Development of a New Method to Assess Nanocrystal Dissolution Based on Light Scattering
ABSTRACT Purpose Nanocrystals exhibit enhanced dissolution rates and can effectively increase the bioavailability of poorly water soluble drug substances. However, methods for in vitro characterization of dissolution are unavailable. The objective of this study was to develop an in situ noninvasive...
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| Veröffentlicht in: | Pharmaceutical research 2012-10, Vol.29 (10), p.2887-2901 |
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| creator | Anhalt, Katharina Geissler, Simon Harms, Meike Weigandt, Markus Fricker, Gert |
| description | ABSTRACT
Purpose
Nanocrystals exhibit enhanced dissolution rates and can effectively increase the bioavailability of poorly water soluble drug substances. However, methods for
in vitro
characterization of dissolution are unavailable. The objective of this study was to develop an
in situ
noninvasive analytical method to measure dissolution of crystalline nanosuspensions based on light scattering.
Methods
Fenofibrate nanosuspensions were prepared by wet media milling. Their solubilities and dissolution profiles in simulated gastric fluid supplemented with 0.1% Tween
®
80 were measured in a small scale setup with an instrument for dynamic light scattering and the intensity of scattered light as readout parameter.
Results
A good correlation was achieved between the dissolution profile of a nanosuspension measured in the light scattering setup and a conventional dissolution experiment. Nanosuspensions of 120–270 nm size could be distinguished by the light scattering method. The suspensions dissolved within 1.9–12.3 min. Over a concentration range of 40–87% of the solubility dissolution profiles of a nanosuspension with 140 nm were monitored and the determined total dissolution times were in good agreement with the Noyes-Whitney dissolution model.
Conclusions
A noninvasive, sensitive and reproducible method is presented to assess nanocrystal dissolution.
In situ
measurements based on light scattering allow a straightforward experimental setup with high temporal resolution. |
| doi_str_mv | 10.1007/s11095-012-0795-4 |
| format | Article |
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Purpose
Nanocrystals exhibit enhanced dissolution rates and can effectively increase the bioavailability of poorly water soluble drug substances. However, methods for
in vitro
characterization of dissolution are unavailable. The objective of this study was to develop an
in situ
noninvasive analytical method to measure dissolution of crystalline nanosuspensions based on light scattering.
Methods
Fenofibrate nanosuspensions were prepared by wet media milling. Their solubilities and dissolution profiles in simulated gastric fluid supplemented with 0.1% Tween
®
80 were measured in a small scale setup with an instrument for dynamic light scattering and the intensity of scattered light as readout parameter.
Results
A good correlation was achieved between the dissolution profile of a nanosuspension measured in the light scattering setup and a conventional dissolution experiment. Nanosuspensions of 120–270 nm size could be distinguished by the light scattering method. The suspensions dissolved within 1.9–12.3 min. Over a concentration range of 40–87% of the solubility dissolution profiles of a nanosuspension with 140 nm were monitored and the determined total dissolution times were in good agreement with the Noyes-Whitney dissolution model.
Conclusions
A noninvasive, sensitive and reproducible method is presented to assess nanocrystal dissolution.
In situ
measurements based on light scattering allow a straightforward experimental setup with high temporal resolution.</description><identifier>ISSN: 0724-8741</identifier><identifier>EISSN: 1573-904X</identifier><identifier>DOI: 10.1007/s11095-012-0795-4</identifier><identifier>PMID: 22688901</identifier><identifier>CODEN: PHREEB</identifier><language>eng</language><publisher>Boston: Springer US</publisher><subject>Bioavailability ; Biochemistry ; Biological and medical sciences ; Biological Availability ; Biomedical and Life Sciences ; Biomedical Engineering and Bioengineering ; Biomedicine ; Dissolution ; Fenofibrate - chemistry ; General pharmacology ; Light ; Medical Law ; Medical sciences ; Nanocrystals ; Nanoparticles - chemistry ; Particle Size ; Pharmaceutical sciences ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Pharmacology/Toxicology ; Pharmacy ; Research Paper ; Scattering ; Scattering, Radiation ; Solubility ; Suspensions - chemistry ; Technology, Pharmaceutical - methods ; Water - chemistry</subject><ispartof>Pharmaceutical research, 2012-10, Vol.29 (10), p.2887-2901</ispartof><rights>Springer Science+Business Media, LLC 2012</rights><rights>2015 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c402t-62e7d37bce9b1494923fd4625305cf081243810e65d994c8614e82f6d550126d3</citedby><cites>FETCH-LOGICAL-c402t-62e7d37bce9b1494923fd4625305cf081243810e65d994c8614e82f6d550126d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s11095-012-0795-4$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s11095-012-0795-4$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>315,781,785,27926,27927,41490,42559,51321</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=26569753$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22688901$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Anhalt, Katharina</creatorcontrib><creatorcontrib>Geissler, Simon</creatorcontrib><creatorcontrib>Harms, Meike</creatorcontrib><creatorcontrib>Weigandt, Markus</creatorcontrib><creatorcontrib>Fricker, Gert</creatorcontrib><title>Development of a New Method to Assess Nanocrystal Dissolution Based on Light Scattering</title><title>Pharmaceutical research</title><addtitle>Pharm Res</addtitle><addtitle>Pharm Res</addtitle><description>ABSTRACT
Purpose
Nanocrystals exhibit enhanced dissolution rates and can effectively increase the bioavailability of poorly water soluble drug substances. However, methods for
in vitro
characterization of dissolution are unavailable. The objective of this study was to develop an
in situ
noninvasive analytical method to measure dissolution of crystalline nanosuspensions based on light scattering.
