformation of the nanoparticles after nanospray drying. The solubility in water was approximately 15 times higher than that of voriconazole. The API-NP tablets exhibited significantly higher plasma exposure, namely, longer acting times and lower variability. The acute administration of voriconazole showed no toxic histopathological effects on organ tissue.
Conclusion: The solubility of voriconazole was greatly improved, it showed higher bioavailability and safety, and the interindividual variability in voriconazole pharmacokinetics was reduced by nanospray drying. |
| doi_str_mv | 10.1080/10837450.2020.1741618 |
| format | Article |
| fullrecord | <record><control><sourceid>pubmed_cross</sourceid><recordid>TN_cdi_crossref_primary_10_1080_10837450_2020_1741618</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>32178565</sourcerecordid><originalsourceid>FETCH-LOGICAL-c366t-d0b6d3d84e328b21752bfc049a9c8b256f79e89846be0ed8a1e0c6973c655d283</originalsourceid><addsrcrecordid>eNp9kN9OwyAUxonRuDl9BE1foBNKoXCnWZwzWeKNXhMKNGI6aKBz6Z5emm5eenP-5fvOOfkBcI_gEkEGH1PAVUngsoBFGlUloohdgDmCvMo5o9XlWDOcj6IZuInxG0LEOCTXYIYLVDFCyRxs1j7s9q3srXeZdDpTXzJI1Ztgj9PQN9mPD1Z5J4--NZmTzscuyCHTwRqddf6gTYi34KqRbTR3p7wAn-uXj9Um376_vq2et7nClPa5hjXVWLPS4ILV6Q1S1I2CJZdcpZ7QpuKGcVbS2kCjmUQGKsorrCghumB4Aci0VwUfYzCN6ILdyTAIBMVIRpzJiJGMOJFJvofJ1-3rndF_rjOKJHiaBNY1iYk8-NBq0cuh9aEJ0ikbBf7_xi8IDXOi</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Formulation and characterization of voriconazole nanospray dried powders</title><source>MEDLINE</source><source>EBSCOhost Business Source Complete</source><creator>Chen, Rui ; Zhang, Tinghua ; Bao, Sha ; Liu, Yinkun ; Xu, Xiaohong</creator><creatorcontrib>Chen, Rui ; Zhang, Tinghua ; Bao, Sha ; Liu, Yinkun ; Xu, Xiaohong</creatorcontrib><description>Purpose: Voriconazole nanoparticles (API-NPs) were prepared by nanospray drying to improve the solubility of voriconazole and reduce its interindividual variability.
Methods: The preparation procedure was optimized by central composite design-response surface methodology. The properties of the nanoparticles were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analyses. The solubility, dissolution, and stability of the API-NPs were determined experimentally. The pharmacokinetics were assessed based on rat plasma levels of voriconazole. An acute oral toxicity test of the API-NPs was performed in mice.
Results: The powers were formulated using cetyltrimethylammonium chloride (CTAC) as the carrier material. SEM and particle size results showed that the API-NPs had a narrow particle size distribution. The XRD, DSC, and FTIR analyses show a decrease in crystallinity and a polymorphic transformation of the nanoparticles after nanospray drying. The solubility in water was approximately 15 times higher than that of voriconazole. The API-NP tablets exhibited significantly higher plasma exposure, namely, longer acting times and lower variability. The acute administration of voriconazole showed no toxic histopathological effects on organ tissue.
