Preparation and characterization of liposomal formulations of neurotensin-degrading enzyme inhibitors
Neurotensin-degrading enzyme (NTDE) inhibitors hold great potential for treating psychotic disorders. However, brain uptake of such compounds in vivo is generally low due to the presence of the blood–brain barrier. In this study, liposomal formulations of two NTDE inhibitors, named compound 1 (C1) a...
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| Veröffentlicht in: | International journal of pharmaceutics 2011-09, Vol.416 (2), p.448-452 |
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| creator | van Rooy, Inge Wu, Shin-Ying Storm, Gert Hennink, Wim E. Dinter-Heidorn, Heike Schiffelers, Raymond M. Mastrobattista, Enrico |
| description | Neurotensin-degrading enzyme (NTDE) inhibitors hold great potential for treating psychotic disorders. However, brain uptake of such compounds
in vivo is generally low due to the presence of the blood–brain barrier. In this study, liposomal formulations of two NTDE inhibitors, named compound 1 (C1) and compound 2 (C2) were prepared. Association of these compounds with the liposomal bilayer, subsequent liposomal stability, and compound release in the presence of albumin was studied. Entrapment of the compounds in the liposomal bilayer showed the solubilizing properties of the liposomes. Size and polydispersity index of the compound-entrapped liposomes did not change over 1 month, showing colloidal stability of the liposomal drug formulations. The amount of compounds associated with the liposomes decreased within one day. After this, the association remained stable at 4
°C. For C1, association remained stable at 37
°C in HEPES buffered saline, and the compound was gradually released in the presence of bovine serum albumin. For C2, the release was rapid in both HBS and BSA at 37
°C. In conclusion, the formulation of NTDE inhibitors C1 and C2 in liposomes has been demonstrated and holds promise to deliver NTDE inhibitors
in vivo. |
| doi_str_mv | 10.1016/j.ijpharm.2011.01.017 |
| format | Article |
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in vivo is generally low due to the presence of the blood–brain barrier. In this study, liposomal formulations of two NTDE inhibitors, named compound 1 (C1) and compound 2 (C2) were prepared. Association of these compounds with the liposomal bilayer, subsequent liposomal stability, and compound release in the presence of albumin was studied. Entrapment of the compounds in the liposomal bilayer showed the solubilizing properties of the liposomes. Size and polydispersity index of the compound-entrapped liposomes did not change over 1 month, showing colloidal stability of the liposomal drug formulations. The amount of compounds associated with the liposomes decreased within one day. After this, the association remained stable at 4
°C. For C1, association remained stable at 37
°C in HEPES buffered saline, and the compound was gradually released in the presence of bovine serum albumin. For C2, the release was rapid in both HBS and BSA at 37
°C. In conclusion, the formulation of NTDE inhibitors C1 and C2 in liposomes has been demonstrated and holds promise to deliver NTDE inhibitors
in vivo.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2011.01.017</identifier><identifier>PMID: 21251959</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Antipsychotic Agents - administration & dosage ; Antipsychotic Agents - chemistry ; Biological and medical sciences ; CNS drugs ; Drug Stability ; Drug Storage ; Enzyme Inhibitors - administration & dosage ; Enzyme Inhibitors - chemistry ; General pharmacology ; HEPES - chemistry ; Liposomes ; Medical sciences ; Metalloendopeptidases - antagonists & inhibitors ; Neurotensin ; NTDE inhibitors ; Particle Size ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Serum Albumin, Bovine - chemistry ; Sodium Chloride - chemistry ; Solubility ; Temperature</subject><ispartof>International journal of pharmaceutics, 2011-09, Vol.416 (2), p.448-452</ispartof><rights>2011 Elsevier B.V.