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Preparation, in vitro and in vivo evaluation of stomach-specific metronidazole-loaded alginate beads as local anti- Helicobacter pylori therapy
Metronidazole (MZ), a common antibacterial drug used in treatment of H. pylori, was prepared in chitosan-treated alginate beads by the ionotropic gelation method. A (3 × 2 × 2) factorially designed experiment was used in which 3 viscosity-imparting polymers namely, methyl cellulose, carbopol 934P an...
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Published in: | Journal of controlled release 2007-06, Vol.119 (2), p.207-214 |
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creator | Ishak, Rania A.H. Awad, Gehanne A.S. Mortada, Nahed D. Nour, Samia A.K. |
description | Metronidazole (MZ), a common antibacterial drug used in treatment of
H. pylori, was prepared in chitosan-treated alginate beads by the ionotropic gelation method. A (3
×
2
×
2) factorially designed experiment was used in which 3 viscosity-imparting polymers namely, methyl cellulose, carbopol 934P and κ-carrageenan, 2 concentrations (0.2 and 0.4% w/v) of chitosan as encapsulating polymer and 2 concentrations (2.5 and 5% w/w) of the low density magnesium stearate as a floating aid were tested. The drug entrapment efficiency (%), the percent of floating beads and the time for 80% of the drug to be released (
T
80%) were the responses evaluated. The bead formula containing 0.5% κ-carrageenan, 0.4% chitosan and 5% magnesium stearate showed immediate buoyancy, optimum drug entrapment efficiency and extended drug release. The histopathological examination of mice stomachs and
in vivo H. pylori clearance tests were carried out by orally administering MZ floating alginate beads or MZ suspension, to
H. pylori infected mice under fed conditions as a single daily dose for 3 successive days in different doses 5, 10, 15 and 20 mg/kg. The histopathological examination showed that groups receiving MZ in the form of floating alginate beads at doses 10, 15 and 20 mg/kg were better than the corresponding suspension form, regarding eradication of
H. pylori infection. The
in vivo H. pylori clearance tests showed that MZ floating beads with a dose of 15 mg/kg provided 100% clearance rate whereas the MZ suspension with a dose of 20 mg/kg gave only 33.33%. |
doi_str_mv | 10.1016/j.jconrel.2007.02.012 |
format | article |
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H. pylori, was prepared in chitosan-treated alginate beads by the ionotropic gelation method. A (3
×
2
×
2) factorially designed experiment was used in which 3 viscosity-imparting polymers namely, methyl cellulose, carbopol 934P and κ-carrageenan, 2 concentrations (0.2 and 0.4% w/v) of chitosan as encapsulating polymer and 2 concentrations (2.5 and 5% w/w) of the low density magnesium stearate as a floating aid were tested. The drug entrapment efficiency (%), the percent of floating beads and the time for 80% of the drug to be released (
T
80%) were the responses evaluated. The bead formula containing 0.5% κ-carrageenan, 0.4% chitosan and 5% magnesium stearate showed immediate buoyancy, optimum drug entrapment efficiency and extended drug release. The histopathological examination of mice stomachs and
in vivo H. pylori clearance tests were carried out by orally administering MZ floating alginate beads or MZ suspension, to
H. pylori infected mice under fed conditions as a single daily dose for 3 successive days in different doses 5, 10, 15 and 20 mg/kg. The histopathological examination showed that groups receiving MZ in the form of floating alginate beads at doses 10, 15 and 20 mg/kg were better than the corresponding suspension form, regarding eradication of
H. pylori infection. The
in vivo H. pylori clearance tests showed that MZ floating beads with a dose of 15 mg/kg provided 100% clearance rate whereas the MZ suspension with a dose of 20 mg/kg gave only 33.33%.</description><identifier>ISSN: 0168-3659</identifier><identifier>EISSN: 1873-4995</identifier><identifier>DOI: 10.1016/j.jconrel.2007.02.012</identifier><identifier>PMID: 17412443</identifier><identifier>CODEN: JCREEC</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject><![CDATA[Alginate beads ; Alginates - administration & dosage ; Alginates - chemical synthesis ; Alginates - pharmacokinetics ; Animals ; Anti-Infective Agents - administration & dosage ; Anti-Infective Agents - chemical synthesis ; Anti-Infective Agents - pharmacokinetics ; Antibacterial agents ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Biological and medical sciences ; Chemistry, Pharmaceutical ; Delayed-Action Preparations - administration & dosage ; Delayed-Action Preparations - chemical synthesis ; Delayed-Action Preparations - pharmacokinetics ; Drug Delivery Systems - methods ; Drug Evaluation, Preclinical - methods ; Floating drug delivery systems (FDDS) ; Gastric Mucosa - drug effects ; Gastric Mucosa - metabolism ; Gastric Mucosa - microbiology ; Gastric Mucosa - pathology ; General pharmacology ; Glucuronic Acid - administration & dosage ; Glucuronic Acid - chemical synthesis ; Glucuronic Acid - pharmacokinetics ; H. pylori clearance ; Helicobacter Infections - drug therapy ; Helicobacter Infections - metabolism ; Helicobacter Infections - pathology ; Helicobacter pylori ; Helicobacter pylori - drug effects ; Helicobacter pylori - isolation & purification ; Hexuronic Acids - administration & dosage ; Hexuronic Acids - chemical synthesis ; Hexuronic Acids - pharmacokinetics ; Humans ; Local delivery ; Male ; Medical sciences ; Metronidazole ; Metronidazole - administration & dosage ; Metronidazole - chemical synthesis ; Metronidazole - pharmacokinetics ; Mice ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Sustained release]]></subject><ispartof>Journal of controlled release, 2007-06, Vol.119 (2), p.207-214</ispartof><rights>2007 Elsevier B.V.</rights><rights>2007 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c476t-8effd2f76651bf84d347e64ba964637d4a2561e37baff687e4f8d7bd39d139363</citedby><cites>FETCH-LOGICAL-c476t-8effd2f76651bf84d347e64ba964637d4a2561e37baff687e4f8d7bd39d139363</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18791476$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17412443$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ishak, Rania A.H.</creatorcontrib><creatorcontrib>Awad, Gehanne A.S.</creatorcontrib><creatorcontrib>Mortada, Nahed D.</creatorcontrib><creatorcontrib>Nour, Samia A.K.</creatorcontrib><title>Preparation, in vitro and in vivo evaluation of stomach-specific metronidazole-loaded alginate beads as local anti- Helicobacter pylori therapy</title><title>Journal of controlled release</title><addtitle>J Control Release</addtitle><description>Metronidazole (MZ), a common antibacterial drug used in treatment of
H. pylori, was prepared in chitosan-treated alginate beads by the ionotropic gelation method. A (3
×
2
×
2) factorially designed experiment was used in which 3 viscosity-imparting polymers namely, methyl cellulose, carbopol 934P and κ-carrageenan, 2 concentrations (0.2 and 0.4% w/v) of chitosan as encapsulating polymer and 2 concentrations (2.5 and 5% w/w) of the low density magnesium stearate as a floating aid were tested. The drug entrapment efficiency (%), the percent of floating beads and the time for 80% of the drug to be released (
T
80%) were the responses evaluated. The bead formula containing 0.5% κ-carrageenan, 0.4% chitosan and 5% magnesium stearate showed immediate buoyancy, optimum drug entrapment efficiency and extended drug release. The histopathological examination of mice stomachs and
in vivo H. pylori clearance tests were carried out by orally administering MZ floating alginate beads or MZ suspension, to
H. pylori infected mice under fed conditions as a single daily dose for 3 successive days in different doses 5, 10, 15 and 20 mg/kg. The histopathological examination showed that groups receiving MZ in the form of floating alginate beads at doses 10, 15 and 20 mg/kg were better than the corresponding suspension form, regarding eradication of
H. pylori infection. The
in vivo H. pylori clearance tests showed that MZ floating beads with a dose of 15 mg/kg provided 100% clearance rate whereas the MZ suspension with a dose of 20 mg/kg gave only 33.33%.</description><subject>Alginate beads</subject><subject>Alginates - administration & dosage</subject><subject>Alginates - chemical synthesis</subject><subject>Alginates - pharmacokinetics</subject><subject>Animals</subject><subject>Anti-Infective Agents - administration & dosage</subject><subject>Anti-Infective Agents - chemical synthesis</subject><subject>Anti-Infective Agents - pharmacokinetics</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Biological and medical sciences</subject><subject>Chemistry, Pharmaceutical</subject><subject>Delayed-Action Preparations - administration & dosage</subject><subject>Delayed-Action Preparations - chemical synthesis</subject><subject>Delayed-Action Preparations - pharmacokinetics</subject><subject>Drug Delivery Systems - methods</subject><subject>Drug Evaluation, Preclinical - methods</subject><subject>Floating drug delivery systems (FDDS)</subject><subject>Gastric Mucosa - drug effects</subject><subject>Gastric Mucosa - metabolism</subject><subject>Gastric Mucosa - microbiology</subject><subject>Gastric