Effects of Particle Size and Surface Modification on Cellular Uptake and Biodistribution of Polymeric Nanoparticles for Drug Delivery
ABSTRACT Purpose To investigate the effects of the particle size and surface coating on the cellular uptake of the polymeric nanoparticles for drug delivery across the physiological drug barrier with emphasis on the gastrointestinal (GI) barrier for oral chemotherapy and the blood–brain barrier (BBB...
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| Veröffentlicht in: | Pharmaceutical research 2013-10, Vol.30 (10), p.2512-2522 |
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| creator | Kulkarni, Sneha A. Feng, Si-Shen |
| description | ABSTRACT
Purpose
To investigate the effects of the particle size and surface coating on the cellular uptake of the polymeric nanoparticles for drug delivery across the physiological drug barrier with emphasis on the gastrointestinal (GI) barrier for oral chemotherapy and the blood–brain barrier (BBB) for imaging and therapy of brain cancer.
Methods
Various sizes of commercial fluorescent polystyrene nanoparticles (PS NPs) (
viz
20 50, 100, 200 and 500 nm) were modified with the d-α-tocopheryl polyethylene glycol 1,000 succinate (vitamin E TPGS or TPGS). The size, surface charge and surface morphology of PS NPs before and after TPGS modification were characterized. The Caco-2 and MDCK cells were employed as an
in vitro
model of the GI barrier for oral and the BBB for drug delivery into the central nerve system respectively. The distribution of fluorescent NPs after
i.v.
administration to rats was analyzed by the high performance liquid chromatography (HPLC).
Results
The
in vitro
investigation showed enhanced cellular uptake efficiency for PS NPs in both of Caco-2 and MDCK cells after TPGS surface coating.
In vivo
investigation showed that the particle size and surface coating are the two parameters which can dramatically influence the NPs biodistribution after
intravenous
administration. The TPGS coated NPs of smaller size (< 200 nm) can escape from recognition by the reticuloendothelial system (RES) and thus prolong the half-life of the NPs in the blood system.
Conclusions
TPGS-coated PS NPs of 100 and 200 nm sizes have potential to deliver the drug across the GI barrier and the BBB. |
| doi_str_mv | 10.1007/s11095-012-0958-3 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_journals_1434120207</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>3077272401</sourcerecordid><originalsourceid>FETCH-LOGICAL-c438t-dd4de636de03e46d0586aeac2360bb3daefbd7e21f11f7539b6bcc1e267476433</originalsourceid><addsrcrecordid>eNp1kEFrFDEUgIModq3-AC8S6Hk0L8lOZo7tttpCW4Va8BYyyUtJnZ1sk5nCeu__NsuspRch8A753vfgI-QjsM_AmPqSAVi7rBjwqsymEq_IApZKVC2Tv16TBVNcVo2ScEDe5XzPGGuglW_JARcCZCvEgjydeY92zDR6-sOkMdge6U34g9QMjt5MyRuL9Cq64IM1Y4gDLW-FfT_1JtHbzWh-z-xJKFAeU-imGSvC2G_XmIKl12aIm70-Ux8TPU3THT3FPjxi2r4nb7zpM37Yz0Ny-_Xs5-q8uvz-7WJ1fFlZKZqxck46rEXtkAmUtWPLpjZoLBc16zrhDPrOKeTgAbxairarO2sBea2kqqUQh-Ro9m5SfJgwj_o-TmkoJzVIIYEzzlShYKZsijkn9HqTwtqkrQamd-H1HF6X8HoXXu_Mn_bmqVuje974V7oAfAZy-RruML04_V_rXwf4kA0</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>1434120207</pqid></control><display><type>article</type><title>Effects of Particle Size and Surface Modification on Cellular Uptake and Biodistribution of Polymeric Nanoparticles for Drug Delivery</title><source>MEDLINE</source><source>SpringerLink Journals - AutoHoldings</source><creator>Kulkarni, Sneha A. ; Feng, Si-Shen</creator><creatorcontrib>Kulkarni, Sneha A. ; Feng, Si-Shen</creatorcontrib><description>ABSTRACT
Purpose
To investigate the effects of the particle size and surface coating on the cellular uptake of the polymeric nanoparticles for drug delivery across the physiological drug barrier with emphasis on the gastrointestinal (GI) barrier for oral chemotherapy and the blood–brain barrier (BBB) for imaging and therapy of brain cancer.