</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2011 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c394t-387ebfe9f04a0c6a9c78c8c33b51d6184897202ec0c1efbee3a5eca8448c8cb73</citedby><cites>FETCH-LOGICAL-c394t-387ebfe9f04a0c6a9c78c8c33b51d6184897202ec0c1efbee3a5eca8448c8cb73</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0378517311000482$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>309,310,314,776,780,785,786,3537,23909,23910,25118,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=24563300$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21251959$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>van Rooy, Inge</creatorcontrib><creatorcontrib>Wu, Shin-Ying</creatorcontrib><creatorcontrib>Storm, Gert</creatorcontrib><creatorcontrib>Hennink, Wim E.</creatorcontrib><creatorcontrib>Dinter-Heidorn, Heike</creatorcontrib><creatorcontrib>Schiffelers, Raymond M.</creatorcontrib><creatorcontrib>Mastrobattista, Enrico</creatorcontrib><title>Preparation and characterization of liposomal formulations of neurotensin-degrading enzyme inhibitors</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>Neurotensin-degrading enzyme (NTDE) inhibitors hold great potential for treating psychotic disorders. However, brain uptake of such compounds
in vivo is generally low due to the presence of the blood–brain barrier. In this study, liposomal formulations of two NTDE inhibitors, named compound 1 (C1) and compound 2 (C2) were prepared. Association of these compounds with the liposomal bilayer, subsequent liposomal stability, and compound release in the presence of albumin was studied. Entrapment of the compounds in the liposomal bilayer showed the solubilizing properties of the liposomes. Size and polydispersity index of the compound-entrapped liposomes did not change over 1 month, showing colloidal stability of the liposomal drug formulations. The amount of compounds associated with the liposomes decreased within one day. After this, the association remained stable at 4
°C. For C1, association remained stable at 37
°C in HEPES buffered saline, and the compound was gradually released in the presence of bovine serum albumin. For C2, the release was rapid in both HBS and BSA at 37
°C. In conclusion, the formulation of NTDE inhibitors C1 and C2 in liposomes has been demonstrated and holds promise to deliver NTDE inhibitors
in vivo.</description><subject>Antipsychotic Agents - administration & dosage</subject><subject>Antipsychotic Agents - chemistry</subject><subject>Biological and medical sciences</subject><subject>CNS drugs</subject><subject>Drug Stability</subject><subject>Drug Storage</subject><subject>Enzyme Inhibitors - administration & dosage</subject><subject>Enzyme Inhibitors - chemistry</subject><subject>General pharmacology</subject><subject>HEPES - chemistry</subject><subject>Liposomes</subject><subject>Medical sciences</subject><subject>Metalloendopeptidases - antagonists & inhibitors</subject><subject>Neurotensin</subject><subject>NTDE inhibitors</subject><subject>Particle Size</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Serum Albumin, Bovine - chemistry</subject><subject>Sodium Chloride - chemistry</subject><subject>Solubility</subject><subject>Temperature</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkEtr3DAQgEVoSLZJfkKKL6UnbyRLtuRTCKEvCKSH5izG43GixZZcyQ4kvz52d9seCwMDM988-Bi7FHwruKiudlu3G58gDtuCC7Hla-gjthFGy1wqXb1jGy61yUuh5Sl7n9KOc14VQp6w00IUpajLesPoR6QRIkwu-Ax8m-GyE3Ci6F73xdBlvRtDCgP0WRfiMPe_G2nteJpjmMgn5_OWHiO0zj9m5F9fBsqcf3KNm0JM5-y4gz7RxSGfsYcvn3_efsvv7r9-v725y1HWasql0dR0VHdcAccKatQGDUrZlKKthFGm1gUvCDkK6hoiCSUhGKVWrNHyjH3a7x1j-DVTmuzgElLfg6cwJ2uMEoVUqlrIck9iDClF6uwY3QDxxQpuV8F2Zw-C7SrY8jXWCx8OF-ZmoPbv1B-jC_DxAEBC6LsIHl36x6mykpLzhbvec7T4eHYUbUJHHql1kXCybXD_eeUN2gqfTA</recordid><startdate>20110920</startdate><enddate>20110920</enddate><creator>van Rooy, Inge</creator><creator>Wu, Shin-Ying</creator><creator>Storm, Gert</creator><creator>Hennink, Wim E.</creator><creator>Dinter-Heidorn, Heike</creator><creator>Schiffelers, Raymond M.