Methods
Fenofibrate nanosuspensions were prepared by wet media milling. Their solubilities and dissolution profiles in simulated gastric fluid supplemented with 0.1% Tween
®
80 were measured in a small scale setup with an instrument for dynamic light scattering and the intensity of scattered light as readout parameter.
Results
A good correlation was achieved between the dissolution profile of a nanosuspension measured in the light scattering setup and a conventional dissolution experiment. Nanosuspensions of 120–270 nm size could be distinguished by the light scattering method. The suspensions dissolved within 1.9–12.3 min. Over a concentration range of 40–87% of the solubility dissolution profiles of a nanosuspension with 140 nm were monitored and the determined total dissolution times were in good agreement with the Noyes-Whitney dissolution model.
Conclusions
A noninvasive, sensitive and reproducible method is presented to assess nanocrystal dissolution.
In situ
measurements based on light scattering allow a straightforward experimental setup with high temporal resolution.</description><subject>Bioavailability</subject><subject>Biochemistry</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedical Engineering and Bioengineering</subject><subject>Biomedicine</subject><subject>Dissolution</subject><subject>Fenofibrate - chemistry</subject><subject>General pharmacology</subject><subject>Light</subject><subject>Medical Law</subject><subject>Medical sciences</subject><subject>Nanocrystals</subject><subject>Nanoparticles - chemistry</subject><subject>Particle Size</subject><subject>Pharmaceutical sciences</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Research Paper</subject><subject>Scattering</subject><subject>Scattering, Radiation</subject><subject>Solubility</subject><subject>Suspensions - chemistry</subject><subject>Technology, Pharmaceutical - methods</subject><subject>Water - chemistry</subject><issn>0724-8741</issn><issn>1573-904X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><recordid>eNp1kE1P3DAQhi1EBVvgB3BBlhDHtGPHduIjX_2QFjjQCm6R15lAUDZePN5W_Hu82qXlwmnm8Mw7Mw9jhwK-CIDqKwkBVhcgZAFVbtQWmwhdlYUFdb_NJlBJVdSVErvsM9ETANTCqh22K6Wpawtiwu4u8A8OYTHHMfHQccev8S-_wvQYWp4CPyVCIn7txuDjCyU38IueKAzL1IeRnznCludm2j88Jn7rXUoY-_Fhn33q3EB4sKl77Pe3y1_nP4rpzfef56fTwiuQqTASq7asZh7tTCirrCy7VhmpS9C-y-dKVdYC0OjWWuVrIxTWsjOt1vlr05Z77Hidu4jheYmUmqewjGNe2QgorbAGapUpsaZ8DEQRu2YR-7mLLxlqViqbtcomhzYrlc1q5miTvJzNsf038eYuAycbwJF3Qxfd6Hv6zxltbKXLzMk1R4uVGYzvT_xo-ytRAImX</recordid><startdate>20121001</startdate><enddate>20121001</enddate><creator>Anhalt, Katharina</creator><creator>Geissler, Simon</creator><creator>Harms, Meike</creator><creator>Weigandt, Markus</creator><creator>Fricker, Gert</creator><general>Springer US</general><general>Springer</general><general>Springer Nature B.V</general><scope>IQODW</scope><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>3V.</scope><scope>7RV</scope><scope>7TK</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>K9.</scope><scope>KB0</scope><scope>M0S</scope><scope>M1P</scope><scope>NAPCQ</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope></search><sort><creationdate>20121001</creationdate><title>Development of a New Method to Assess Nanocrystal Dissolution Based on Light Scattering</title><author>Anhalt, Katharina ; Geissler, Simon ; Harms, Meike ; Weigandt, Markus ; Fricker, Gert</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c402t-62e7d37bce9b1494923fd4625305cf081243810e65d994c8614e82f6d550126d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Bioavailability</topic><topic>Biochemistry</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedical Engineering and Bioengineering</topic><topic>Biomedicine</topic><topic>Dissolution</topic><topic>Fenofibrate - chemistry</topic><topic>General pharmacology</topic><topic>Light</topic><topic>Medical Law</topic><topic>Medical sciences</topic><topic>Nanocrystals</topic><topic>Nanoparticles - chemistry</topic><topic>Particle Size</topic><topic>Pharmaceutical sciences</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Research