Methods
Various sizes of commercial fluorescent polystyrene nanoparticles (PS NPs) (
viz
20 50, 100, 200 and 500 nm) were modified with the d-α-tocopheryl polyethylene glycol 1,000 succinate (vitamin E TPGS or TPGS). The size, surface charge and surface morphology of PS NPs before and after TPGS modification were characterized. The Caco-2 and MDCK cells were employed as an
in vitro
model of the GI barrier for oral and the BBB for drug delivery into the central nerve system respectively. The distribution of fluorescent NPs after
i.v.
administration to rats was analyzed by the high performance liquid chromatography (HPLC).
Results
The
in vitro
investigation showed enhanced cellular uptake efficiency for PS NPs in both of Caco-2 and MDCK cells after TPGS surface coating.
In vivo
investigation showed that the particle size and surface coating are the two parameters which can dramatically influence the NPs biodistribution after
intravenous
administration. The TPGS coated NPs of smaller size (< 200 nm) can escape from recognition by the reticuloendothelial system (RES) and thus prolong the half-life of the NPs in the blood system.
Conclusions
TPGS-coated PS NPs of 100 and 200 nm sizes have potential to deliver the drug across the GI barrier and the BBB.</description><identifier>ISSN: 0724-8741</identifier><identifier>EISSN: 1573-904X</identifier><identifier>DOI: 10.1007/s11095-012-0958-3</identifier><identifier>PMID: 23314933</identifier><language>eng</language><publisher>Boston: Springer US</publisher><subject>Administration, Oral ; Animals ; Biochemistry ; Biodegradable materials ; Biomedical and Life Sciences ; Biomedical Engineering and Bioengineering ; Biomedicine ; Blood-brain barrier ; Blood-Brain Barrier - metabolism ; Caco-2 Cells ; Chemotherapy ; Chromatography, High Pressure Liquid ; Dogs ; Drug Carriers - chemistry ; Drug Carriers - pharmacokinetics ; Drug delivery systems ; Drug Delivery Systems - methods ; Endocytosis - physiology ; Fluorescent Dyes - chemistry ; Gastrointestinal Tract - metabolism ; Humans ; Madin Darby Canine Kidney Cells ; Male ; Medical Law ; Nanoparticles - chemistry ; Nanotechnology ; Particle Size ; Pharmacology/Toxicology ; Pharmacy ; Polyethylene Glycols - chemistry ; Polyethylene Glycols - pharmacokinetics ; Polystyrenes - chemistry ; Polystyrenes - pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Research Paper ; Surface Properties ; Tissue Distribution ; Vitamin E - analogs & derivatives ; Vitamin E - chemistry ; Vitamin E - pharmacokinetics</subject><ispartof>Pharmaceutical research, 2013-10, Vol.30 (10), p.2512-2522</ispartof><rights>Springer Science+Business Media New York 2013</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c438t-dd4de636de03e46d0586aeac2360bb3daefbd7e21f11f7539b6bcc1e267476433</citedby><cites>FETCH-LOGICAL-c438t-dd4de636de03e46d0586aeac2360bb3daefbd7e21f11f7539b6bcc1e267476433</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/s11095-012-0958-3$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s11095-012-0958-3$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,780,784,27923,27924,41487,42556,51318</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23314933$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kulkarni, Sneha A.</creatorcontrib><creatorcontrib>Feng, Si-Shen</creatorcontrib><title>Effects of Particle Size and Surface Modification on Cellular Uptake and Biodistribution of Polymeric Nanoparticles for Drug Delivery</title><title>Pharmaceutical research</title><addtitle>Pharm Res</addtitle><addtitle>Pharm Res</addtitle><description>ABSTRACT
Purpose
To investigate the effects of the particle size and surface coating on the cellular uptake of the polymeric nanoparticles for drug delivery across the physiological drug barrier with emphasis on the gastrointestinal (GI) barrier for oral chemotherapy and the blood–brain barrier (BBB) for imaging and therapy of brain cancer.
Methods
Various sizes of commercial fluorescent polystyrene nanoparticles (PS NPs) (
viz
20 50, 100, 200 and 500 nm) were modified with the d-α-tocopheryl polyethylene glycol 1,000 succinate (vitamin E TPGS or TPGS). The size, surface charge and surface morphology of PS NPs before and after TPGS modification were characterized. The Caco-2 and MDCK cells were employed as an
in vitro
model of the GI barrier for oral and the BBB for drug delivery into the central nerve system respectively. The distribution of fluorescent NPs after
i.v.
administration to rats was analyzed by the high performance liquid chromatography (HPLC).