</creator><creator>Mastrobattista, Enrico</creator><general>Elsevier B.V</general><general>Elsevier</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>7X8</scope></search><sort><creationdate>20110920</creationdate><title>Preparation and characterization of liposomal formulations of neurotensin-degrading enzyme inhibitors</title><author>van Rooy, Inge ; Wu, Shin-Ying ; Storm, Gert ; Hennink, Wim E. ; Dinter-Heidorn, Heike ; Schiffelers, Raymond M. ; Mastrobattista, Enrico</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c394t-387ebfe9f04a0c6a9c78c8c33b51d6184897202ec0c1efbee3a5eca8448c8cb73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Antipsychotic Agents - administration & dosage</topic><topic>Antipsychotic Agents - chemistry</topic><topic>Biological and medical sciences</topic><topic>CNS drugs</topic><topic>Drug Stability</topic><topic>Drug Storage</topic><topic>Enzyme Inhibitors - administration & dosage</topic><topic>Enzyme Inhibitors - chemistry</topic><topic>General pharmacology</topic><topic>HEPES - chemistry</topic><topic>Liposomes</topic><topic>Medical sciences</topic><topic>Metalloendopeptidases - antagonists & inhibitors</topic><topic>Neurotensin</topic><topic>NTDE inhibitors</topic><topic>Particle Size</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Serum Albumin, Bovine - chemistry</topic><topic>Sodium Chloride - chemistry</topic><topic>Solubility</topic><topic>Temperature</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>van Rooy, Inge</creatorcontrib><creatorcontrib>Wu, Shin-Ying</creatorcontrib><creatorcontrib>Storm, Gert</creatorcontrib><creatorcontrib>Hennink, Wim E.</creatorcontrib><creatorcontrib>Dinter-Heidorn, Heike</creatorcontrib><creatorcontrib>Schiffelers, Raymond M.</creatorcontrib><creatorcontrib>Mastrobattista, Enrico</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>MEDLINE - Academic</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>van Rooy, Inge</au><au>Wu, Shin-Ying</au><au>Storm, Gert</au><au>Hennink, Wim E.</au><au>Dinter-Heidorn, Heike</au><au>Schiffelers, Raymond M.</au><au>Mastrobattista, Enrico</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation and characterization of liposomal formulations of neurotensin-degrading enzyme inhibitors</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2011-09-20</date><risdate>2011</risdate><volume>416</volume><issue>2</issue><spage>448</spage><epage>452</epage><pages>448-452</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>Neurotensin-degrading enzyme (NTDE) inhibitors hold great potential for treating psychotic disorders. However, brain uptake of such compounds
in vivo is generally low due to the presence of the blood–brain barrier. In this study, liposomal formulations of two NTDE inhibitors, named compound 1 (C1) and compound 2 (C2) were prepared. Association of these compounds with the liposomal bilayer, subsequent liposomal stability, and compound release in the presence of albumin was studied. Entrapment of the compounds in the liposomal bilayer showed the solubilizing properties of the liposomes. Size and polydispersity index of the compound-entrapped liposomes did not change over 1 month, showing colloidal stability of the liposomal drug formulations. The amount of compounds associated with the liposomes decreased within one day. After this, the association remained stable at 4
°C. For C1, association remained stable at 37
°C in HEPES buffered saline, and the compound was gradually released in the presence of bovine serum albumin. For C2, the release was rapid in both HBS and BSA at 37
°C. In conclusion, the formulation of NTDE inhibitors C1 and C2 in liposomes has been demonstrated and holds promise to deliver NTDE inhibitors
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| subjects | Antipsychotic Agents - administration & dosage Antipsychotic Agents - chemistry Biological and medical sciences CNS drugs Drug Stability Drug Storage Enzyme Inhibitors - administration & dosage Enzyme Inhibitors - chemistry General pharmacology HEPES - chemistry Liposomes Medical sciences Metalloendopeptidases - antagonists & inhibitors Neurotensin NTDE inhibitors Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Serum Albumin, Bovine - chemistry Sodium Chloride - chemistry Solubility Temperature |
| title | Preparation and characterization of liposomal formulations of neurotensin-degrading enzyme inhibitors |
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