Mucosa - pathology</subject><subject>General pharmacology</subject><subject>Glucuronic Acid - administration & dosage</subject><subject>Glucuronic Acid - chemical synthesis</subject><subject>Glucuronic Acid - pharmacokinetics</subject><subject>H. pylori clearance</subject><subject>Helicobacter Infections - drug therapy</subject><subject>Helicobacter Infections - metabolism</subject><subject>Helicobacter Infections - pathology</subject><subject>Helicobacter pylori</subject><subject>Helicobacter pylori - drug effects</subject><subject>Helicobacter pylori - isolation & purification</subject><subject>Hexuronic Acids - administration & dosage</subject><subject>Hexuronic Acids - chemical synthesis</subject><subject>Hexuronic Acids - pharmacokinetics</subject><subject>Humans</subject><subject>Local delivery</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Metronidazole</subject><subject>Metronidazole - administration & dosage</subject><subject>Metronidazole - chemical synthesis</subject><subject>Metronidazole - pharmacokinetics</subject><subject>Mice</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Sustained release</subject><issn>0168-3659</issn><issn>1873-4995</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><recordid>eNqFkcGO1SAUhhujca6jj6BhoytboVBoV2YyUcdkEl3ompzCweGGlgq9N7m-hK8s420yy1kRku8_cP6vql4z2jDK5Id9szdxThiallLV0LahrH1S7ViveC2GoXta7QrX11x2w0X1Iuc9pbTjQj2vLpgSrBWC76q_3xMukGD1cX5P_EyOfk2RwGzPl2MkeIRw-A-Q6Ehe4wTmrs4LGu-8IROWwOwt_IkB6xDBoiUQfvkZViQjgs0EMgnRQChzV1-TGwzexBHMiokspxCTJ-sdJlhOL6tnDkLGV9t5Wf38_OnH9U19--3L1-ur29oIJde6R-ds65SUHRtdL2zZC6UYYZBCcmUFtJ1kyNUIzsleoXC9VaPlg2V84JJfVu_Oc5cUfx8wr3ry2WAIMGM8ZK1o16qhHR4F2SBZT7koYHcGTYo5J3R6SX6CdNKM6ntleq83ZfpemaatLspK7s32wGGc0D6kNkcFeLsBkEuHLsFsfH7gejWwUkrhPp45LL0dPSadjcfZoPUJzapt9I985R-n3boh</recordid><startdate>20070601</startdate><enddate>20070601</enddate><creator>Ishak, Rania A.H.</creator><creator>Awad, Gehanne A.S.</creator><creator>Mortada, Nahed D.</creator><creator>Nour, Samia A.K.</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>7QL</scope><scope>7QO</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20070601</creationdate><title>Preparation, in vitro and in vivo evaluation of stomach-specific metronidazole-loaded alginate beads as local anti- Helicobacter pylori therapy</title><author>Ishak, Rania A.H. ; Awad, Gehanne A.S. ; Mortada, Nahed D. ; Nour, Samia A.K.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c476t-8effd2f76651bf84d347e64ba964637d4a2561e37baff687e4f8d7bd39d139363</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Alginate beads</topic><topic>Alginates - administration & dosage</topic><topic>Alginates - chemical synthesis</topic><topic>Alginates - pharmacokinetics</topic><topic>Animals</topic><topic>Anti-Infective Agents - administration & dosage</topic><topic>Anti-Infective Agents - chemical synthesis</topic><topic>Anti-Infective Agents - pharmacokinetics</topic><topic>Antibacterial agents</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Biological and medical sciences</topic><topic>Chemistry, Pharmaceutical</topic><topic>Delayed-Action Preparations - administration & dosage</topic><topic>Delayed-Action Preparations - chemical synthesis</topic><topic>Delayed-Action Preparations - pharmacokinetics</topic><topic>Drug Delivery Systems - methods</topic><topic>Drug Evaluation, Preclinical - methods</topic><topic>Floating drug delivery systems (FDDS)</topic><topic>Gastric Mucosa - drug effects</topic><topic>Gastric Mucosa - metabolism</topic><topic>Gastric Mucosa - microbiology</topic><topic>Gastric Mucosa - pathology</topic><topic>General pharmacology</topic><topic>Glucuronic Acid - administration & dosage</topic><topic>Glucuronic Acid - chemical synthesis</topic><topic>Glucuronic Acid - pharmacokinetics</topic><topic>H. pylori clearance</topic><topic>Helicobacter Infections - drug therapy</topic><topic>Helicobacter Infections - metabolism</topic><topic>Helicobacter Infections - pathology</topic><topic>Helicobacter pylori</topic><topic>Helicobacter pylori - drug effects</topic><topic>Helicobacter pylori - isolation & purification</topic><topic>Hexuronic Acids - administration & dosage</topic><topic>Hexuronic Acids - chemical synthesis</topic><topic>Hexuronic Acids - pharmacokinetics</topic><topic>Humans</topic><topic>Local delivery</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Metronidazole</topic><topic>Metronidazole - administration & dosage</topic><topic>Metronidazole - chemical synthesis</topic><topic>Metronidazole - pharmacokinetics</topic><topic>Mice</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Sustained release</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ishak, Rania A.H.