Indirect evidence that drug brain targeting using polysorbate 80-coated polybutylcyanoacrylate nanoparticles is related to toxicity
To investigate the mechanism underlying the entry of the analgesic peptide dalargin into brain using biodegradable polybutylcyanoacrylate (PBCA) nanoparticles (NP) overcoated with polysorbate 80. The investigations were carried out with PBCA NP and with non biodegradable polystyrene (PS) NP (200 nm...
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| Veröffentlicht in: | Pharmaceutical research 1999-12, Vol.16 (12), p.1836-1842 |
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| creator | OLIVIER, J.-C FENART, L CHAUVET, R PARIAT, C CECCHELLI, R COUET, W |
| description | To investigate the mechanism underlying the entry of the analgesic peptide dalargin into brain using biodegradable polybutylcyanoacrylate (PBCA) nanoparticles (NP) overcoated with polysorbate 80.
The investigations were carried out with PBCA NP and with non biodegradable polystyrene (PS) NP (200 nm diameter). Dalargin adsorption was assessed by HPLC. Its entry into the CNS in mice was evaluated using the tail-flick procedure. Locomotor activity measurements were performed to compare NP toxicities. BBB permeabilization by PBCA NP was studied in vitro using a coculture of bovine brain capillary endothelial cells and rat astrocytes.
Dalargin loading was 11.7 microg/mg on PBCA NP and 16.5 microg/ mg on PS NP. Adding polysorbate 80 to NP led to a complete desorption. Nevertheless, dalargin associated with PBCA NP and polysorbate 80 induced a potent and prolonged analgesia, which could not be obtained using PS NP in place of PBCA NP. Locomotor activity dramatically decreased in mice dosed with PBCA NP, but not with PS NP. PBCA NP also caused occasional mortality. In vitro, PBCA NP (10 microg/ml) induced a permeabilization of the BBB model.
A non specific permeabilization of the BBB, probably related to the toxicity of the carrier, may account for the CNS penetration of dalargin associated with PBCA NP and polysorbate 80. |
| doi_str_mv | 10.1023/A:1018947208597 |
| format | Article |
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The investigations were carried out with PBCA NP and with non biodegradable polystyrene (PS) NP (200 nm diameter). Dalargin adsorption was assessed by HPLC. Its entry into the CNS in mice was evaluated using the tail-flick procedure. Locomotor activity measurements were performed to compare NP toxicities. BBB permeabilization by PBCA NP was studied in vitro using a coculture of bovine brain capillary endothelial cells and rat astrocytes.
Dalargin loading was 11.7 microg/mg on PBCA NP and 16.5 microg/ mg on PS NP. Adding polysorbate 80 to NP led to a complete desorption. Nevertheless, dalargin associated with PBCA NP and polysorbate 80 induced a potent and prolonged analgesia, which could not be obtained using PS NP in place of PBCA NP. Locomotor activity dramatically decreased in mice dosed with PBCA NP, but not with PS NP. PBCA NP also caused occasional mortality. In vitro, PBCA NP (10 microg/ml) induced a permeabilization of the BBB model.
