Passive targeting and lung tolerability of enoxaparin microspheres for a sustained antithrombotic activity in rats
Pulmonary bed can retain microparticles (MP) larger than their capillaries' diameter, hence we offer a promising way for lung passive targeting following intravenous (IV) administration. In this study, enoxaparin (Enox)-albumin microspheres (Enox-Alb MS) were, optimally, developed as lung targe...
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| Veröffentlicht in: | Drug delivery 2017-01, Vol.24 (1), p.243-251 |
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| creator | Ibrahim, Shaimaa S. Osman, Rihab Mortada, Nahed D. Geneidy, Ahmed-Shawky Awad, Gehanne A. S. |
| description | Pulmonary bed can retain microparticles (MP) larger than their capillaries' diameter, hence we offer a promising way for lung passive targeting following intravenous (IV) administration. In this study, enoxaparin (Enox)-albumin microspheres (Enox-Alb MS) were, optimally, developed as lung targeted sustained release MP for IV use. Lung tolerability and targeting efficiency of Enox-Alb MS were tested, and the pharmacokinetic profile following IV administration to albino rats was constructed. In vivo studies confirmed high lung targeting efficiency of Enox-Alb MS with lack of potential tissue toxicity. The anticoagulant activity of the selected Alb MS was significantly sustained for up to 38 h compared to 5 h for the market product. Alb MS are promising delivery carriers for controlled and targeted delivery of Enox to the lungs for prophylaxis and treatment of pulmonary embolism. |
| doi_str_mv | 10.1080/10717544.2016.1245368 |
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S.</creator><creatorcontrib>Ibrahim, Shaimaa S. ; Osman, Rihab ; Mortada, Nahed D. ; Geneidy, Ahmed-Shawky ; Awad, Gehanne A. S.</creatorcontrib><description>Pulmonary bed can retain microparticles (MP) larger than their capillaries' diameter, hence we offer a promising way for lung passive targeting following intravenous (IV) administration. In this study, enoxaparin (Enox)-albumin microspheres (Enox-Alb MS) were, optimally, developed as lung targeted sustained release MP for IV use. Lung tolerability and targeting efficiency of Enox-Alb MS were tested, and the pharmacokinetic profile following IV administration to albino rats was constructed. In vivo studies confirmed high lung targeting efficiency of Enox-Alb MS with lack of potential tissue toxicity. The anticoagulant activity of the selected Alb MS was significantly sustained for up to 38 h compared to 5 h for the market product. Alb MS are promising delivery carriers for controlled and targeted delivery of Enox to the lungs for prophylaxis and treatment of pulmonary embolism.</description><identifier>ISSN: 1071-7544</identifier><identifier>EISSN: 1521-0464</identifier><identifier>DOI: 10.1080/10717544.2016.1245368</identifier><identifier>PMID: 28156170</identifier><language>eng</language><publisher>England: Taylor & Francis</publisher><subject>Administration, Intravenous - methods ; Albumin ; Albumins - chemistry ; Animals ; anticoagulant ; Anticoagulants ; Anticoagulants - administration & dosage ; controlled delivery ; Delayed-Action Preparations - administration & dosage ; Drug delivery systems ; Drug Delivery Systems - methods ; Embolisms ; enoxaparin ; Enoxaparin - administration & dosage ; Growth factors ; Lung - drug effects ; Lungs ; Male ; Microspheres ; Molecular weight ; Nanoparticles ; passive lung targeting ; Pharmacy ; Rats</subject><ispartof>Drug delivery, 2017-01, Vol.24 (1), p.243-251</ispartof><rights>2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. 2017</rights><rights>2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This work is licensed under the Creative Commons Attribution License http://creativecommons.org/Licenses/by/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2017 The Author(s). 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S.</creatorcontrib><title>Passive targeting and lung tolerability of enoxaparin microspheres for a sustained antithrombotic activity in rats</title><title>Drug delivery</title><addtitle>Drug Deliv</addtitle><description>Pulmonary bed can retain microparticles (MP) larger than their capillaries' diameter, hence we offer a promising way for lung passive targeting following intravenous (IV) administration. In this study, enoxaparin (Enox)-albumin microspheres (Enox-Alb MS) were, optimally, developed as lung targeted sustained release MP for IV use. Lung tolerability and targeting efficiency of Enox-Alb MS were tested, and the pharmacokinetic profile following IV administration to albino rats was constructed. In vivo studies confirmed high lung targeting efficiency of Enox-Alb MS with lack of potential tissue toxicity. The anticoagulant activity of the selected Alb MS was significantly sustained for up to 38 h compared to 5 h for the market product. Alb MS are promising delivery carriers for controlled and targeted delivery of Enox to the lungs for prophylaxis and treatment of pulmonary embolism.