</creatorcontrib><creatorcontrib>Awad, Gehanne A.S.</creatorcontrib><creatorcontrib>Mortada, Nahed D.</creatorcontrib><creatorcontrib>Nour, Samia A.K.</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>Bacteriology Abstracts (Microbiology B)</collection><collection>Biotechnology Research 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>MEDLINE - Academic</collection><jtitle>Journal of controlled release</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ishak, Rania A.H.</au><au>Awad, Gehanne A.S.</au><au>Mortada, Nahed D.</au><au>Nour, Samia A.K.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation, in vitro and in vivo evaluation of stomach-specific metronidazole-loaded alginate beads as local anti- Helicobacter pylori therapy</atitle><jtitle>Journal of controlled release</jtitle><addtitle>J Control Release</addtitle><date>2007-06-01</date><risdate>2007</risdate><volume>119</volume><issue>2</issue><spage>207</spage><epage>214</epage><pages>207-214</pages><issn>0168-3659</issn><eissn>1873-4995</eissn><coden>JCREEC</coden><abstract>Metronidazole (MZ), a common antibacterial drug used in treatment of
H. pylori, was prepared in chitosan-treated alginate beads by the ionotropic gelation method. A (3
×
2
×
2) factorially designed experiment was used in which 3 viscosity-imparting polymers namely, methyl cellulose, carbopol 934P and κ-carrageenan, 2 concentrations (0.2 and 0.4% w/v) of chitosan as encapsulating polymer and 2 concentrations (2.5 and 5% w/w) of the low density magnesium stearate as a floating aid were tested. The drug entrapment efficiency (%), the percent of floating beads and the time for 80% of the drug to be released (
T
80%) were the responses evaluated. The bead formula containing 0.5% κ-carrageenan, 0.4% chitosan and 5% magnesium stearate showed immediate buoyancy, optimum drug entrapment efficiency and extended drug release. The histopathological examination of mice stomachs and
in vivo H. pylori clearance tests were carried out by orally administering MZ floating alginate beads or MZ suspension, to
H. pylori infected mice under fed conditions as a single daily dose for 3 successive days in different doses 5, 10, 15 and 20 mg/kg. The histopathological examination showed that groups receiving MZ in the form of floating alginate beads at doses 10, 15 and 20 mg/kg were better than the corresponding suspension form, regarding eradication of
H. pylori infection. The
in vivo H. pylori clearance tests showed that MZ floating beads with a dose of 15 mg/kg provided 100% clearance rate whereas the MZ suspension with a dose of 20 mg/kg gave only 33.33%.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>17412443</pmid><doi>10.1016/j.jconrel.2007.02.012</doi><tpages>8</tpages></addata></record> |
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ispartof | Journal of controlled release, 2007-06, Vol.119 (2), p.207-214 |
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language | eng |
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source | ScienceDirect Journals |
subjects | Alginate beads Alginates - administration & dosage Alginates - chemical synthesis Alginates - pharmacokinetics Animals Anti-Infective Agents - administration & dosage Anti-Infective Agents - chemical synthesis Anti-Infective Agents - pharmacokinetics Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Chemistry, Pharmaceutical Delayed-Action Preparations - administration & dosage Delayed-Action Preparations - chemical synthesis Delayed-Action Preparations - pharmacokinetics Drug Delivery Systems - methods Drug Evaluation, Preclinical - methods Floating drug delivery systems (FDDS) Gastric Mucosa - drug effects Gastric Mucosa - metabolism Gastric Mucosa - microbiology Gastric Mucosa - pathology General pharmacology Glucuronic Acid - administration & dosage Glucuronic Acid - chemical synthesis Glucuronic Acid - pharmacokinetics H. pylori clearance Helicobacter Infections - drug therapy Helicobacter Infections - metabolism Helicobacter Infections - pathology Helicobacter pylori Helicobacter pylori - drug effects Helicobacter pylori - isolation & purification Hexuronic Acids - administration & dosage Hexuronic Acids - chemical synthesis Hexuronic Acids - pharmacokinetics Humans Local delivery Male Medical sciences Metronidazole Metronidazole - administration & dosage Metronidazole - chemical synthesis Metronidazole - pharmacokinetics Mice Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Sustained release |
title | Preparation, in vitro and in vivo evaluation of stomach-specific metronidazole-loaded alginate beads as local anti- Helicobacter pylori therapy |
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