Results
The
in vitro
investigation showed enhanced cellular uptake efficiency for PS NPs in both of Caco-2 and MDCK cells after TPGS surface coating.
In vivo
investigation showed that the particle size and surface coating are the two parameters which can dramatically influence the NPs biodistribution after
intravenous
administration. The TPGS coated NPs of smaller size (< 200 nm) can escape from recognition by the reticuloendothelial system (RES) and thus prolong the half-life of the NPs in the blood system.
Conclusions
TPGS-coated PS NPs of 100 and 200 nm sizes have potential to deliver the drug across the GI barrier and the BBB.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Biochemistry</subject><subject>Biodegradable materials</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedical Engineering and Bioengineering</subject><subject>Biomedicine</subject><subject>Blood-brain barrier</subject><subject>Blood-Brain Barrier - metabolism</subject><subject>Caco-2 Cells</subject><subject>Chemotherapy</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Dogs</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Carriers - pharmacokinetics</subject><subject>Drug delivery systems</subject><subject>Drug Delivery Systems - methods</subject><subject>Endocytosis - physiology</subject><subject>Fluorescent Dyes - chemistry</subject><subject>Gastrointestinal Tract - metabolism</subject><subject>Humans</subject><subject>Madin Darby Canine Kidney Cells</subject><subject>Male</subject><subject>Medical Law</subject><subject>Nanoparticles - chemistry</subject><subject>Nanotechnology</subject><subject>Particle Size</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Polyethylene Glycols - chemistry</subject><subject>Polyethylene Glycols - pharmacokinetics</subject><subject>Polystyrenes - chemistry</subject><subject>Polystyrenes - pharmacokinetics</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Research Paper</subject><subject>Surface Properties</subject><subject>Tissue Distribution</subject><subject>Vitamin E - analogs & derivatives</subject><subject>Vitamin E - chemistry</subject><subject>Vitamin E - pharmacokinetics</subject><issn>0724-8741</issn><issn>1573-904X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><recordid>eNp1kEFrFDEUgIModq3-AC8S6Hk0L8lOZo7tttpCW4Va8BYyyUtJnZ1sk5nCeu__NsuspRch8A753vfgI-QjsM_AmPqSAVi7rBjwqsymEq_IApZKVC2Tv16TBVNcVo2ScEDe5XzPGGuglW_JARcCZCvEgjydeY92zDR6-sOkMdge6U34g9QMjt5MyRuL9Cq64IM1Y4gDLW-FfT_1JtHbzWh-z-xJKFAeU-imGSvC2G_XmIKl12aIm70-Ux8TPU3THT3FPjxi2r4nb7zpM37Yz0Ny-_Xs5-q8uvz-7WJ1fFlZKZqxck46rEXtkAmUtWPLpjZoLBc16zrhDPrOKeTgAbxairarO2sBea2kqqUQh-Ro9m5SfJgwj_o-TmkoJzVIIYEzzlShYKZsijkn9HqTwtqkrQamd-H1HF6X8HoXXu_Mn_bmqVuje974V7oAfAZy-RruML04_V_rXwf4kA0</recordid><startdate>20131001</startdate><enddate>20131001</enddate><creator>Kulkarni, Sneha A.</creator><creator>Feng, Si-Shen</creator><general>Springer US</general><general>Springer Nature 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>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>20131001</creationdate><title>Effects of Particle Size and Surface Modification on Cellular Uptake and Biodistribution of Polymeric Nanoparticles for Drug Delivery</title><author>Kulkarni, Sneha A. ; Feng, Si-Shen</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c438t-dd4de636de03e46d0586aeac2360bb3daefbd7e21f11f7539b6bcc1e267476433</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Biochemistry</topic><topic>Biodegradable materials</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedical Engineering and Bioengineering</topic><topic>Biomedicine</topic><topic>Blood-brain barrier</topic><topic>Blood-Brain Barrier - metabolism</topic><topic>Caco-2 Cells</topic><topic>Chemotherapy</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Dogs</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Carriers - pharmacokinetics</topic><topic>Drug delivery systems</topic><topic>Drug Delivery Systems - methods</topic><topic>Endocytosis - physiology</topic><topic>Fluorescent Dyes - chemistry</topic><topic>Gastrointestinal Tract - metabolism</topic><topic>Humans</topic><topic>Madin Darby Canine Kidney Cells</topic><topic>Male</topic><topic>Medical Law</topic><topic>Nanoparticles - chemistry</topic><topic>Nanotechnology</topic><topic>Particle Size</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Polyethylene Glycols - chemistry</topic><topic>Polyethylene Glycols - pharmacokinetics</topic><topic>Polystyrenes - chemistry</topic><topic>Polystyrenes - pharmacokinetics</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Research Paper</topic><topic>Surface Properties</topic><topic>Tissue Distribution</topic><topic>Vitamin E - analogs & derivatives</topic><topic>Vitamin E - chemistry</topic><topic>Vitamin E - pharmacokinetics</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kulkarni, Sneha A.