Paper</topic><topic>Scattering</topic><topic>Scattering, Radiation</topic><topic>Solubility</topic><topic>Suspensions - chemistry</topic><topic>Technology, Pharmaceutical - methods</topic><topic>Water - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Anhalt, Katharina</creatorcontrib><creatorcontrib>Geissler, Simon</creatorcontrib><creatorcontrib>Harms, Meike</creatorcontrib><creatorcontrib>Weigandt, Markus</creatorcontrib><creatorcontrib>Fricker, Gert</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Nursing & Allied Health Database</collection><collection>Neurosciences Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Nursing & Allied Health Premium</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><jtitle>Pharmaceutical research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Anhalt, Katharina</au><au>Geissler, Simon</au><au>Harms, Meike</au><au>Weigandt, Markus</au><au>Fricker, Gert</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development of a New Method to Assess Nanocrystal Dissolution Based on Light Scattering</atitle><jtitle>Pharmaceutical research</jtitle><stitle>Pharm Res</stitle><addtitle>Pharm Res</addtitle><date>2012-10-01</date><risdate>2012</risdate><volume>29</volume><issue>10</issue><spage>2887</spage><epage>2901</epage><pages>2887-2901</pages><issn>0724-8741</issn><eissn>1573-904X</eissn><coden>PHREEB</coden><abstract>ABSTRACT
Purpose
Nanocrystals exhibit enhanced dissolution rates and can effectively increase the bioavailability of poorly water soluble drug substances. However, methods for
in vitro
characterization of dissolution are unavailable. The objective of this study was to develop an
in situ
noninvasive analytical method to measure dissolution of crystalline nanosuspensions based on light scattering.
Methods
Fenofibrate nanosuspensions were prepared by wet media milling. Their solubilities and dissolution profiles in simulated gastric fluid supplemented with 0.1% Tween
®
80 were measured in a small scale setup with an instrument for dynamic light scattering and the intensity of scattered light as readout parameter.
Results
A good correlation was achieved between the dissolution profile of a nanosuspension measured in the light scattering setup and a conventional dissolution experiment. Nanosuspensions of 120–270 nm size could be distinguished by the light scattering method. The suspensions dissolved within 1.9–12.3 min. Over a concentration range of 40–87% of the solubility dissolution profiles of a nanosuspension with 140 nm were monitored and the determined total dissolution times were in good agreement with the Noyes-Whitney dissolution model.
Conclusions
A noninvasive, sensitive and reproducible method is presented to assess nanocrystal dissolution.
In situ
measurements based on light scattering allow a straightforward experimental setup with high temporal resolution.</abstract><cop>Boston</cop><pub>Springer US</pub><pmid>22688901</pmid><doi>10.1007/s11095-012-0795-4</doi><tpages>15</tpages></addata></record> |
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| identifier | ISSN: 0724-8741 |
| ispartof | Pharmaceutical research, 2012-10, Vol.29 (10), p.2887-2901 |
| issn | 0724-8741 1573-904X |
| language | eng |
| recordid | cdi_proquest_journals_1039196084 |
| source | MEDLINE; SpringerNature Journals |
| subjects | Bioavailability Biochemistry Biological and medical sciences Biological Availability Biomedical and Life Sciences Biomedical Engineering and Bioengineering Biomedicine Dissolution Fenofibrate - chemistry General pharmacology Light Medical Law Medical sciences Nanocrystals Nanoparticles - chemistry Particle Size Pharmaceutical sciences Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Pharmacology/Toxicology Pharmacy Research Paper Scattering Scattering, Radiation Solubility Suspensions - chemistry Technology, Pharmaceutical - methods Water - chemistry |
| title | Development of a New Method to Assess Nanocrystal Dissolution Based on Light Scattering |
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