</description><subject>Administration, Intravenous - methods</subject><subject>Albumin</subject><subject>Albumins - chemistry</subject><subject>Animals</subject><subject>anticoagulant</subject><subject>Anticoagulants</subject><subject>Anticoagulants - administration & dosage</subject><subject>controlled delivery</subject><subject>Delayed-Action Preparations - administration & dosage</subject><subject>Drug delivery systems</subject><subject>Drug Delivery Systems - methods</subject><subject>Embolisms</subject><subject>enoxaparin</subject><subject>Enoxaparin - administration & dosage</subject><subject>Growth factors</subject><subject>Lung - drug effects</subject><subject>Lungs</subject><subject>Male</subject><subject>Microspheres</subject><subject>Molecular weight</subject><subject>Nanoparticles</subject><subject>passive lung targeting</subject><subject>Pharmacy</subject><subject>Rats</subject><issn>1071-7544</issn><issn>1521-0464</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>0YH</sourceid><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><sourceid>DOA</sourceid><recordid>eNp9kktvEzEURkcIREvhJ4BGYsMmwfb4lQ2iqlqoVAkWsLbueO4kjmbsYHsC-fd4SFpRFqxs2eee68dXVa8pWVKiyXtKFFWC8yUjVC4p46KR-kl1TgWjC8Ilf1rmhVnM0Fn1IqUtIURTJp5XZ0xTIaki51X8Cim5PdYZ4hqz8-safFcPU5nkMGCE1g0uH-rQ1-jDL9hBdL4enY0h7TYYMdV9iDXUaUoZnMeuCLLLmxjGNmRna7DZ7WdFqYuQ08vqWQ9Dwlen8aL6fnP97erz4u7Lp9ury7uFFZLlBSjVKamUkmitbFctKK4sI1rbpqFa9R0S4Ly3vZRKAMceCKOitVyLvlXYXFS3R28XYGt20Y0QDyaAM38WQlwbiOWAAxreKYtqxYA3giNrteWiRasZJ7xXnBXXh6NrN7UjdhZ9jjA8kj7e8W5j1mFvioJSrYvg3UkQw48JUzajSxaHATyGKRmqpRCl0WpG3_6DbsMUfXkqw-hKsEatyEyJIzV_RIrYPxyGEjMnxNwnxMwJMaeElLo3f9_koeo-EgX4eAScLx87ws8Qh85kOAwh9hG8dck0_-_xG5-3zVI</recordid><startdate>20170101</startdate><enddate>20170101</enddate><creator>Ibrahim, Shaimaa S.</creator><creator>Osman, Rihab</creator><creator>Mortada, Nahed D.</creator><creator>Geneidy, Ahmed-Shawky</creator><creator>Awad, Gehanne A. 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S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Passive targeting and lung tolerability of enoxaparin microspheres for a sustained antithrombotic activity in rats</atitle><jtitle>Drug delivery</jtitle><addtitle>Drug Deliv</addtitle><date>2017-01-01</date><risdate>2017</risdate><volume>24</volume><issue>1</issue><spage>243</spage><epage>251</epage><pages>243-251</pages><issn>1071-7544</issn><eissn>1521-0464</eissn><abstract>Pulmonary bed can retain microparticles (MP) larger than their capillaries' diameter, hence we offer a promising way for lung passive targeting following intravenous (IV) administration. In this study, enoxaparin (Enox)-albumin microspheres (Enox-Alb MS) were, optimally, developed as lung targeted sustained release MP for IV use. Lung tolerability and targeting efficiency of Enox-Alb MS were tested, and the pharmacokinetic profile following IV administration to albino rats was constructed. In vivo studies confirmed high lung targeting efficiency of Enox-Alb MS with lack of potential tissue toxicity. The anticoagulant activity of the selected Alb MS was significantly sustained for up to 38 h compared to 5 h for the market product. Alb MS are promising delivery carriers for controlled and targeted delivery of Enox to the lungs for prophylaxis and treatment of pulmonary embolism.</abstract><cop>England</cop><pub>Taylor & Francis</pub><pmid>28156170</pmid><doi>10.1080/10717544.2016.1245368</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Administration, Intravenous - methods Albumin Albumins - chemistry Animals anticoagulant Anticoagulants Anticoagulants - administration & dosage controlled delivery Delayed-Action Preparations - administration & dosage Drug delivery systems Drug Delivery Systems - methods Embolisms enoxaparin Enoxaparin - administration & dosage Growth factors Lung - drug effects Lungs Male Microspheres Molecular weight Nanoparticles passive lung targeting Pharmacy Rats |
| title | Passive targeting and lung tolerability of enoxaparin microspheres for a sustained antithrombotic activity in rats |
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