Development of biodegradable in situ implant and microparticle injectable formulations for sustained delivery of haloperidol
The objective of this study is to formulate injectable, biodegradable sustained release in situ implant (ISI), and in situ microparticle (ISM) formulations of haloperidol. Factors affecting the in vitro drug release, pharmacokinetics, and stability of the formulations were investigated. The concentr...
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| Veröffentlicht in: | Journal of pharmaceutical sciences 2012-10, Vol.101 (10), p.3753-3762 |
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| creator | Ahmed, Tarek A. Ibrahim, Hany M. Ibrahim, Fathy Samy, Ahmed M. Kaseem, Alaa H. Nutan, Mohammad T. Hussain, Muhammad Delwar |
| description | The objective of this study is to formulate injectable, biodegradable sustained release in situ implant (ISI), and in situ microparticle (ISM) formulations of haloperidol. Factors affecting the in vitro drug release, pharmacokinetics, and stability of the formulations were investigated. The concentration of the polymer, poly(lactide-co-glycolide) acid (PLGA), and the type of solvents showed a pronounced effect on the in vitro drug release from the ISI and ISM formulations. The ISM formulation [20% PLGA in N-methyl-2-pyrrolidone (NMP)–peanut oil, 1:4] showed reduced maximum plasma concentration (60 versus 44 ng/mL) and longer release (30 days, plasma concentration of 8 ng/mL versus 20 days, plasma concentration of 6 ng/mL) compared with the ISI formulation (20% PLGA in NMP) after intramuscular injection in rats. The delivery of haloperidol can be extended further by changing the concentration, molecular weight, and lactide-to-glycolide ratio of the PLGA. These formulations can be easily administered by both intramuscular and subcutaneous injections. The shelf lives of both systems were found to be 2 years when stored at 4°C. Haloperidol can be formulated as an injectable ISI or ISM systems suitable for 1 month or longer release. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:3753–3762, 2012 |
| doi_str_mv | 10.1002/jps.23250 |
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Nutan, Mohammad T. ; Hussain, Muhammad Delwar</creator><creatorcontrib>Ahmed, Tarek A. ; Ibrahim, Hany M. ; Ibrahim, Fathy ; Samy, Ahmed M. ; Kaseem, Alaa ; H. Nutan, Mohammad T. ; Hussain, Muhammad Delwar</creatorcontrib><description>The objective of this study is to formulate injectable, biodegradable sustained release in situ implant (ISI), and in situ microparticle (ISM) formulations of haloperidol. Factors affecting the in vitro drug release, pharmacokinetics, and stability of the formulations were investigated. The concentration of the polymer, poly(lactide-co-glycolide) acid (PLGA), and the type of solvents showed a pronounced effect on the in vitro drug release from the ISI and ISM formulations. The ISM formulation [20% PLGA in N-methyl-2-pyrrolidone (NMP)–peanut oil, 1:4] showed reduced maximum plasma concentration (60 versus 44 ng/mL) and longer release (30 days, plasma concentration of 8 ng/mL versus 20 days, plasma concentration of 6 ng/mL) compared with the ISI formulation (20% PLGA in NMP) after intramuscular injection in rats. The delivery of haloperidol can be extended further by changing the concentration, molecular weight, and lactide-to-glycolide ratio of the PLGA. These formulations can be easily administered by both intramuscular and subcutaneous injections. The shelf lives of both systems were found to be 2 years when stored at 4°C. Haloperidol can be formulated as an injectable ISI or ISM systems suitable for 1 month or longer release. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:3753–3762, 2012</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1002/jps.23250</identifier><identifier>PMID: 22753324</identifier><identifier>CODEN: JPMSAE</identifier><language>eng</language><publisher>Hoboken: Elsevier Inc</publisher><subject>Absorbable Implants ; Animals ; biodegradable polymers ; Biological and medical sciences ; Chemistry, Pharmaceutical - methods ; Delayed-Action Preparations ; Drug Delivery Systems - methods ; Drug Stability ; General pharmacology ; haloperidol ; Haloperidol - administration & dosage ; Haloperidol - chemistry ; Haloperidol - pharmacokinetics ; in situ implants ; in situ microparticles ; injectables ; Injections - methods ; Lactic Acid - administration & dosage ; Lactic Acid - chemistry ; Male ; Medical sciences ; Molecular Weight ; Pharmaceutical technology. Pharmaceutical industry ; pharmacokinetics ; Pharmacology. Drug treatments ; PLGA ; Polyglycolic Acid - administration & dosage ; Polyglycolic Acid - chemistry ; Polymers - administration & dosage ; Polymers - chemistry ; Rats ; Rats, Sprague-Dawley ; Solvents - chemistry ; stability ; sustained release</subject><ispartof>Journal of pharmaceutical sciences, 2012-10, Vol.101 (10), p.3753-3762</ispartof><rights>2012 Wiley Periodicals, Inc.</rights><rights>Copyright © 2012 Wiley Periodicals, Inc.</rights><rights>2015 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4980-433b90e1c576fad221e090a59eda924d5ff338fa214b5aee21387f7cf9fd4ca93</citedby><cites>FETCH-LOGICAL-c4980-433b90e1c576fad221e090a59eda924d5ff338fa214b5aee21387f7cf9fd4ca93</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fjps.23250$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjps.23250$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1417,27924,27925,45574,45575</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=26376523$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22753324$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ahmed, Tarek A.</creatorcontrib><creatorcontrib>Ibrahim, Hany M.</creatorcontrib><creatorcontrib>Ibrahim, Fathy</creatorcontrib><creatorcontrib>Samy, Ahmed M.</creatorcontrib><creatorcontrib>Kaseem, Alaa</creatorcontrib><creatorcontrib>H. Nutan, Mohammad T.</creatorcontrib><creatorcontrib>Hussain, Muhammad Delwar</creatorcontrib><title>Development of biodegradable in situ implant and microparticle injectable formulations for sustained delivery of haloperidol</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>The objective of this study is to formulate injectable, biodegradable sustained release in situ implant (ISI), and in situ microparticle (ISM) formulations of haloperidol. Factors affecting the in vitro drug release, pharmacokinetics, and stability of the formulations were investigated. The concentration of the polymer, poly(lactide-co-glycolide) acid (PLGA), and the type of solvents showed a pronounced effect on the in vitro drug release from the ISI and ISM formulations. The ISM formulation [20% PLGA in N-methyl-2-pyrrolidone (NMP)–peanut oil, 1:4] showed reduced maximum plasma concentration (60 versus 44 ng/mL) and longer release (30 days, plasma concentration of 8 ng/mL versus 20 days, plasma concentration of 6 ng/mL) compared with the ISI formulation (20% PLGA in NMP) after intramuscular injection in rats. The delivery of haloperidol can be extended further by changing the concentration, molecular weight, and lactide-to-glycolide ratio of the PLGA. These formulations can be easily administered by both intramuscular and subcutaneous injections. The shelf lives of both systems were found to be 2 years when stored at 4°C. Haloperidol can be formulated as an injectable ISI or ISM systems suitable for 1 month or longer release. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:3753–3762, 2012</description><subject>Absorbable Implants</subject><subject>Animals</subject><subject>biodegradable polymers</subject><subject>Biological and medical sciences</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>Delayed-Action Preparations</subject><subject>Drug Delivery Systems - methods</subject><subject>Drug Stability</subject><subject>General pharmacology</subject><subject>haloperidol</subject><subject>Haloperidol - administration & dosage</subject><subject>Haloperidol - chemistry</subject><subject>Haloperidol - pharmacokinetics</subject><subject>in situ implants</subject><subject>in situ microparticles</subject><subject>injectables</subject><subject>Injections - methods</subject><subject>Lactic Acid - administration & dosage</subject><subject>Lactic Acid - chemistry</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Molecular Weight</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>PLGA</subject><subject>Polyglycolic Acid - administration & dosage</subject><subject>Polyglycolic Acid - chemistry</subject><subject>Polymers - administration & dosage</subject><subject>Polymers - chemistry</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Solvents - chemistry</subject><subject>stability</subject><subject>sustained release</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0l2L1DAUBuAgiju7euEfkIII60V389E07eWy6qg7qOCKlyFNTjRj29SkHR3wx5uZzq4gileh5Dnn9PQtQo8IPiMY0_P1EM8ooxzfQQvCKc5LTMRdtEh3NGe8qI_QcYxrjHGJOb-PjigVnDFaLNDP57CB1g8d9GPmbdY4b-BzUEY1LWSuz6Ibp8x1Q6sSUL3JOqeDH1QYnd6LNehxj60P3dSq0fk-7h6yOMVRuR5MZqB1Gwjb3YQvKo2D4IxvH6B7VrURHh7OE_Tx5Yvry1f56t3y9eXFKtdFXeG8YKypMRDNRWmVoZQArrHiNRhV08JwaxmrrKKkaLgCoIRVwgpta2sKrWp2gk7nvkPw3yaIo-xc1NCmncBPURJeFJjQqsT_p5hxgmlFRaJP_qBrP4U-LZIaEsGqimKa1LNZpa8WYwArh-A6FbapldylJ1N6cp9eso8PHaemA3Mrb-JK4OkBqKhVa4PqtYu_XclEySlL7nx2310L239PlG_ef7gZnc8VLo7w47ZCha-yFExw-entUq7qq2teLa_k7k3Y7CHltnEQZNQOeg3GhfRDSOPdXxb8BUdk0tk</recordid><startdate>201210</startdate><enddate>201210</enddate><creator>Ahmed, Tarek A.</creator><creator>Ibrahim, Hany M.</creator><creator>Ibrahim, Fathy</creator><creator>Samy, Ahmed M.</creator><creator>Kaseem, Alaa</creator><creator>H. Nutan, Mohammad T.</creator><creator>Hussain, Muhammad Delwar</creator><general>Elsevier Inc</general><general>Wiley Subscription Services, Inc., A Wiley Company</general><general>Wiley</general><general>American Pharmaceutical Association</general><general>Elsevier Limited</general><scope>BSCLL</scope><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>7QO</scope><scope>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7U7</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope><scope>RC3</scope><scope>7X8</scope><scope>7T7</scope></search><sort><creationdate>201210</creationdate><title>Development of biodegradable in situ implant and microparticle injectable formulations for sustained delivery of haloperidol</title><author>Ahmed, Tarek A. ; Ibrahim, Hany M. ; Ibrahim, Fathy ; Samy, Ahmed M. ; Kaseem, Alaa ; H. Nutan, Mohammad T. ; Hussain, Muhammad Delwar</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4980-433b90e1c576fad221e090a59eda924d5ff338fa214b5aee21387f7cf9fd4ca93</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Absorbable Implants</topic><topic>Animals</topic><topic>biodegradable polymers</topic><topic>Biological and medical sciences</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>Delayed-Action Preparations</topic><topic>Drug Delivery Systems - methods</topic><topic>Drug Stability</topic><topic>General pharmacology</topic><topic>haloperidol</topic><topic>Haloperidol - administration & dosage</topic><topic>Haloperidol - chemistry</topic><topic>Haloperidol - pharmacokinetics</topic><topic>in situ implants</topic><topic>in situ microparticles</topic><topic>injectables</topic><topic>Injections - methods</topic><topic>Lactic Acid - administration & dosage</topic><topic>Lactic Acid - chemistry</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Molecular Weight</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>PLGA</topic><topic>Polyglycolic Acid - administration & dosage</topic><topic>Polyglycolic Acid - chemistry</topic><topic>Polymers - administration & dosage</topic><topic>Polymers - chemistry</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Solvents - chemistry</topic><topic>stability</topic><topic>sustained release</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ahmed, Tarek A.