Conclusion: The solubility of voriconazole was greatly improved, it showed higher bioavailability and safety, and the interindividual variability in voriconazole pharmacokinetics was reduced by nanospray drying.</description><identifier>ISSN: 1083-7450</identifier><identifier>EISSN: 1097-9867</identifier><identifier>DOI: 10.1080/10837450.2020.1741618</identifier><identifier>PMID: 32178565</identifier><language>eng</language><publisher>England: Taylor & Francis</publisher><subject>Animals ; Antifungal Agents - chemical synthesis ; Antifungal Agents - pharmacology ; Antifungal Agents - toxicity ; dissolution behavior ; Drug Compounding - methods ; interindividual variability ; Mice ; Nanoparticles - chemistry ; Nanoparticles - metabolism ; Nanoparticles - toxicity ; nanospray drying ; pharmacokinetic ; Powders ; Random Allocation ; Rats ; Rats, Wistar ; Toxicity Tests, Acute - methods ; Voriconazole ; Voriconazole - chemical synthesis ; Voriconazole - pharmacokinetics ; Voriconazole - toxicity ; X-Ray Diffraction - methods</subject><ispartof>Pharmaceutical development and technology, 2020-08, Vol.25 (7), p.815-822</ispartof><rights>2020 Informa UK Limited, trading as Taylor & Francis Group 2020</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c366t-d0b6d3d84e328b21752bfc049a9c8b256f79e89846be0ed8a1e0c6973c655d283</citedby><cites>FETCH-LOGICAL-c366t-d0b6d3d84e328b21752bfc049a9c8b256f79e89846be0ed8a1e0c6973c655d283</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/32178565$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chen, Rui</creatorcontrib><creatorcontrib>Zhang, Tinghua</creatorcontrib><creatorcontrib>Bao, Sha</creatorcontrib><creatorcontrib>Liu, Yinkun</creatorcontrib><creatorcontrib>Xu, Xiaohong</creatorcontrib><title>Formulation and characterization of voriconazole nanospray dried powders</title><title>Pharmaceutical development and technology</title><addtitle>Pharm Dev Technol</addtitle><description>Purpose: Voriconazole nanoparticles (API-NPs) were prepared by nanospray drying to improve the solubility of voriconazole and reduce its interindividual variability.
Methods: The preparation procedure was optimized by central composite design-response surface methodology. The properties of the nanoparticles were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analyses. The solubility, dissolution, and stability of the API-NPs were determined experimentally. The pharmacokinetics were assessed based on rat plasma levels of voriconazole. An acute oral toxicity test of the API-NPs was performed in mice.
Results: The powers were formulated using cetyltrimethylammonium chloride (CTAC) as the carrier material. SEM and particle size results showed that the API-NPs had a narrow particle size distribution. The XRD, DSC, and FTIR analyses show a decrease in crystallinity and a polymorphic transformation of the nanoparticles after nanospray drying. The solubility in water was approximately 15 times higher than that of voriconazole. The API-NP tablets exhibited significantly higher plasma exposure, namely, longer acting times and lower variability. The acute administration of voriconazole showed no toxic histopathological effects on organ tissue.
Conclusion: The solubility of voriconazole was greatly improved, it showed higher bioavailability and safety, and the interindividual variability in voriconazole pharmacokinetics was reduced by nanospray drying.</description><subject>Animals</subject><subject>Antifungal Agents - chemical synthesis</subject><subject>Antifungal Agents - pharmacology</subject><subject>Antifungal Agents - toxicity</subject><subject>dissolution behavior</subject><subject>Drug Compounding - methods</subject><subject>interindividual variability</subject><subject>Mice</subject><subject>Nanoparticles - chemistry</subject><subject>Nanoparticles - metabolism</subject><subject>Nanoparticles - toxicity</subject><subject>nanospray drying</subject><subject>pharmacokinetic</subject><subject>Powders</subject><subject>Random Allocation</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Toxicity Tests, Acute - methods</subject><subject>Voriconazole</subject><subject>Voriconazole - chemical synthesis</subject><subject>Voriconazole - pharmacokinetics</subject><subject>Voriconazole - toxicity</subject><subject>X-Ray Diffraction - methods</subject><issn>1083-7450</issn><issn>1097-9867</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kN9OwyAUxonRuDl9BE1foBNKoXCnWZwzWeKNXhMKNGI6aKBz6Z5emm5eenP-5fvOOfkBcI_gEkEGH1PAVUngsoBFGlUloohdgDmCvMo5o9XlWDOcj6IZuInxG0LEOCTXYIYLVDFCyRxs1j7s9q3srXeZdDpTXzJI1Ztgj9PQN9mPD1Z5J4--NZmTzscuyCHTwRqddf6gTYi34KqRbTR3p7wAn-uXj9Um376_vq2et7nClPa5hjXVWLPS4ILV6Q1S1I2CJZdcpZ7QpuKGcVbS2kCjmUQGKsorrCghumB4Aci0VwUfYzCN6ILdyTAIBMVIRpzJiJGMOJFJvofJ1-3rndF_rjOKJHiaBNY1iYk8-NBq0cuh9aEJ0ikbBf7_xi8IDXOi</recordid><startdate>20200808</startdate><enddate>20200808</enddate><creator>Chen, Rui</creator><creator>Zhang, Tinghua</creator><creator>Bao, Sha</creator><creator>Liu, Yinkun</creator><creator>Xu, Xiaohong</creator><general>Taylor & Francis</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></search><sort><creationdate>20200808</creationdate><title>Formulation and characterization of voriconazole nanospray dried powders</title><author>Chen, Rui ; Zhang, Tinghua ; Bao, Sha ; Liu, Yinkun ; Xu, Xiaohong</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c366t-d0b6d3d84e328b21752bfc049a9c8b256f79e89846be0ed8a1e0c6973c655d283</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>Animals</topic><topic>Antifungal Agents - chemical synthesis</topic><topic>Antifungal Agents - pharmacology</topic><topic>Antifungal Agents - toxicity</topic><topic>dissolution behavior</topic><topic>Drug Compounding - methods</topic><topic>interindividual variability</topic><topic>Mice</topic><topic>Nanoparticles - chemistry</topic><topic>Nanoparticles - metabolism</topic><topic>Nanoparticles - toxicity</topic><topic>nanospray drying</topic><topic>pharmacokinetic</topic><topic>Powders</topic><topic>Random Allocation</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Toxicity Tests, Acute - methods</topic><topic>Voriconazole</topic><topic>Voriconazole - chemical synthesis</topic><topic>Voriconazole - pharmacokinetics</topic><topic>Voriconazole - toxicity</topic><topic>X-Ray Diffraction - methods</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chen, Rui</creatorcontrib><creatorcontrib>Zhang, Tinghua</creatorcontrib><creatorcontrib>Bao, Sha</creatorcontrib><creatorcontrib>Liu, Yinkun</creatorcontrib><creatorcontrib>Xu, Xiaohong</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Pharmaceutical development and technology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chen, Rui</au><au>Zhang, Tinghua</au><au>Bao, Sha</au><au>Liu, Yinkun</au><au>Xu, Xiaohong</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Formulation and characterization of voriconazole nanospray dried powders</atitle><jtitle>Pharmaceutical development and technology</jtitle><addtitle>Pharm Dev Technol</addtitle><date>2020-08-08</date><risdate>2020</risdate><volume>25</volume><issue>7</issue><spage>815</spage><epage>822</epage><pages>815-822</pages><issn>1083-7450</issn><eissn>1097-9867</eissn><abstract>Purpose: Voriconazole nanoparticles (API-NPs) were prepared by nanospray drying to improve the solubility of voriconazole and reduce its interindividual variability.
Methods: The preparation procedure was optimized by central composite design-response surface methodology. The properties of the nanoparticles were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analyses. The solubility, dissolution, and stability of the API-NPs were determined experimentally. The pharmacokinetics were assessed based on rat plasma levels of voriconazole. An acute oral toxicity test of the API-NPs was performed in mice.
Results: The powers were formulated using cetyltrimethylammonium chloride (CTAC) as the carrier material. SEM and particle size results showed that the API-NPs had a narrow particle size distribution. The XRD, DSC, and FTIR analyses show a decrease in crystallinity and a polymorphic transformation of the nanoparticles after nanospray drying. The solubility in water was approximately 15 times higher than that of voriconazole. The API-NP tablets exhibited significantly higher plasma exposure, namely, longer acting times and lower variability. The acute administration of voriconazole showed no toxic histopathological effects on organ tissue.
Conclusion: The solubility of voriconazole was greatly improved, it showed higher bioavailability and safety, and the interindividual variability in voriconazole pharmacokinetics was reduced by nanospray drying.</abstract><cop>England</cop><pub>Taylor & Francis</pub><pmid>32178565</pmid><doi>10.1080/10837450.2020.1741618</doi><tpages>8</tpages></addata></record> |
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| subjects | Animals Antifungal Agents - chemical synthesis Antifungal Agents - pharmacology Antifungal Agents - toxicity dissolution behavior Drug Compounding - methods interindividual variability Mice Nanoparticles - chemistry Nanoparticles - metabolism Nanoparticles - toxicity nanospray drying pharmacokinetic Powders Random Allocation Rats Rats, Wistar Toxicity Tests, Acute - methods Voriconazole Voriconazole - chemical synthesis Voriconazole - pharmacokinetics Voriconazole - toxicity X-Ray Diffraction - methods |
| title | Formulation and characterization of voriconazole nanospray dried powders |
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