A non specific permeabilization of the BBB, probably related to the toxicity of the carrier, may account for the CNS penetration of dalargin associated with PBCA NP and polysorbate 80.</description><identifier>ISSN: 0724-8741</identifier><identifier>EISSN: 1573-904X</identifier><identifier>DOI: 10.1023/A:1018947208597</identifier><identifier>PMID: 10644071</identifier><identifier>CODEN: PHREEB</identifier><language>eng</language><publisher>New York, NY: Springer</publisher><subject><![CDATA[Analgesics ; Analgesics - administration & dosage ; Analgesics - toxicity ; Animals ; Biochemistry, Molecular Biology ; Biological and medical sciences ; Blood-Brain Barrier - drug effects ; Brain - metabolism ; Cells, Cultured ; Chromatography, High Pressure Liquid ; Enbucrilate - administration & dosage ; Enbucrilate - toxicity ; Endothelium - cytology ; Endothelium - metabolism ; Enkephalin, Leucine-2-Alanine - administration & dosage ; Enkephalin, Leucine-2-Alanine - analogs & derivatives ; Enkephalin, Leucine-2-Alanine - toxicity ; Excipients - administration & dosage ; Excipients - toxicity ; General pharmacology ; Life Sciences ; Male ; Medical sciences ; Mice ; Microspheres ; Motor Activity - drug effects ; Neuropharmacology ; Pain Measurement - drug effects ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Polysorbates - administration & dosage ; Polysorbates - toxicity]]></subject><ispartof>Pharmaceutical research, 1999-12, Vol.16 (12), p.1836-1842</ispartof><rights>2000 INIST-CNRS</rights><rights>Copyright Kluwer Academic Publishers Dec 1999</rights><rights>Distributed under a Creative Commons Attribution 4.0 International License</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c368t-f5bfb12d22b3092d2b66f44044774d7a5aa5dbfab19efc3892b31a5f2fc6100b3</citedby><orcidid>0000-0001-9285-0579</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,314,776,780,881,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1259250$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10644071$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://univ-artois.hal.science/hal-00534822$$DView record in HAL$$Hfree_for_read</backlink></links><search><creatorcontrib>OLIVIER, J.-C</creatorcontrib><creatorcontrib>FENART, L</creatorcontrib><creatorcontrib>CHAUVET, R</creatorcontrib><creatorcontrib>PARIAT, C</creatorcontrib><creatorcontrib>CECCHELLI, R</creatorcontrib><creatorcontrib>COUET, W</creatorcontrib><title>Indirect evidence that drug brain targeting using polysorbate 80-coated polybutylcyanoacrylate nanoparticles is related to toxicity</title><title>Pharmaceutical research</title><addtitle>Pharm Res</addtitle><description>To investigate the mechanism underlying the entry of the analgesic peptide dalargin into brain using biodegradable polybutylcyanoacrylate (PBCA) nanoparticles (NP) overcoated with polysorbate 80.
The investigations were carried out with PBCA NP and with non biodegradable polystyrene (PS) NP (200 nm diameter). Dalargin adsorption was assessed by HPLC. Its entry into the CNS in mice was evaluated using the tail-flick procedure. Locomotor activity measurements were performed to compare NP toxicities. BBB permeabilization by PBCA NP was studied in vitro using a coculture of bovine brain capillary endothelial cells and rat astrocytes.
Dalargin loading was 11.7 microg/mg on PBCA NP and 16.5 microg/ mg on PS NP. Adding polysorbate 80 to NP led to a complete desorption. Nevertheless, dalargin associated with PBCA NP and polysorbate 80 induced a potent and prolonged analgesia, which could not be obtained using PS NP in place of PBCA NP. Locomotor activity dramatically decreased in mice dosed with PBCA NP, but not with PS NP. PBCA NP also caused occasional mortality. In vitro, PBCA NP (10 microg/ml) induced a permeabilization of the BBB model.
A non specific permeabilization of the BBB, probably related to the toxicity of the carrier, may account for the CNS penetration of dalargin associated with PBCA NP and polysorbate 80.</description><subject>Analgesics</subject><subject>Analgesics - administration & dosage</subject><subject>Analgesics - toxicity</subject><subject>Animals</subject><subject>Biochemistry, Molecular Biology</subject><subject>Biological and medical sciences</subject><subject>Blood-Brain Barrier - drug effects</subject><subject>Brain - metabolism</subject><subject>Cells, Cultured</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Enbucrilate - administration & dosage</subject><subject>Enbucrilate - toxicity</subject><subject>Endothelium - cytology</subject><subject>Endothelium - metabolism</subject><subject>Enkephalin, Leucine-2-Alanine - administration & dosage</subject><subject>Enkephalin, Leucine-2-Alanine - analogs & derivatives</subject><subject>Enkephalin, Leucine-2-Alanine - toxicity</subject><subject>Excipients - administration & dosage</subject><subject>Excipients - toxicity</subject><subject>General pharmacology</subject><subject>Life Sciences</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Microspheres</subject><subject>Motor Activity - drug effects</subject><subject>Neuropharmacology</subject><subject>Pain Measurement - drug effects</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. 