</creatorcontrib><creatorcontrib>Ibrahim, Hany M.</creatorcontrib><creatorcontrib>Ibrahim, Fathy</creatorcontrib><creatorcontrib>Samy, Ahmed M.</creatorcontrib><creatorcontrib>Kaseem, Alaa</creatorcontrib><creatorcontrib>H. Nutan, Mohammad T.</creatorcontrib><creatorcontrib>Hussain, Muhammad Delwar</creatorcontrib><collection>Istex</collection><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>Biotechnology Research Abstracts</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Toxicology Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Genetics Abstracts</collection><collection>MEDLINE - Academic</collection><collection>Industrial and Applied Microbiology Abstracts (Microbiology A)</collection><jtitle>Journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ahmed, Tarek A.</au><au>Ibrahim, Hany M.</au><au>Ibrahim, Fathy</au><au>Samy, Ahmed M.</au><au>Kaseem, Alaa</au><au>H. Nutan, Mohammad T.</au><au>Hussain, Muhammad Delwar</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development of biodegradable in situ implant and microparticle injectable formulations for sustained delivery of haloperidol</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>2012-10</date><risdate>2012</risdate><volume>101</volume><issue>10</issue><spage>3753</spage><epage>3762</epage><pages>3753-3762</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><coden>JPMSAE</coden><abstract>The objective of this study is to formulate injectable, biodegradable sustained release in situ implant (ISI), and in situ microparticle (ISM) formulations of haloperidol. Factors affecting the in vitro drug release, pharmacokinetics, and stability of the formulations were investigated. The concentration of the polymer, poly(lactide-co-glycolide) acid (PLGA), and the type of solvents showed a pronounced effect on the in vitro drug release from the ISI and ISM formulations. The ISM formulation [20% PLGA in N-methyl-2-pyrrolidone (NMP)–peanut oil, 1:4] showed reduced maximum plasma concentration (60 versus 44 ng/mL) and longer release (30 days, plasma concentration of 8 ng/mL versus 20 days, plasma concentration of 6 ng/mL) compared with the ISI formulation (20% PLGA in NMP) after intramuscular injection in rats. The delivery of haloperidol can be extended further by changing the concentration, molecular weight, and lactide-to-glycolide ratio of the PLGA. These formulations can be easily administered by both intramuscular and subcutaneous injections. The shelf lives of both systems were found to be 2 years when stored at 4°C. Haloperidol can be formulated as an injectable ISI or ISM systems suitable for 1 month or longer release. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:3753–3762, 2012</abstract><cop>Hoboken</cop><pub>Elsevier Inc</pub><pmid>22753324</pmid><doi>10.1002/jps.23250</doi><tpages>10</tpages></addata></record> |
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| subjects | Absorbable Implants Animals biodegradable polymers Biological and medical sciences Chemistry, Pharmaceutical - methods Delayed-Action Preparations Drug Delivery Systems - methods Drug Stability General pharmacology haloperidol Haloperidol - administration & dosage Haloperidol - chemistry Haloperidol - pharmacokinetics in situ implants in situ microparticles injectables Injections - methods Lactic Acid - administration & dosage Lactic Acid - chemistry Male Medical sciences Molecular Weight Pharmaceutical technology. Pharmaceutical industry pharmacokinetics Pharmacology. Drug treatments PLGA Polyglycolic Acid - administration & dosage Polyglycolic Acid - chemistry Polymers - administration & dosage Polymers - chemistry Rats Rats, Sprague-Dawley Solvents - chemistry stability sustained release |
| title | Development of biodegradable in situ implant and microparticle injectable formulations for sustained delivery of haloperidol |
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