</creatorcontrib><creatorcontrib>Feng, Si-Shen</creatorcontrib><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>Kulkarni, Sneha A.</au><au>Feng, Si-Shen</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effects of Particle Size and Surface Modification on Cellular Uptake and Biodistribution of Polymeric Nanoparticles for Drug Delivery</atitle><jtitle>Pharmaceutical research</jtitle><stitle>Pharm Res</stitle><addtitle>Pharm Res</addtitle><date>2013-10-01</date><risdate>2013</risdate><volume>30</volume><issue>10</issue><spage>2512</spage><epage>2522</epage><pages>2512-2522</pages><issn>0724-8741</issn><eissn>1573-904X</eissn><abstract>ABSTRACT
Purpose
To investigate the effects of the particle size and surface coating on the cellular uptake of the polymeric nanoparticles for drug delivery across the physiological drug barrier with emphasis on the gastrointestinal (GI) barrier for oral chemotherapy and the blood–brain barrier (BBB) for imaging and therapy of brain cancer.
Methods
Various sizes of commercial fluorescent polystyrene nanoparticles (PS NPs) (
viz
20 50, 100, 200 and 500 nm) were modified with the d-α-tocopheryl polyethylene glycol 1,000 succinate (vitamin E TPGS or TPGS). The size, surface charge and surface morphology of PS NPs before and after TPGS modification were characterized. The Caco-2 and MDCK cells were employed as an
in vitro
model of the GI barrier for oral and the BBB for drug delivery into the central nerve system respectively. The distribution of fluorescent NPs after
i.v.
administration to rats was analyzed by the high performance liquid chromatography (HPLC).
Results
The
in vitro
investigation showed enhanced cellular uptake efficiency for PS NPs in both of Caco-2 and MDCK cells after TPGS surface coating.
In vivo
investigation showed that the particle size and surface coating are the two parameters which can dramatically influence the NPs biodistribution after
intravenous
administration. The TPGS coated NPs of smaller size (< 200 nm) can escape from recognition by the reticuloendothelial system (RES) and thus prolong the half-life of the NPs in the blood system.
Conclusions
TPGS-coated PS NPs of 100 and 200 nm sizes have potential to deliver the drug across the GI barrier and the BBB.</abstract><cop>Boston</cop><pub>Springer US</pub><pmid>23314933</pmid><doi>10.1007/s11095-012-0958-3</doi><tpages>11</tpages></addata></record> |
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| identifier | ISSN: 0724-8741 |
| ispartof | Pharmaceutical research, 2013-10, Vol.30 (10), p.2512-2522 |
| issn | 0724-8741 1573-904X |
| language | eng |
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| source | MEDLINE; SpringerLink Journals - AutoHoldings |
| subjects | Administration, Oral Animals Biochemistry Biodegradable materials Biomedical and Life Sciences Biomedical Engineering and Bioengineering Biomedicine Blood-brain barrier Blood-Brain Barrier - metabolism Caco-2 Cells Chemotherapy Chromatography, High Pressure Liquid Dogs Drug Carriers - chemistry Drug Carriers - pharmacokinetics Drug delivery systems Drug Delivery Systems - methods Endocytosis - physiology Fluorescent Dyes - chemistry Gastrointestinal Tract - metabolism Humans Madin Darby Canine Kidney Cells Male Medical Law Nanoparticles - chemistry Nanotechnology Particle Size Pharmacology/Toxicology Pharmacy Polyethylene Glycols - chemistry Polyethylene Glycols - pharmacokinetics Polystyrenes - chemistry Polystyrenes - pharmacokinetics Rats Rats, Sprague-Dawley Research Paper Surface Properties Tissue Distribution Vitamin E - analogs & derivatives Vitamin E - chemistry Vitamin E - pharmacokinetics |
| title | Effects of Particle Size and Surface Modification on Cellular Uptake and Biodistribution of Polymeric Nanoparticles for Drug Delivery |
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