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Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Polysorbates - administration & dosage</topic><topic>Polysorbates - toxicity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>OLIVIER, J.-C</creatorcontrib><creatorcontrib>FENART, L</creatorcontrib><creatorcontrib>CHAUVET, R</creatorcontrib><creatorcontrib>PARIAT, C</creatorcontrib><creatorcontrib>CECCHELLI, R</creatorcontrib><creatorcontrib>COUET, W</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>ProQuest Central (Corporate)</collection><collection>Nursing & Allied Health Database</collection><collection>Neurosciences Abstracts</collection><collection>ProQuest - Health & Medical Complete保健、医学与药学数据库</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)</collection><collection>ProQuest Central</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><collection>Hyper Article en Ligne (HAL)</collection><jtitle>Pharmaceutical research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>OLIVIER, J.-C</au><au>FENART, L</au><au>CHAUVET, R</au><au>PARIAT, C</au><au>CECCHELLI, R</au><au>COUET, W</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Indirect evidence that drug brain targeting using polysorbate 80-coated polybutylcyanoacrylate nanoparticles is related to toxicity</atitle><jtitle>Pharmaceutical research</jtitle><addtitle>Pharm Res</addtitle><date>1999-12-01</date><risdate>1999</risdate><volume>16</volume><issue>12</issue><spage>1836</spage><epage>1842</epage><pages>1836-1842</pages><issn>0724-8741</issn><eissn>1573-904X</eissn><coden>PHREEB</coden><abstract>To investigate the mechanism underlying the entry of the analgesic peptide dalargin into brain using biodegradable polybutylcyanoacrylate (PBCA) nanoparticles (NP) overcoated with polysorbate 80.
The investigations were carried out with PBCA NP and with non biodegradable polystyrene (PS) NP (200 nm diameter). Dalargin adsorption was assessed by HPLC. Its entry into the CNS in mice was evaluated using the tail-flick procedure. Locomotor activity measurements were performed to compare NP toxicities. BBB permeabilization by PBCA NP was studied in vitro using a coculture of bovine brain capillary endothelial cells and rat astrocytes.
Dalargin loading was 11.7 microg/mg on PBCA NP and 16.5 microg/ mg on PS NP. Adding polysorbate 80 to NP led to a complete desorption. Nevertheless, dalargin associated with PBCA NP and polysorbate 80 induced a potent and prolonged analgesia, which could not be obtained using PS NP in place of PBCA NP. Locomotor activity dramatically decreased in mice dosed with PBCA NP, but not with PS NP. PBCA NP also caused occasional mortality. In vitro, PBCA NP (10 microg/ml) induced a permeabilization of the BBB model.
A non specific permeabilization of the BBB, probably related to the toxicity of the carrier, may account for the CNS penetration of dalargin associated with PBCA NP and polysorbate 80.</abstract><cop>New York, NY</cop><pub>Springer</pub><pmid>10644071</pmid><doi>10.1023/A:1018947208597</doi><tpages>7</tpages><orcidid>https://orcid.org/0000-0001-9285-0579</orcidid></addata></record> |
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| ispartof | Pharmaceutical research, 1999-12, Vol.16 (12), p.1836-1842 |
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| subjects | Analgesics Analgesics - administration & dosage Analgesics - toxicity Animals Biochemistry, Molecular Biology Biological and medical sciences Blood-Brain Barrier - drug effects Brain - metabolism Cells, Cultured Chromatography, High Pressure Liquid Enbucrilate - administration & dosage Enbucrilate - toxicity Endothelium - cytology Endothelium - metabolism Enkephalin, Leucine-2-Alanine - administration & dosage Enkephalin, Leucine-2-Alanine - analogs & derivatives Enkephalin, Leucine-2-Alanine - toxicity Excipients - administration & dosage Excipients - toxicity General pharmacology Life Sciences Male Medical sciences Mice Microspheres Motor Activity - drug effects Neuropharmacology Pain Measurement - drug effects Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Polysorbates - administration & dosage Polysorbates - toxicity |
| title | Indirect evidence that drug brain targeting using polysorbate 80-coated polybutylcyanoacrylate nanoparticles is related to toxicity |
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